• Lou, K, Steri V, Ge AY, Hwang YC, Yogodzinski CH, Shkedi AR, Choi ALM, Mitchell DC, Swaney DL, Hann B, Gordan JD, Shokat KM, Gilbert LA. KRASG12C inhibition produces a driver-limited state revealing collateral dependencies. Sci Signal. 2019 May 28; 12(583).

    (PMID 31138768) (PDF)

  • Hernández-Ortega S, Sánchez-Botet A, Quandt E, Masip N, Gasa L, Verde G, Jiménez J, Levin RS, Rutaganira FU, Burlingame AL, Wolfgeher D, Ribeiro MPC, Kron SJ, Shokat KM, Clotet J. Phosphoregulation of the oncogenic protein regulator of cytokinesis 1 (PRC1) by the atypical CDK16/CCNY complex. Exp Mol Med. 2019 Apr 16; 51(4):44.

    (PMID 30992425) (PDF)

  • Moss SM, Taylor IR, Ruggero D, Gestwicki JE, Shokat KM, Mukherjee S. A legionella pneumophila kinase phosphorylates the Hsp70 chaperone family to inhibit eukaryotic protein synthesis. Cell Host Microbe. 2019 Mar 13; 25(3):454-462.e6.

    (PMID 30827827)

  • Katsuno Y, Meyer DS, Zhang Z, Shokat KM, Akhurst RJ, Miyazono K, Derynck R. Chronic TGF-ß exposure drives stabilized EMT, tumor stemness, and cancer drug resistance with vulnerability to bitopic mTOR inhibition. Sci Signal. 2019 Feb 26; 12(570).

    (PMID 30808819) (PDF)

  • Wong AW, Urisman A, Burlingame AL, Shokat KM. Chemically reprogramming the phospho-transfer reaction to crosslink protein kinases to their substrates. Protein Sci. 2019 Jan 13.

    (PMID 30636329) (PDF)

  • Chamberlain CE, German MS, Yang K, Wang J, VanBrocklin H, Regan M, Shokat KM, Ducker GS, Kim GE, Hann B, Donner DB, Warren RS, Venook AP, Bergsland EK, Lee D, Wang Y, Nakakura EK. A patient-derived xenograft model of pancreatic neuroendocrine tumors identifies sapanisertib as a possible new treatment for everolimus-resistant tumors. Mol Cancer Ther. 2018 Dec; 17(12):2702-2709.

    (PMID 30254185) (PDF)

  • Ocasio CA, Warkentin AA, McIntyre PJ, Barkovich KJ, Vesely C, Spencer J, Shokat KM, Bayliss R. Type II kinase inhibitors targeting cys-gatekeeper kinases display orthogonality with wild type and ala/gly-gatekeeper kinases. ACS Chem Biol. 2018 Oct 19; 13(10):2956-2965.

    (PMID 30239186) (PDF)

  • Barkovich KJ, Moore MK, Hu Q, Shokat KM. Chemical genetic inhibition of DEAD-box proteins using covalent complementarity. Nucleic Acids Res. 2018 Sep 28; 46(17):8689-8699.

    (PMID 30102385) (PDF)

  • Chorba JS, Galvan AM, Shokat KM. A high-throughput luciferase sssay to rvaluate proteolysis of the dingle-turnover protease PCSK9. J Vis Exp. 2018 Aug 28; (138).

    (PMID 30222160) (PDF)

  • Donnella HJ, Webber JT, Levin RS, Camarda R, Momcilovic O, Bayani N, Shah KN, Korkola JE, Shokat KM, Goga A, Gordan JD, Bandyopadhyay S. Kinome rewiring reveals AURKA limits PI3K-pathway inhibitor efficacy in breast cancer. Nat Chem Biol. 2018 Aug; 14(8):768-777.

    (PMID 29942081) (PDF)

  • Ksionda O, Mues M, Wandler AM, Donker L, Tenhagen M, Jun J, Ducker GS, Matlawska-Wasowska K, Shannon K, Shokat KM, Roose JP. Comprehensive analysis of T cell leukemia signals reveals heterogeneity in the PI3 kinase-Akt pathway and limitations of PI3 kinase inhibitors as monotherapy. PLoS One. 2018 May 25; 13(5):e0193849.

    (PMID 29799846) (PDF)

  • Hu Q, Shokat KM. Disease-causing mutations in the G protein gas subvert the roles of GDP and GTP. Cell. 2018 May 17; 173(5):1254-1264.e11.

    (PMID 29628140) (PDF)

  • Chorba JS, Galvan AM, Shokat KM. Stepwise processing analyses of the single-turnover PCSK9 protease reveal its substrate sequence specificity and link clinical genotype to lipid phenotype. J Biol Chem. 2018 May 04; 293(18):6692.

    (PMID 29728531) (PDF)

  • Morisot N, Novotny CJ, Shokat KM, Ron D. A new generation of mTORC1 inhibitor attenuates alcohol intake and reward in mice. Addict Biol. 2018 Mar; 23(2):713-722.

    (PMID 28681511) (PDF)

  • Nnadi CI, Jenkins ML, Gentile DR, Bateman LA, Zaidman D, Balius TE, Nomura DK, Burke JE, Shokat KM, London N. Novel K-Ras G12C switch-II covalent binders destabilize Ras and accelerate nucleotide exchange. J Chem Inf Model. 2018 Feb 26; 58(2):464-471.

    (PMID 29320178) (PDF)

  • Chorba JS, Galvan AM, Shokat KM. Stepwise processing analyses of the single-turnover PCSK9 protease reveal its substrate sequence specificity and link clinical genotype to lipid phenotype. J Biol Chem. 2018 Feb 09; 293(6):1875-1886.

    (PMID 29259136) (PDF)

  • Rutaganira FU, Barks J, Dhason MS, Wang Q, Lopez MS, Long S, Radke JB, Jones NG, Maddirala AR, Janetka JW, El Bakkouri M, Hui R, Shokat KM, Sibley LD. Inhibition of calcium dependent protein kinase 1 (CDPK1) by pyrazolopyrimidine analogs decreases establishment and reoccurrence of central nervous system disease by toxoplasma gondii. J Med Chem. 2017 Dec 28; 60(24):9976-9989.

    (PMID 28933846) (PDF)

  • Gentile DR, Rathinaswamy MK, Jenkins ML, Moss SM, Siempelkamp BD, Renslo AR, Burke JE, Shokat KM. Ras binder induces a modified switch-II pocket in GTP and GDP states. Cell Chem Biol. 2017 Dec 21; 24(12):1455-1466.e14.

    (PMID 29033317) (PDF)

  • Orr AL, Rutaganira FU, de Roulet D, Huang EJ, Hertz NT, Shokat KM, Nakamura K. Long-term oral kinetin does not protect against a-synuclein-induced neurodegeneration in rodent models of Parkinson’s disease. Neurochem Int. 2017 Oct; 109:106-116.

    (PMID 28434973) (PDF)

  • Dang CV, Reddy EP, Shokat KM, Soucek L. Drugging the ‘undruggable’ cancer targets. Nat Rev Cancer. 2017 Aug; 17(8):502-508.

    (PMID 28643779) (PDF)

  • Hoppmann C, Wong A, Yang B, Li S, Hunter T, Shokat KM, Wang L. Site-specific incorporation of phosphotyrosine using an expanded genetic code. Nat Chem Biol. 2017 Aug; 13(8):842-844.

    (PMID 28604697) (PDF)

  • Novotny CJ, Hamilton GL, McCormick F, Shokat KM. Farnesyltransferase-mediated delivery of a covalent inhibitor overcomes alternative prenylation to mislocalize K-ras. ACS Chem Biol. 2017 Jul 21; 12(7):1956-1962.

    (PMID 28530791) (PDF)

  • McGregor LM, Jenkins ML, Kerwin C, Burke JE, Shokat KM. Expanding the scope of electrophiles capable of targeting K-ras oncogenes. Biochemistry. 2017 Jun 27; 56(25):3178-3183.

    (PMID 28621541) (PDF)

  • Plenker D, Riedel M, Brägelmann J, Dammert MA, Chauhan R, Knowles PP, Lorenz C, Keul M, Bührmann M, Pagel O, Tischler V, Scheel AH, Schütte D, Song Y, Stark J, Mrugalla F, Alber Y, Richters A, Engel J, Leenders F, Heuckmann JM, Wolf J, Diebold J, Pall G, Peifer M, Aerts M, Gevaert K, Zahedi RP, Buettner R, Shokat KM, McDonald NQ, Kast SM, Gautschi O, Thomas RK, Sos ML. Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors. Sci Transl Med. 2017 Jun 14; 9(394).

    (PMID 28615362) (PDF)

  • Kharas MG, Janes MR, Scarfone VM, Lilly MB, Knight ZA, Shokat KM, Fruman DA. Ablation of PI3K blocks BCR-ABL leukemogenesis in mice, and a dual PI3K/mTOR inhibitor prevents expansion of human BCR-ABL+ leukemia cells. J Clin Invest. 2017 Jun 01; 127(6):2438.

    (PMID 28569734) (PDF)

  • Reed DE, Shokat KM. INPP4B and PTEN loss leads to PI-3,4-P2 accumulation and inhibition of PI3K in TNBC. Mol Cancer Res. 2017 Jun; 15(6):765-775.

    (PMID 28196852) (PDF)

  • Liu KH, Niu Y, Konishi M, Wu Y, Du H, Sun Chung H, Li L, Boudsocq M, McCormack M, Maekawa S, Ishida T, Zhang C, Shokat K, Yanagisawa S, Sheen J. Discovery of nitrate-CPK-NLP signalling in central nutrient-growth networks. Nature. 2017 May 18; 545(7654):311-316.

    (PMID 28489820) (PDF)

  • Fan Q, Aksoy O, Wong RA, Ilkhanizadeh S, Novotny CJ, Gustafson WC, Truong AY, Cayanan G, Simonds EF, Haas-Kogan D, Phillips JJ, Nicolaides T, Okaniwa M, Shokat KM, Weiss WA. A kinase inhibitor targeted to mTORC1 drives regression in glioblastoma. Cancer Cell. 2017 Mar 13; 31(3):424-435.

    (PMID 28292440) (PDF)

  • Urisman A, Levin RS, Gordan JD, Webber JT, Hernandez H, Ishihama Y, Shokat KM, Burlingame AL. An optimized chromatographic strategy for multiplexing in parallel reaction monitoring mass spectrometry: Insights from quantitation of activated kinases. Mol Cell Proteomics. 2017 Feb; 16(2):265-277.

    (PMID 27940637) (PDF)

  • Jo A, Choi TG, Jo YH, Jyothi KR, Nguyen MN, Kim JH, Lim S, Shahid M, Akter S, Lee S, Lee KH, Kim W, Cho H, Lee J, Shokat KM, Yoon KS, Kang I, Ha J, Kim SS. Inhibition of carbonyl reductase 1 safely improves the efficacy of doxorubicin in breast cancer treatment. Antioxid Redox Signal. 2017 Jan 10; 26(2):70-83.

    (PMID 27357096) (PDF)

  • Uchida Y, Rutaganira FU, Jullié D, Shokat KM, von Zastrow M. Endosomal phosphatidylinositol 3-kinase Is essential for canonical GPCR signaling. Mol Pharmacol. 2017 Jan; 91(1):65-73.

    (PMID 27821547) (PDF)

  • Lazarus MB, Levin RS, Shokat KM. Discovery of new substrates of the elongation factor-2 kinase suggests a broader role in the cellular nutrient response. Cell Signal. 2017 Jan; 29:78-83.

    (PMID 27760376) (PDF)

  • Novotny CJ, Pollari S, Park JH, Lemmon MA, Shen W, Shokat KM. Overcoming resistance to HER2 inhibitors through state-specific kinase binding. Nat Chem Biol. 2016 Nov; 12(11):923-930.

    (PMID 27595329) (PDF)

  • Ostrem JM, Shokat KM. Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design. Nat Rev Drug Discov. 2016 Nov; 15(11):771-785.

    (PMID 27469033) (PDF)

  • Kostic M, Crews CM, Hertweck C, Shokat K, Suga H. From powerful review articles to research breakthroughs. Cell Chem Biol. 2016 Aug 18; 23(8):883-4.

    (PMID 27541190) (PDF)

  • Levin RS, Hertz NT, Burlingame AL, Shokat KM, Mukherjee S. Innate immunity kinase TAK1 phosphorylates Rab1 on a hotspot for posttranslational modifications by host and pathogen. Proc Natl Acad Sci U S A. 2016 Aug 16; 113(33):E4776-83.

    (PMID 27482120) (PDF)

  • Miller RE, Brough R, Bajrami I, Williamson CT, McDade S, Campbell J, Kigozi A, Rafiq R, Pemberton H, Natrajan R, Joel J, Astley H, Mahoney C, Moore JD, Torrance C, Gordan JD, Webber JT, Levin RS, Shokat KM, Bandyopadhyay S, Lord CJ, Ashworth A. Synthetic lethal targeting of ARID1A-mutant ovarian clear cell tumors with dasatinib. Mol Cancer Ther. 2016 Jul; 15(7):1472-84.

    (PMID 27364904) (PDF)

  • Saha SK, Gordan JD, Kleinstiver BP, Vu P, Najem MS, Yeo JC, Shi L, Kato Y, Levin RS, Webber JT, Damon LJ, Egan RK, Greninger P, McDermott U, Garnett MJ, Jenkins RL, Rieger-Christ KM, Sullivan TB, Hezel AF, Liss AS, Mizukami Y, Goyal L, Ferrone CR, Zhu AX, Joung JK, Shokat KM, Benes CH, Bardeesy N. Isocitrate dehydrogenase mutations confer dasatinib hypersensitivity and SRC dependence in intrahepatic cholangiocarcinoma. Cancer Discov. 2016 Jul; 6(7):727-39.

    (PMID 27231123) (PDF)

  • Rodrik-Outmezguine VS, Okaniwa M, Yao Z, Novotny CJ, McWhirter C, Banaji A, Won H, Wong W, Berger M, de Stanchina E, Barratt DG, Cosulich S, Klinowska T, Rosen N, Shokat KM. Overcoming mTOR resistance mutations with a new-generation mTOR inhibitor. Nature. 2016 Jun 09; 534(7606):272-6.

    (PMID 27279227) (PDF)

  • Tabaei SR, Guo F, Rutaganira FU, Vafaei S, Choong I, Shokat KM, Glenn JS, Cho NJ. Multistep compositional remodeling of supported lipid membranes by interfacially active phosphatidylinositol kinases. Anal Chem. 2016 May 17; 88(10):5042-5.

    (PMID 27118725) (PDF)

  • Lee JK, Phillips JW, Smith BA, Park JW, Stoyanova T, McCaffrey EF, Baertsch R, Sokolov A, Meyerowitz JG, Mathis C, Cheng D, Stuart JM, Shokat KM, Gustafson WC, Huang J, Witte ON. N-Myc drives neuroendocrine prostate cancer initiated from human prostate epithelial cells. Cancer Cell. 2016 Apr 11; 29(4):536-547.

    (PMID 27050099) (PDF)

  • Fowler ML, McPhail JA, Jenkins ML, Masson GR, Rutaganira FU, Shokat KM, Williams RL, Burke JE. Using hydrogen deuterium exchange mass spectrometry to engineer optimized constructs for crystallization of protein complexes: Case study of PI4KIIIß with Rab11. Protein Sci. 2016 Apr; 25(4):826-39.

    (PMID 26756197) (PDF)

  • Floor SN, Barkovich KJ, Condon KJ, Shokat KM, Doudna JA. Analog sensitive chemical inhibition of the DEAD-box protein DDX3. Protein Sci. 2016 Mar; 25(3):638-49.

    (PMID 26650549) (PDF)

  • Kostic M, Crews CM, Hertweck C, Shokat K, Suga H. Our advisors, our ambassadors, our editorial board members. Cell Chem Biol. 2016 Mar 17; 23(3):311-2.

    (PMID 26991096) (PDF)

  • Rutaganira FU, Fowler ML, McPhail JA, Gelman MA, Nguyen K, Xiong A, Dornan GL, Tavshanjian B, Glenn JS, Shokat KM, Burke JE. Design and structural characterization of potent and selective inhibitors of phosphatidylinositol 4 kinase IIIß. J Med Chem. 2016 Mar 10; 59(5):1830-9.

    (PMID 26885694) (PDF)

  • Kostic M, Crews CM, Hertweck C, Shokat K, Suga H. Voices of chemical biology: Charting the next decade. Cell Chem Biol. 2016 Feb 18; 23(2):199.

    (PMID 26971865) (PDF)

  • Kostic M, Crews CM, Hertweck C, Shokat K, Suga H. Cell chemical biology: Home of exciting chemical biology. Cell Chem Biol. 2016 Jan 21; 23(1):1-2.

    (PMID 26933730) (PDF)

  • Sansó M, Levin RS, Lipp JJ, Wang VY, Greifenberg AK, Quezada EM, Ali A, Ghosh A, Larochelle S, Rana TM, Geyer M, Tong L, Shokat KM, Fisher RP. P-TEFb regulation of transcription termination factor Xrn2 revealed by a chemical genetic screen for Cdk9 substrates. Genes Dev. 2016 Jan 01; 30(1):117-31.

    (PMID 26728557) (PDF)

  • Kuhlenschmidt TB, Rutaganira FU, Long S, Tang K, Shokat KM, Kuhlenschmidt MS, Sibley LD. Inhibition of calcium-dependent protein kinase 1 (CDPK1) in vitro by pyrazolopyrimidine derivatives does not correlate with sensitivity of cryptosporidium parvum growth in cell culture. Antimicrob Agents Chemother. 2016 Jan; 60(1):570-9.

    (PMID 26552986) (PDF)

  • Costa HA, Leitner MG, Sos ML, Mavrantoni A, Rychkova A, Johnson JR, Newton BW, Yee MC, De La Vega FM, Ford JM, Krogan NJ, Shokat KM, Oliver D, Halaszovich CR, Bustamante CD. Discovery and functional characterization of a neomorphic PTEN mutation. Proc Natl Acad Sci U S A. 2015 Nov 10; 112(45):13976-81.

    (PMID 26504226) (PDF)

  • Schaffer BE, Levin RS, Hertz NT, Maures TJ, Schoof ML, Hollstein PE, Benayoun BA, Banko MR, Shaw RJ, Shokat KM, Brunet A. Identification of AMPK phosphorylation sites reveals a network of proteins involved in cell invasion and facilitates large-scale substrate prediction. Cell Metab. 2015 Nov 03; 22(5):907-21.

    (PMID 26456332) (PDF)

  • Lazarus MB, Shokat KM. Discovery and structure of a new inhibitor scaffold of the autophagy initiating kinase ULK1. Bioorg Med Chem. 2015 Sep 01; 23(17):5483-8.

    (PMID 26275681) (PDF)

  • Manz BN, Tan YX, Courtney AH, Rutaganira F, Palmer E, Shokat KM, Weiss A. Small molecule inhibition of Csk alters affinity recognition by T cells. Elife. 2015 Aug 24; 4.

    (PMID 26302204) (PDF)

  • Lipp JJ, Marvin MC, Shokat KM, Guthrie C. SR protein kinases promote splicing of nonconsensus introns. Nat Struct Mol Biol. 2015 Aug; 22(8):611-7.

    (PMID 26167880) (PDF)

  • Friedel P, Kahle KT, Zhang J, Hertz N, Pisella LI, Buhler E, Schaller F, Duan J, Khanna AR, Bishop PN, Shokat KM, Medina I. WNK1-regulated inhibitory phosphorylation of the KCC2 cotransporter maintains the depolarizing action of GABA in immature neurons. Sci Signal. 2015 Jun 30; 8(383):ra65.

    (PMID 26126716) (PDF)

  • Mendez AS, Alfaro J, Morales-Soto MA, Dar AC, McCullagh E, Gotthardt K, Li H, Acosta-Alvear D, Sidrauski C, Korennykh AV, Bernales S, Shokat KM, Walter P. Endoplasmic reticulum stress-independent activation of unfolded protein response kinases by a small molecule ATP-mimic. Elife. 2015 May 19; 4.

    (PMID 25986605) (PDF)

  • Cage TA, Chanthery Y, Chesler L, Grimmer M, Knight Z, Shokat K, Weiss WA, Gustafson WC. Downregulation of MYCN through PI3K inhibition in mouse models of pediatric neural cancer. Front Oncol. 2015 May 12; 5:111.

    (PMID 26029667) (PDF)

  • Martin H, Shales M, Fernandez-Piñar P, Wei P, Molina M, Fiedler D, Shokat KM, Beltrao P, Lim W, Krogan NJ. Differential genetic interactions of yeast stress response MAPK pathways. Mol Syst Biol. 2015 Apr 17; 11(4):800.

    (PMID 25888283) (PDF)

  • Bailey FP, Byrne DP, Oruganty K, Eyers CE, Novotny CJ, Shokat KM, Kannan N, Eyers PA. The Tribbles 2 (TRB2) pseudokinase binds to ATP and autophosphorylates in a metal-independent manner. Biochem J. 2015 Apr 01; 467(1):47-62.

    (PMID 25583260) (PDF)

  • Li N, Maly DJ, Chanthery YH, Sirkis DW, Nakamura JL, Berger MS, James CD, Shokat KM, Weiss WA, Persson AI. Radiotherapy followed by aurora kinase inhibition targets tumor-propagating cells in human glioblastoma. Mol Cancer Ther. 2015 Feb; 14(2):419-28.

    (PMID 25522764) (PDF)

  • Martins MM, Zhou AY, Corella A, Horiuchi D, Yau C, Rakshandehroo T, Gordan JD, Levin RS, Johnson J, Jascur J, Shales M, Sorrentino A, Cheah J, Clemons PA, Shamji AF, Schreiber SL, Krogan NJ, Shokat KM, McCormick F, Goga A, Bandyopadhyay S. Linking tumor mutations to drug responses via a quantitative chemical-genetic interaction map. Cancer Discov. 2015 Feb; 5(2):154-67.

    (PMID 25501949) (PDF)

  • Lazarus MB, Novotny CJ, Shokat KM. Structure of the human autophagy initiating kinase ULK1 in complex with potent inhibitors. ACS Chem Biol. 2015 Jan 16; 10(1):257-61.

    (PMID 25551253) (PDF)

  • Reed DE, Shokat KM. Targeting osteosarcoma. Proc Natl Acad Sci U S A. 2014 Dec 23; 111(51):18100-1.

    (PMID 25512494) (PDF)

  • Warkentin AA, Lopez MS, Lasater EA, Lin K, He BL, Leung AY, Smith CC, Shah NP, Shokat KM. Overcoming myelosuppression due to synthetic lethal toxicity for FLT3-targeted acute myeloid leukemia therapy. Elife. 2014 Dec 22; 3.

    (PMID 25531068) (PDF)

  • Ultanir SK, Yadav S, Hertz NT, Oses-Prieto JA, Claxton S, Burlingame AL, Shokat KM, Jan LY, Jan YN. MST3 kinase phosphorylates TAO1/2 to enable Myosin Va function in promoting spine synapse development. Neuron. 2014 Dec 03; 84(5):968-82.

    (PMID 25456499) (PDF)

  • Chorba JS, Shokat KM. The proprotein convertase subtilisin/kexin type 9 (PCSK9) active site and cleavage sequence differentially regulate protein secretion from proteolysis. J Biol Chem. 2014 Oct 17; 289(42):29030-43.

    (PMID 25210046) (PDF)

  • Mantilla CB, Stowe JM, Sieck DC, Ermilov LG, Greising SM, Zhang C, Shokat KM, Sieck GC. TrkB kinase activity maintains synaptic function and structural integrity at adult neuromuscular junctions. J Appl Physiol. 2014 Oct 15; 117(8):910-20.

    (PMID 25170066) (PDF)

  • Parker N, Falk H, Singh D, Fidaleo A, Smith B, Lopez MS, Shokat KM, Wright WW. Responses to glial cell line-derived neurotrophic factor change in mice as spermatogonial stem cells form progenitor spermatogonia which replicate and give rise to more differentiated progeny. Biol Reprod. 2014 Oct; 91(4):92.

    (PMID 25165119) (PDF)

  • Crews C, Hertweck C, Shokat K, Suga H, Kostic M. Reflecting on the past and looking forward to the future of bridging chemistry and biology. Chem Biol. 2014 Sep 18; 21(9):1035-6.

    (PMID 25237850) (PDF)

  • Gustafson WC, Meyerowitz JG, Nekritz EA, Chen J, Benes C, Charron E, Simonds EF, Seeger R, Matthay KK, Hertz NT, Eilers M, Shokat KM, Weiss WA. Drugging MYCN through an allosteric transition in Aurora kinase A. Cancer Cell. 2014 Sep 08; 26(3):414-427.

    (PMID 25175806) (PDF)

  • Au-Yeung BB, Zikherman J, Mueller JL, Ashouri JF, Matloubian M, Cheng DA, Chen Y, Shokat KM, Weiss A. A sharp T-cell antigen receptor signaling threshold for T-cell proliferation. Proc Natl Acad Sci U S A. 2014 Sep 02; 111(35):E3679-88.

    (PMID 25136127) (PDF)

  • Guo T, Marmol P, Moliner A, Björnholm M, Zhang C, Shokat KM, Ibanez CF. Adipocyte ALK7 links nutrient overload to catecholamine resistance in obesity. Elife. 2014 Aug 25; 3:e03245.

    (PMID 25161195) (PDF)

  • Sos ML, Levin RS, Gordan JD, Oses-Prieto JA, Webber JT, Salt M, Hann B, Burlingame AL, McCormick F, Bandyopadhyay S, Shokat KM. Oncogene mimicry as a mechanism of primary resistance to BRAF inhibitors. Cell Rep. 2014 Aug 21; 8(4):1037-48.

    (PMID 25127139) (PDF)

  • Chen L, Shu Y, Liang X, Chen EC, Yee SW, Zur AA, Li S, Xu L, Keshari KR, Lin MJ, Chien HC, Zhang Y, Morrissey KM, Liu J, Ostrem J, Younger NS, Kurhanewicz J, Shokat KM, Ashrafi K, Giacomini KM. OCT1 is a high-capacity thiamine transporter that regulates hepatic steatosis and is a target of metformin. Proc Natl Acad Sci U S A. 2014 Jul 08; 111(27):9983-8.

    (PMID 24961373) (PDF)

  • Au-Yeung BB, Melichar HJ, Ross JO, Cheng DA, Zikherman J, Shokat KM, Robey EA, Weiss A. Quantitative and temporal requirements revealed for Zap70 catalytic activity during T cell development. Nat Immunol. 2014 Jul; 15(7):687-94.

    (PMID 24908390) (PDF)

  • Burke JE, Inglis AJ, Perisic O, Masson GR, McLaughlin SH, Rutaganira F, Shokat KM, Williams RL. Structures of PI4KIIIß complexes show simultaneous recruitment of Rab11 and its effectors. Science. 2014 May 30; 344(6187):1035-8.

    (PMID 24876499) (PDF)

  • Riel-Mehan MM, Shokat KM. A crosslinker based on a tethered electrophile for mapping kinase-substrate networks. Chem Biol. 2014 May 22; 21(5):585-90.

    (PMID 24746561) (PDF)

  • Ducker GS, Atreya CE, Simko JP, Hom YK, Matli MR, Benes CH, Hann B, Nakakura EK, Bergsland EK, Donner DB, Settleman J, Shokat KM, Warren RS. Incomplete inhibition of phosphorylation of 4E-BP1 as a mechanism of primary resistance to ATP-competitive mTOR inhibitors. Oncogene. 2014 Mar 20; 33(12):1590-600.

    (PMID 23542178) (PDF)

  • Tan YX, Manz BN, Freedman TS, Zhang C, Shokat KM, Weiss A. Inhibition of the kinase Csk in thymocytes reveals a requirement for actin remodeling in the initiation of full TCR signaling. Nat Immunol. 2014 Feb; 15(2):186-94.

    (PMID 24317039) (PDF)

  • Davies JM, Robinson AE, Cowdrey C, Mummaneni PV, Ducker GS, Shokat KM, Bollen A, Hann B, Phillips JJ. Generation of a patient-derived chordoma xenograft and characterization of the phosphoproteome in a recurrent chordoma. J Neurosurg. 2014 Feb; 120(2):331-6.

    (PMID 24286145) (PDF)

  • Shokat KM. Methods in Enzymology. Protein kinase inhibitors in research and medicine. Preface. Methods Enzymol. 2014; 548:xi-xii.

    (PMID 25399648) (PDF)

  • Lopez MS, Kliegman JI, Shokat KM. The logic and design of analog-sensitive kinases and their small molecule inhibitors. Methods Enzymol. 2014; 548:189-213.

    (PMID 25399647) (PDF)

  • Kliegman JI, Fiedler D, Ryan CJ, Xu YF, Su XY, Thomas D, Caccese MC, Cheng A, Shales M, Rabinowitz JD, Krogan NJ, Shokat KM. Chemical genetics of rapamycin-insensitive TORC2 in S. cerevisiae. Cell Rep. 2013 Dec 26; 5(6):1725-36.

    (PMID 24360963) (PDF)

  • Lopez MS, Choy JW, Peters U, Sos ML, Morgan DO, Shokat KM. Staurosporine-derived inhibitors broaden the scope of analog-sensitive kinase technology. J Am Chem Soc. 2013 Dec 04; 135(48):18153-9.

    (PMID 24171479) (PDF)

  • Diaz-Flores E, Goldschmidt H, Depeille P, Ng V, Akutagawa J, Krisman K, Crone M, Burgess MR, Williams O, Houseman B, Shokat K, Sampath D, Bollag G, Roose JP, Braun BS, Shannon K. PLC-? and PI3K link cytokines to ERK activation in hematopoietic cells with normal and oncogenic Kras. Sci Signal. 2013 Dec 03; 6(304):ra105.

    (PMID 24300897) (PDF)

  • Ostrem JM, Peters U, Sos ML, Wells JA, Shokat KM. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature. 2013 Nov 28; 503(7477):548-51.

    (PMID 24256730) (PDF)

  • Fan QW, Cheng CK, Gustafson WC, Charron E, Zipper P, Wong RA, Chen J, Lau J, Knobbe-Thomsen C, Weller M, Jura N, Reifenberger G, Shokat KM, Weiss WA. EGFR phosphorylates tumor-derived EGFRvIII driving STAT3/5 and progression in glioblastoma. Cancer Cell. 2013 Oct 14; 24(4):438-49.

    (PMID 24135280) (PDF)

  • Zhang C, Lopez MS, Dar AC, Ladow E, Finkbeiner S, Yun CH, Eck MJ, Shokat KM. Structure-guided inhibitor design expands the scope of analog-sensitive kinase technology. ACS Chem Biol. 2013 Sep 20; 8(9):1931-8.

    (PMID 23841803) (PDF)

  • Hertz NT, Berthet A, Sos ML, Thorn KS, Burlingame AL, Nakamura K, Shokat KM. A neo-substrate that amplifies catalytic activity of parkinson’s-disease-related kinase PINK1. Cell. 2013 Aug 15; 154(4):737-47.

    (PMID 23953109) (PDF)

  • Atreya CE, Sangale Z, Xu N, Matli MR, Tikishvili E, Welbourn W, Stone S, Shokat KM, Warren RS. PTEN expression is consistent in colorectal cancer primaries and metastases and associates with patient survival. Cancer Med. 2013 Aug; 2(4):496-506.

    (PMID 24156022) (PDF)

  • Pourdehnad M, Truitt ML, Siddiqi IN, Ducker GS, Shokat KM, Ruggero D. Myc and mTOR converge on a common node in protein synthesis control that confers synthetic lethality in Myc-driven cancers. Proc Natl Acad Sci U S A. 2013 Jul 16; 110(29):11988-93.

    (PMID 23803853) (PDF)

  • Schachter MM, Merrick KA, Larochelle S, Hirschi A, Zhang C, Shokat KM, Rubin SM, Fisher RP. A Cdk7-Cdk4 T-loop phosphorylation cascade promotes G1 progression. Mol Cell. 2013 Apr 25; 50(2):250-60.

    (PMID 23622515) (PDF)

  • Lourido S, Zhang C, Lopez MS, Tang K, Barks J, Wang Q, Wildman SA, Shokat KM, Sibley LD. Optimizing small molecule inhibitors of calcium-dependent protein kinase 1 to prevent infection by Toxoplasma gondii. J Med Chem. 2013 Apr 11; 56(7):3068-77.

    (PMID 23470217) (PDF)

  • Kaasik K, Kivimäe S, Allen JJ, Chalkley RJ, Huang Y, Baer K, Kissel H, Burlingame AL, Shokat KM, Ptácek LJ, Fu YH. Glucose sensor O-GlcNAcylation coordinates with phosphorylation to regulate circadian clock. Cell Metab. 2013 Feb 05; 17(2):291-302.

    (PMID 23395175) (PDF)

  • Soskis MJ, Ho HY, Bloodgood BL, Robichaux MA, Malik AN, Ataman B, Rubin AA, Zieg J, Zhang C, Shokat KM, Sharma N, Cowan CW, Greenberg ME. A chemical genetic approach reveals distinct EphB signaling mechanisms during brain development. Nat Neurosci. 2012 Dec; 15(12):1645-54.

    (PMID 23143520) (PDF)

  • Atreya CE, Ducker GS, Feldman ME, Bergsland EK, Warren RS, Shokat KM. Combination of ATP-competitive mammalian target of rapamycin inhibitors with standard chemotherapy for colorectal cancer. Invest New Drugs. 2012 Dec; 30(6):2219-25.

    (PMID 22270257) (PDF)

  • Crews C, Shokat K, Suga H, Kostic M. News from the Chemistry & Biology editorial team. Chem Biol. 2012 Nov 21; 19(11):1355.

    (PMID 23177188) (PDF)

  • Larochelle S, Amat R, Glover-Cutter K, Sansó M, Zhang C, Allen JJ, Shokat KM, Bentley DL, Fisher RP. Cyclin-dependent kinase control of the initiation-to-elongation switch of RNA polymerase II. Nat Struct Mol Biol. 2012 Nov; 19(11):1108-15.

    (PMID 23064645) (PDF)

  • Young ET, Zhang C, Shokat KM, Parua PK, Braun KA. The AMP-activated protein kinase Snf1 regulates transcription factor binding, RNA polymerase II activity, and mRNA stability of glucose-repressed genes in Saccharomyces cerevisiae. J Biol Chem. 2012 Aug 17; 287(34):29021-34.

    (PMID 22761425) (PDF)

  • Jang M, Kim Y, Won H, Lim S, K R J, Dashdorj A, Min YH, Kim SY, Shokat KM, Ha J, Kim SS. Carbonyl reductase 1 offers a novel therapeutic target to enhance leukemia treatment by arsenic trioxide. Cancer Res. 2012 Aug 15; 72(16):4214-24.

    (PMID 22719067) (PDF)

  • Chen C, Kudo M, Rutaganira F, Takano H, Lee C, Atakilit A, Robinett KS, Uede T, Wolters PJ, Shokat KM, Huang X, Sheppard D. Integrin a9ß1 in airway smooth muscle suppresses exaggerated airway narrowing. J Clin Invest. 2012 Aug; 122(8):2916-27.

    (PMID 22772469) (PDF)

  • Wohlbold L, Merrick KA, De S, Amat R, Kim JH, Larochelle S, Allen JJ, Zhang C, Shokat KM, Petrini JH, Fisher RP. Chemical genetics reveals a specific requirement for Cdk2 activity in the DNA damage response and identifies Nbs1 as a Cdk2 substrate in human cells. PLoS Genet. 2012 Aug; 8(8):e1002935.

    (PMID 22927831) (PDF)

  • Sansó M, Lee KM, Viladevall L, Jacques PÉ, Pagé V, Nagy S, Racine A, St Amour CV, Zhang C, Shokat KM, Schwer B, Robert F, Fisher RP, Tanny JC. A positive feedback loop links opposing functions of P-TEFb/Cdk9 and histone H2B ubiquitylation to regulate transcript elongation in fission yeast. PLoS Genet. 2012 Aug; 8(8):e1002822.

    (PMID 22876190) (PDF)

  • Cheng CK, Gustafson WC, Charron E, Houseman BT, Zunder E, Goga A, Gray NS, Pollok B, Oakes SA, James CD, Shokat KM, Weiss WA, Fan QW. Dual blockade of lipid and cyclin-dependent kinases induces synthetic lethality in malignant glioma. Proc Natl Acad Sci U S A. 2012 Jul 31; 109(31):12722-7.

    (PMID 22802621) (PDF)

  • St Amour CV, Sansó M, Bösken CA, Lee KM, Larochelle S, Zhang C, Shokat KM, Geyer M, Fisher RP. Separate domains of fission yeast Cdk9 (P-TEFb) are required for capping enzyme recruitment and primed (Ser7-phosphorylated) Rpb1 carboxyl-terminal domain substrate recognition. Mol Cell Biol. 2012 Jul; 32(13):2372-83.

    (PMID 22508988) (PDF)

  • Ryan CJ, Roguev A, Patrick K, Xu J, Jahari H, Tong Z, Beltrao P, Shales M, Qu H, Collins SR, Kliegman JI, Jiang L, Kuo D, Tosti E, Kim HS, Edelmann W, Keogh MC, Greene D, Tang C, Cunningham P, Shokat KM, Cagney G, Svensson JP, Guthrie C, Espenshade PJ, Ideker T, Krogan NJ. Hierarchical modularity and the evolution of genetic interactomes across species. Mol Cell. 2012 Jun 08; 46(5):691-704.

    (PMID 22681890) (PDF)

  • Dar AC, Das TK, Shokat KM, Cagan RL. Chemical genetic discovery of targets and anti-targets for cancer polypharmacology. Nature. 2012 Jun 06; 486(7401):80-4.

    (PMID 22678283) (PDF)

  • Sun Y, Miao Y, Yamane Y, Zhang C, Shokat KM, Takematsu H, Kozutsumi Y, Drubin DG. Orm protein phosphoregulation mediates transient sphingolipid biosynthesis response to heat stress via the Pkh-Ypk and Cdc55-PP2A pathways. Mol Biol Cell. 2012 Jun; 23(12):2388-98.

    (PMID 22535525) (PDF)

  • Cibrián Uhalte E, Kirchner M, Hellwig N, Allen JJ, Donat S, Shokat KM, Selbach M, Abdelilah-Seyfried S. In vivo conditions to identify Prkci phosphorylation targets using the analog-sensitive kinase method in zebrafish. PLoS One. 2012 Jun; 7(6):e40000.

    (PMID 22768194) (PDF)

  • Hengeveld RC, Hertz NT, Vromans MJ, Zhang C, Burlingame AL, Shokat KM, Lens SM. Development of a chemical genetic approach for human aurora B kinase identifies novel substrates of the chromosomal passenger complex. Mol Cell Proteomics. 2012 May; 11(5):47-59.

    (PMID 22267324) (PDF)

  • Barkovich KJ, Hariono S, Garske AL, Zhang J, Blair JA, Fan QW, Shokat KM, Nicolaides T, Weiss WA. Kinetics of inhibitor cycling underlie therapeutic disparities between EGFR-driven lung and brain cancers. Cancer Discov. 2012 May; 2(5):450-7.

    (PMID 22588882) (PDF)

  • Horiuchi D, Huskey NE, Kusdra L, Wohlbold L, Merrick KA, Zhang C, Creasman KJ, Shokat KM, Fisher RP, Goga A. Chemical-genetic analysis of cyclin dependent kinase 2 function reveals an important role in cellular transformation by multiple oncogenic pathways. Proc Natl Acad Sci U S A. 2012 Apr 24; 109(17):E1019-27.

    (PMID 22474407) (PDF)

  • Savitt J, Singh D, Zhang C, Chen LC, Folmer J, Shokat KM, Wright WW. The in vivo response of stem and other undifferentiated spermatogonia to the reversible inhibition of glial cell line-derived neurotrophic factor signaling in the adult. Stem Cells. 2012 Apr; 30(4):732-40.

    (PMID 22232066) (PDF)

  • Ultanir SK, Hertz NT, Li G, Ge WP, Burlingame AL, Pleasure SJ, Shokat KM, Jan LY, Jan YN. Chemical genetic identification of NDR1/2 kinase substrates AAK1 and Rabin8 Uncovers their roles in dendrite arborization and spine development. Neuron. 2012 Mar 22; 73(6):1127-42.

    (PMID 22445341) (PDF)

  • Hsieh AC, Liu Y, Edlind MP, Ingolia NT, Janes MR, Sher A, Shi EY, Stumpf CR, Christensen C, Bonham MJ, Wang S, Ren P, Martin M, Jessen K, Feldman ME, Weissman JS, Shokat KM, Rommel C, Ruggero D. The translational landscape of mTOR signalling steers cancer initiation and metastasis. Nature. 2012 Feb 22; 485(7396):55-61.

    (PMID 22367541) (PDF)

  • Dorsey SG, Lovering RM, Renn CL, Leitch CC, Liu X, Tallon LJ, Sadzewicz LD, Pratap A, Ott S, Sengamalay N, Jones KM, Barrick C, Fulgenzi G, Becker J, Voelker K, Talmadge R, Harvey BK, Wyatt RM, Vernon-Pitts E, Zhang C, Shokat K, Fraser-Liggett C, Balice-Gordon RJ, Tessarollo L, Ward CW. Genetic deletion of trkB.T1 increases neuromuscular function. Am J Physiol Cell Physiol. 2012 Jan 01; 302(1):C141-53.

    (PMID 21865582) (PDF)

  • Simon MD, Shokat KM. A method to site-specifically incorporate methyl-lysine analogues into recombinant proteins. Methods Enzymol. 2012; 512:57-69.

    (PMID 22910202) (PDF)

  • Statsuk AV, Shokat KM. Covalent cross-linking of kinases with their corresponding peptide substrates. Methods Mol Biol. 2012; 795:179-90.

    (PMID 21960223) (PDF)

  • Banko MR, Allen JJ, Schaffer BE, Wilker EW, Tsou P, White JL, Villén J, Wang B, Kim SR, Sakamoto K, Gygi SP, Cantley LC, Yaffe MB, Shokat KM, Brunet A. Chemical genetic screen for AMPKa2 substrates uncovers a network of proteins involved in mitosis. Mol Cell. 2011 Dec 23; 44(6):878-92.

    (PMID 22137581) (PDF)

  • Cipak L, Zhang C, Kovacikova I, Rumpf C, Miadokova E, Shokat KM, Gregan J. Generation of a set of conditional analog-sensitive alleles of essential protein kinases in the fission yeast Schizosaccharomyces pombe. Cell Cycle. 2011 Oct 15; 10(20):3527-32.

    (PMID 22030861) (PDF)

  • Artz JD, Wernimont AK, Allali-Hassani A, Zhao Y, Amani M, Lin YH, Senisterra G, Wasney GA, Fedorov O, King O, Roos A, Lunin VV, Qiu W, Finerty P, Hutchinson A, Chau I, von Delft F, MacKenzie F, Lew J, Kozieradzki I, Vedadi M, Schapira M, Zhang C, Shokat K, Heightman T, Hui R. The Cryptosporidium parvum kinome. BMC Genomics. 2011 Sep 30; 12:478.

    (PMID 21962082) (PDF)

  • Schoenborn JR, Tan YX, Zhang C, Shokat KM, Weiss A. Feedback circuits monitor and adjust basal Lck-dependent events in T cell receptor signaling. Sci Signal. 2011 Sep 13; 4(190):ra59.

    (PMID 21917715) (PDF)

  • Wang BT, Ducker GS, Barczak AJ, Barbeau R, Erle DJ, Shokat KM. The mammalian target of rapamycin regulates cholesterol biosynthetic gene expression and exhibits a rapamycin-resistant transcriptional profile. Proc Natl Acad Sci U S A. 2011 Sep 13; 108(37):15201-6.

    (PMID 21876130) (PDF)

  • Garske AL, Peters U, Cortesi AT, Perez JL, Shokat KM. Chemical genetic strategy for targeting protein kinases based on covalent complementarity. Proc Natl Acad Sci U S A. 2011 Sep 13; 108(37):15046-52.

    (PMID 21852571) (PDF)

  • Mirzoeva OK, Hann B, Hom YK, Debnath J, Aftab D, Shokat K, Korn WM. Autophagy suppression promotes apoptotic cell death in response to inhibition of the PI3K-mTOR pathway in pancreatic adenocarcinoma. J Mol Med (Berl). 2011 Sep; 89(9):877-89.

    (PMID 21678117) (PDF)

  • Yoshii A, Murata Y, Kim J, Zhang C, Shokat KM, Constantine-Paton M. TrkB and protein kinase Mζ regulate synaptic localization of PSD-95 in developing cortex. J Neurosci. 2011 Aug 17; 31(33):11894-904.

    (PMID 21849550) (PDF)

  • Korennykh AV, Egea PF, Korostelev AA, Finer-Moore J, Stroud RM, Zhang C, Shokat KM, Walter P. Cofactor-mediated conformational control in the bifunctional kinase/RNase Ire1. BMC Biol. 2011 Jul 06; 9:48.

    (PMID 21729334) (PDF)

  • Korennykh AV, Korostelev AA, Egea PF, Finer-Moore J, Stroud RM, Zhang C, Shokat KM, Walter P. Structural and functional basis for RNA cleavage by Ire1. BMC Biol. 2011 Jul 06; 9:47.

    (PMID 21729333) (PDF)

  • Merrick KA, Wohlbold L, Zhang C, Allen JJ, Horiuchi D, Huskey NE, Goga A, Shokat KM, Fisher RP. Switching Cdk2 on or off with small molecules to reveal requirements in human cell proliferation. Mol Cell. 2011 Jun 10; 42(5):624-36.

    (PMID 21658603) (PDF)

  • Dar AC, Shokat KM. The evolution of protein kinase inhibitors from antagonists to agonists of cellular signaling. Annu Rev Biochem. 2011 May 6; 80:769-95.

    (PMID 21548788) (PDF)

  • Brennan DF, Dar AC, Hertz NT, Chao WC, Burlingame AL, Shokat KM, Barford D. A Raf-induced allosteric transition of KSR stimulates phosphorylation of MEK. Nature. 2011 Apr 21; 472(7343):366-9.

    (PMID 21441910) (PDF)

  • Crews C, Shokat K, Wohlleben W, Kostic M. Chemistry & Biology editors announce changes to the editorial team. Chem Biol. 2011 Feb 25; 18(2):141.

    (PMID 21338910) (PDF)

  • Tak E, Lee S, Lee J, Rashid MA, Kim YW, Park JH, Park WS, Shokat KM, Ha J, Kim SS. Human carbonyl reductase 1 upregulated by hypoxia renders resistance to apoptosis in hepatocellular carcinoma cells. J Hepatol. 2011 Feb; 54(2):328-39.

    (PMID 21056497) (PDF)

  • Nakamura JL, Phong C, Pinarbasi E, Kogan SC, Vandenberg S, Horvai AE, Faddegon BA, Fiedler D, Shokat K, Houseman BT, Chao R, Pieper RO, Shannon K. Dose-dependent effects of focal fractionated irradiation on secondary malignant neoplasms in Nf1 mutant mice. Cancer Res. 2011 Jan 01; 71(1):106-15.

    (PMID 21199799) (PDF)

  • Salomon D, Zhang C, Shokat KM, Sessa G. Sensitizing plant protein kinases to specific inhibition by ATP-competitive molecules. Methods Mol Biol. 2011; 779:185-97.

    (PMID 21837567) (PDF)

  • Bodenmiller B, Wanka S, Kraft C, Urban J, Campbell D, Pedrioli PG, Gerrits B, Picotti P, Lam H, Vitek O, Brusniak MY, Roschitzki B, Zhang C, Shokat KM, Schlapbach R, Colman-Lerner A, Nolan GP, Nesvizhskii AI, Peter M, Loewith R, von Mering C, Aebersold R. Phosphoproteomic analysis reveals interconnected system-wide responses to perturbations of kinases and phosphatases in yeast. Sci Signal. 2010 Dec 21; 3(153):rs4.

    (PMID 21177495) (PDF)

  • Bandyopadhyay S, Mehta M, Kuo D, Sung MK, Chuang R, Jaehnig EJ, Bodenmiller B, Licon K, Copeland W, Shales M, Fiedler D, Dutkowski J, Guénolé A, van Attikum H, Shokat KM, Kolodner RD, Huh WK, Aebersold R, Keogh MC, Krogan NJ, Ideker T. Rewiring of genetic networks in response to DNA damage. Science. 2010 Dec 03; 330(6009):1385-9.

    (PMID 21127252) (PDF)

  • Chuluunbaatar U, Roller R, Feldman ME, Brown S, Shokat KM, Mohr I. Constitutive mTORC1 activation by a herpesvirus Akt surrogate stimulates mRNA translation and viral replication. Genes Dev. 2010 Dec 01; 24(23):2627-39.

    (PMID 21123650) (PDF)

  • Au-Yeung BB, Levin SE, Zhang C, Hsu LY, Cheng DA, Killeen N, Shokat KM, Weiss A. A genetically selective inhibitor demonstrates a function for the kinase Zap70 in regulatory T cells independent of its catalytic activity. Nat Immunol. 2010 Dec; 11(12):1085-92.

    (PMID 21037577) (PDF)

  • Su T, Bryant DM, Luton F, Vergés M, Ulrich SM, Hansen KC, Datta A, Eastburn DJ, Burlingame AL, Shokat KM, Mostov KE. A kinase cascade leading to Rab11-FIP5 controls transcytosis of the polymeric immunoglobulin receptor. Nat Cell Biol. 2010 Dec; 12(12):1143-53.

    (PMID 21037565) (PDF)

  • Fan QW, Cheng C, Hackett C, Feldman M, Houseman BT, Nicolaides T, Haas-Kogan D, James CD, Oakes SA, Debnath J, Shokat KM, Weiss WA. Akt and autophagy cooperate to promote survival of drug-resistant glioma. Sci Signal. 2010 Nov 09; 3(147):ra81.

    (PMID 21062993) (PDF)

  • Gomez-Sjoberg R, Leyrat AA, Houseman BT, Shokat K, Quake SR. Biocompatibility and reduced drug absorption of sol-gel-treated poly(dimethyl siloxane) for microfluidic cell culture applications. Anal Chem. 2010 Nov 01; 82(21):8954-60.

    (PMID 20936785) (PDF)

  • Chou WH, Wang D, McMahon T, Qi ZH, Song M, Zhang C, Shokat KM, Messing RO. GABAA receptor trafficking is regulated by protein kinase C(epsilon) and the N-ethylmaleimide-sensitive factor. J Neurosci. 2010 Oct 20; 30(42):13955-65.

    (PMID 20962217) (PDF)

  • Tietjen JR, Zhang DW, Rodríguez-Molina JB, White BE, Akhtar MS, Heidemann M, Li X, Chapman RD, Shokat K, Keles S, Eick D, Ansari AZ. Chemical-genomic dissection of the CTD code. Nat Struct Mol Biol. 2010 Sep; 17(9):1154-61.

    (PMID 20802488) (PDF)

  • Okuzumi T, Ducker GS, Zhang C, Aizenstein B, Hoffman R, Shokat KM. Synthesis and evaluation of indazole based analog sensitive Akt inhibitors. Mol Biosyst. 2010 Aug; 6(8):1389-402.

    (PMID 20582381) (PDF)

  • Maciejowski J, George KA, Terret ME, Zhang C, Shokat KM, Jallepalli PV. Mps1 directs the assembly of Cdc20 inhibitory complexes during interphase and mitosis to control M phase timing and spindle checkpoint signaling. J Cell Biol. 2010 Jul 12; 190(1):89-100.

    (PMID 20624902) (PDF)

  • Feldman ME, Shokat KM. New inhibitors of the PI3K-Akt-mTOR pathway: insights into mTOR signaling from a new generation of Tor kinase domain inhibitors (TORKinibs). Curr Top Microbiol Immunol. 2010 Jun 12; 347:241-62.

    (PMID 20549474) (PDF)

  • Lu M, Wang J, Jones KT, Ives HE, Feldman ME, Yao LJ, Shokat KM, Ashrafi K, Pearce D. mTOR complex-2 activates ENaC by phosphorylating SGK1. J Am Soc Nephrol. 2010 May; 21(5):811-8.

    (PMID 20338997) (PDF)

  • Lourido S, Shuman J, Zhang C, Shokat KM, Hui R, Sibley LD. Calcium-dependent protein kinase 1 is an essential regulator of exocytosis in Toxoplasma. Nature. 2010 May 20; 465(7296):359-62.

    (PMID 20485436) (PDF)

  • Shokat KM. A drug-drug interaction crystallizes a new entry point into the UPR. Mol Cell. 2010 Apr 23; 38(2):161-3.

    (PMID 20417596) (PDF)

  • Sliedrecht T, Zhang C, Shokat KM, Kops GJ. Chemical genetic inhibition of Mps1 in stable human cell lines reveals novel aspects of Mps1 function in mitosis. PLoS One. 2010 Apr 22; 5(4):e10251.

    (PMID 20422024) (PDF)

  • An S, Kyoung M, Allen JJ, Shokat KM, Benkovic SJ. Dynamic regulation of a metabolic multi-enzyme complex by protein kinase CK2. J Biol Chem. 2010 Apr 09; 285(15):11093-9.

    (PMID 20157113) (PDF)

  • Miller S, Tavshanjian B, Oleksy A, Perisic O, Houseman BT, Shokat KM, Williams RL. Shaping development of autophagy inhibitors with the structure of the lipid kinase Vps34. Science. 2010 Mar 26; 327(5973):1638-42.

    (PMID 20339072) (PDF)

  • Poulikakos PI, Zhang C, Bollag G, Shokat KM, Rosen N. RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF. Nature. 2010 Mar 18; 464(7287):427-30.

    (PMID 20179705) (PDF)

  • Hsieh AC, Costa M, Zollo O, Davis C, Feldman ME, Testa JR, Meyuhas O, Shokat KM, Ruggero D. Genetic dissection of the oncogenic mTOR pathway reveals druggable addiction to translational control via 4EBP-eIF4E. Cancer Cell. 2010 Mar 16; 17(3):249-61.

    (PMID 20227039) (PDF)

  • Dail M, Li Q, McDaniel A, Wong J, Akagi K, Huang B, Kang HC, Kogan SC, Shokat K, Wolff L, Braun BS, Shannon K. Mutant Ikzf1, KrasG12D, and Notch1 cooperate in T lineage leukemogenesis and modulate responses to targeted agents. Proc Natl Acad Sci U S A. 2010 Mar 16; 107(11):5106-11.

    (PMID 20194733) (PDF)

  • Hertz NT, Wang BT, Allen JJ, Zhang C, Dar AC, Burlingame AL, Shokat KM. Chemical genetic approach for kinase-substrate mapping by covalent capture of thiophosphopeptides and analysis by mass spectrometry. Curr Protoc Chem Biol. 2010 Mar 01; 2(1):15-36. View on PubMed

    (PMID 23836541) (PDF)

  • Berndt A, Miller S, Williams O, Le DD, Houseman BT, Pacold JI, Gorrec F, Hon WC, Liu Y, Rommel C, Gaillard P, Rückle T, Schwarz MK, Shokat KM, Shaw JP, Williams RL. The p110delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors. Nat Chem Biol. 2010 Mar; 6(3):244.

    (PMID 20154668) (PDF)

  • Williams O, Houseman BT, Kunkel EJ, Aizenstein B, Hoffman R, Knight ZA, Shokat KM. Discovery of dual inhibitors of the immune cell PI3Ks p110delta and p110gamma: a prototype for new anti-inflammatory drugs. Chem Biol. 2010 Feb 26; 17(2):123-34.

    (PMID 20189103) (PDF)

  • Carlson HK, Plate L, Price MS, Allen JJ, Shokat KM, Marletta MA. Use of a semisynthetic epitope to probe histidine kinase activity and regulation. Anal Biochem. 2010 Feb 15; 397(2):139-43.

    (PMID 19819215) (PDF)

  • Roux J, Carles M, Koh H, Goolaerts A, Ganter MT, Chesebro BB, Howard M, Houseman BT, Finkbeiner W, Shokat KM, Paquet AC, Matthay MA, Pittet JF. Transforming growth factor beta1 inhibits cystic fibrosis transmembrane conductance regulator-dependent cAMP-stimulated alveolar epithelial fluid transport via a phosphatidylinositol 3-kinase-dependent mechanism. J Biol Chem. 2010 Feb 12; 285(7):4278-90.

    (PMID 19996317) (PDF)

  • Knight ZA, Lin H, Shokat KM. Targeting the cancer kinome through polypharmacology. Nat Rev Cancer. 2010 Feb; 10(2):130-7.

    (PMID 20094047) (PDF)

  • Berndt A, Miller S, Williams O, Le DD, Houseman BT, Pacold JI, Gorrec F, Hon WC, Liu Y, Rommel C, Gaillard P, Rückle T, Schwarz MK, Shokat KM, Shaw JP, Williams RL. The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors. Nat Chem Biol. 2010 Feb; 6(2):117-24.

    (PMID 20081827) (PDF)

  • Amin DN, Sergina N, Ahuja D, McMahon M, Blair JA, Wang D, Hann B, Koch KM, Shokat KM, Moasser MM. Resiliency and vulnerability in the HER2-HER3 tumorigenic driver. Sci Transl Med. 2010 Jan 27; 2(16):16ra7.

    (PMID 20371474) (PDF)

  • Niu H, Wan L, Busygina V, Kwon Y, Allen JA, Li X, Kunz RC, Kubota K, Wang B, Sung P, Shokat KM, Gygi SP, Hollingsworth NM. Regulation of meiotic recombination via Mek1-mediated Rad54 phosphorylation. Mol Cell. 2009 Nov 13; 36(3):393-404. View on PubMed

    (PMID 19917248) (PDF)

  • Sos ML, Fischer S, Ullrich R, Peifer M, Heuckmann JM, Koker M, Heynck S, Stückrath I, Weiss J, Fischer F, Michel K, Goel A, Regales L, Politi KA, Perera S, Getlik M, Heukamp LC, Ansén S, Zander T, Beroukhim R, Kashkar H, Shokat KM, Sellers WR, Rauh D, Orr C, Hoeflich KP, Friedman L, Wong KK, Pao W, Thomas RK. Identifying genotype-dependent efficacy of single and combined PI3K- and MAPK-pathway inhibition in cancer. Proc Natl Acad Sci U S A. 2009 Oct 27; 106(43):18351-6.

    (PMID 19805051) (PDF)

  • Herbert SP, Huisken J, Kim TN, Feldman ME, Houseman BT, Wang RA, Shokat KM, Stainier DY. Arterial-venous segregation by selective cell sprouting: an alternative mode of blood vessel formation. Science. 2009 Oct 09; 326(5950):294-8.

    (PMID 19815777) (PDF)

  • Glover-Cutter K, Larochelle S, Erickson B, Zhang C, Shokat K, Fisher RP, Bentley DL. TFIIH-associated Cdk7 kinase functions in phosphorylation of C-terminal domain Ser7 residues, promoter-proximal pausing, and termination by RNA polymerase II. Mol Cell Biol. 2009 Oct; 29(20):5455-64.

    (PMID 19667075) (PDF)

  • Liu Y, Warfield L, Zhang C, Luo J, Allen J, Lang WH, Ranish J, Shokat KM, Hahn S. Phosphorylation of the transcription elongation factor Spt5 by yeast Bur1 kinase stimulates recruitment of the PAF complex. Mol Cell Biol. 2009 Sep; 29(17):4852-63.

    (PMID 19581288) (PDF)

  • de Lartigue J, Polson H, Feldman M, Shokat K, Tooze SA, Urbé S, Clague MJ. PIKfyve regulation of endosome-linked pathways. Traffic. 2009 Jul; 10(7):883-93.

    (PMID 19582903) (PDF)

  • Okuzumi T, Fiedler D, Zhang C, Gray DC, Aizenstein B, Hoffman R, Shokat KM. Inhibitor hijacking of Akt activation. Nat Chem Biol. 2009 Jul; 5(7):484-93.

    (PMID 19465931) (PDF)

  • Beltrao P, Trinidad JC, Fiedler D, Roguev A, Lim WA, Shokat KM, Burlingame AL, Krogan NJ. Evolution of phosphoregulation: comparison of phosphorylation patterns across yeast species. PLoS Biol. 2009 Jun 16; 7(6):e1000134.

    (PMID 19547744) (PDF)

  • Wang H, Kakaradov B, Collins SR, Karotki L, Fiedler D, Shales M, Shokat KM, Walther TC, Krogan NJ, Koller D. A complex-based reconstruction of the Saccharomyces cerevisiae interactome. Mol Cell Proteomics. 2009 Jun; 8(6):1361-81.

    (PMID 19176519) (PDF)

  • Salomon D, Bonshtien A, Mayrose M, Zhang C, Shokat KM, Sessa G. Bypassing kinase activity of the tomato Pto resistance protein with small molecule ligands. J Biol Chem. 2009 May 29; 284(22):15289-98.

    (PMID 19332544) (PDF)

  • Niedermeier M, Hennessy BT, Knight ZA, Henneberg M, Hu J, Kurtova AV, Wierda WG, Keating MJ, Shokat KM, Burger JA. Isoform-selective phosphoinositide 3’-kinase inhibitors inhibit CXCR4 signaling and overcome stromal cell-mediated drug resistance in chronic lymphocytic leukemia: a novel therapeutic approach. Blood. 2009 May 28; 113(22):5549-57.

    (PMID 19318683) (PDF)

  • Burkard ME, Maciejowski J, Rodriguez-Bravo V, Repka M, Lowery DM, Clauser KR, Zhang C, Shokat KM, Carr SA, Yaffe MB, Jallepalli PV. Plk1 self-organization and priming phosphorylation of HsCYK-4 at the spindle midzone regulate the onset of division in human cells. PLoS Biol. 2009 May 05; 7(5):e1000111.

    (PMID 19468302) (PDF)

  • Justman QA, Serber Z, Ferrell JE, El-Samad H, Shokat KM. Tuning the activation threshold of a kinase network by nested feedback loops. Science. 2009 Apr 24; 324(5926):509-12.

    (PMID 19390045) (PDF)

  • Wong CH, Baehner FL, Spassov DS, Ahuja D, Wang D, Hann B, Blair J, Shokat K, Welm AL, Moasser MM. Phosphorylation of the SRC epithelial substrate Trask is tightly regulated in normal epithelia but widespread in many human epithelial cancers. Clin Cancer Res. 2009 Apr 01; 15(7):2311-22.

    (PMID 19318475) (PDF)

  • Viladevall L, St Amour CV, Rosebrock A, Schneider S, Zhang C, Allen JJ, Shokat KM, Schwer B, Leatherwood JK, Fisher RP. TFIIH and P-TEFb coordinate transcription with capping enzyme recruitment at specific genes in fission yeast. Mol Cell. 2009 Mar 27; 33(6):738-51.

    (PMID 19328067) (PDF)

  • Sly LM, Hamilton MJ, Kuroda E, Ho VW, Antignano FL, Omeis SL, van Netten-Thomas CJ, Wong D, Brugger HK, Williams O, Feldman ME, Houseman BT, Fiedler D, Shokat KM, Krystal G. SHIP prevents lipopolysaccharide from triggering an antiviral response in mice. Blood. 2009 Mar 26; 113(13):2945-54.

    (PMID 19139077) (PDF)

  • Fiedler D, Braberg H, Mehta M, Chechik G, Cagney G, Mukherjee P, Silva AC, Shales M, Collins SR, van Wageningen S, Kemmeren P, Holstege FC, Weissman JS, Keogh MC, Koller D, Shokat KM, Krogan NJ. Functional organization of the S. cerevisiae phosphorylation network. Cell. 2009 Mar 06; 136(5):952-63.

    (PMID 19269370) (PDF)

  • Feldman ME, Apsel B, Uotila A, Loewith R, Knight ZA, Ruggero D, Shokat KM. Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2. PLoS Biol. 2009 Feb 10; 7(2):e38.

    (PMID 19209957) (PDF)

  • Korennykh AV, Egea PF, Korostelev AA, Finer-Moore J, Zhang C, Shokat KM, Stroud RM, Walter P. The unfolded protein response signals through high-order assembly of Ire1. Nature. 2009 Feb 05; 457(7230):687-93.

    (PMID 19079236) (PDF)

  • Fan QW, Cheng C, Knight ZA, Haas-Kogan D, Stokoe D, James CD, McCormick F, Shokat KM, Weiss WA. EGFR signals to mTOR through PKC and independently of Akt in glioma. Sci Signal. 2009 Jan 27; 2(55):ra4.

    (PMID 19176518) (PDF)

  • Mirzoeva OK, Das D, Heiser LM, Bhattacharya S, Siwak D, Gendelman R, Bayani N, Wang NJ, Neve RM, Guan Y, Hu Z, Knight Z, Feiler HS, Gascard P, Parvin B, Spellman PT, Shokat KM, Wyrobek AJ, Bissell MJ, McCormick F, Kuo WL, Mills GB, Gray JW, Korn WM. Basal subtype and MAPK/ERK kinase (MEK)-phosphoinositide 3-kinase feedback signaling determine susceptibility of breast cancer cells to MEK inhibition. Cancer Res. 2009 Jan 15; 69(2):565-72.

    (PMID 19147570) (PDF)

  • Miller AL, Zhang C, Shokat KM, Lowell CA. Generation of a novel system for studying spleen tyrosine kinase function in macrophages and B cells. J Immunol. 2009 Jan 15; 182(2):988-98.

    (PMID 19124742) (PDF)

  • Li S, Makovets S, Matsuguchi T, Blethrow JD, Shokat KM, Blackburn EH. Cdk1-dependent phosphorylation of Cdc13 coordinates telomere elongation during cell-cycle progression. Cell. 2009 Jan 09; 136(1):50-61.

    (PMID 19135888) (PDF)

  • Morgan DJ, Weisenhaus M, Shum S, Su T, Zheng R, Zhang C, Shokat KM, Hille B, Babcock DF, McKnight GS. Tissue-specific PKA inhibition using a chemical genetic approach and its application to studies on sperm capacitation. Proc Natl Acad Sci U S A. 2008 Dec 30; 105(52):20740-5.

    (PMID 19074277) (PDF)

  • Statsuk AV, Maly DJ, Seeliger MA, Fabian MA, Biggs WH, Lockhart DJ, Zarrinkar PP, Kuriyan J, Shokat KM. Tuning a three-component reaction for trapping kinase substrate complexes. J Am Chem Soc. 2008 Dec 24; 130(51):17568-74.

    (PMID 19053485) (PDF)

  • Bateman RL, Rauh D, Tavshanjian B, Shokat KM. Human carbonyl reductase 1 is an S-nitrosoglutathione reductase. J Biol Chem. 2008 Dec 19; 283(51):35756-62.

    (PMID 18826943) (PDF)

  • Shirra MK, McCartney RR, Zhang C, Shokat KM, Schmidt MC, Arndt KM. A chemical genomics study identifies Snf1 as a repressor of GCN4 translation. J Biol Chem. 2008 Dec 19; 283(51):35889-98.

    (PMID 18955495) (PDF)

  • Papakonstanti EA, Zwaenepoel O, Bilancio A, Burns E, Nock GE, Houseman B, Shokat K, Ridley AJ, Vanhaesebroeck B. Distinct roles of class IA PI3K isoforms in primary and immortalised macrophages. J Cell Sci. 2008 Dec 15; 121(Pt 24):4124-33.

    (PMID 19033389) (PDF)

  • Merrick KA, Larochelle S, Zhang C, Allen JJ, Shokat KM, Fisher RP. Distinct activation pathways confer cyclin-binding specificity on Cdk1 and Cdk2 in human cells. Mol Cell. 2008 Dec 05; 32(5):662-72.

    (PMID 19061641) (PDF)

  • Kurischko C, Kuravi VK, Wannissorn N, Nazarov PA, Husain M, Zhang C, Shokat KM, McCaffery JM, Luca FC. The yeast LATS/Ndr kinase Cbk1 regulates growth via Golgi-dependent glycosylation and secretion. Mol Biol Cell. 2008 Dec; 19(12):5559-78.

    (PMID 18843045) (PDF)

  • Choi DS, Wei W, Deitchman JK, Kharazia VN, Lesscher HM, McMahon T, Wang D, Qi ZH, Sieghart W, Zhang C, Shokat KM, Mody I, Messing RO. Protein kinase Cdelta regulates ethanol intoxication and enhancement of GABA-stimulated tonic current. J Neurosci. 2008 Nov 12; 28(46):11890-9.

    (PMID 19005054) (PDF)

  • Kang J, Yang M, Li B, Qi W, Zhang C, Shokat KM, Tomchick DR, Machius M, Yu H. Structure and substrate recruitment of the human spindle checkpoint kinase Bub1. Mol Cell. 2008 Nov 07; 32(3):394-405.

    (PMID 18995837) (PDF)

  • Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA. Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov; 4(11):691-9.

    (PMID 18849971) (PDF)

  • Dar AC, Lopez MS, Shokat KM. Small molecule recognition of c-Src via the Imatinib-binding conformation. Chem Biol. 2008 Oct 20; 15(10):1015-22.

    (PMID 18940662) (PDF)

  • Chaisuparat R, Hu J, Jham BC, Knight ZA, Shokat KM, Montaner S. Dual inhibition of PI3Kalpha and mTOR as an alternative treatment for Kaposi’s sarcoma. Cancer Res. 2008 Oct 15; 68(20):8361-8.

    (PMID 18922908) (PDF)

  • Oda K, Okada J, Timmerman L, Rodriguez-Viciana P, Stokoe D, Shoji K, Taketani Y, Kuramoto H, Knight ZA, Shokat KM, McCormick F. PIK3CA cooperates with other phosphatidylinositol 3’-kinase pathway mutations to effect oncogenic transformation. Cancer Res. 2008 Oct 01; 68(19):8127-36.

    (PMID 18829572) (PDF)

  • Torbett NE, Luna-Moran A, Knight ZA, Houk A, Moasser M, Weiss W, Shokat KM, Stokoe D. A chemical screen in diverse breast cancer cell lines reveals genetic enhancers and suppressors of sensitivity to PI3K isoform-selective inhibition. Biochem J. 2008 Oct 01; 415(1):97-110.

    (PMID 18498248) (PDF)

  • Zhang TT, Okkenhaug K, Nashed BF, Puri KD, Knight ZA, Shokat KM, Vanhaesebroeck B, Marshall AJ. Genetic or pharmaceutical blockade of p110delta phosphoinositide 3-kinase enhances IgE production. J Allergy Clin Immunol. 2008 Oct; 122(4):811-819.e2.

    (PMID 19014771) (PDF)

  • Lu X, Simon MD, Chodaparambil JV, Hansen JC, Shokat KM, Luger K. The effect of H3K79 dimethylation and H4K20 trimethylation on nucleosome and chromatin structure. Nat Struct Mol Biol. 2008 Oct; 15(10):1122-4.

    (PMID 18794842) (PDF)

  • Kim JS, Lilley BN, Zhang C, Shokat KM, Sanes JR, Zhen M. A chemical-genetic strategy reveals distinct temporal requirements for SAD-1 kinase in neuronal polarization and synapse formation. Neural Dev. 2008 Sep 22; 3:23.

    (PMID 18808695) (PDF)

  • Sordet O, Larochelle S, Nicolas E, Stevens EV, Zhang C, Shokat KM, Fisher RP, Pommier Y. Hyperphosphorylation of RNA polymerase II in response to topoisomerase I cleavage complexes and its association with transcription- and BRCA1-dependent degradation of topoisomerase I. J Mol Biol. 2008 Sep 05; 381(3):540-9.

    (PMID 18588899) (PDF)

  • Kharas MG, Janes MR, Scarfone VM, Lilly MB, Knight ZA, Shokat KM, Fruman DA. Ablation of PI3K blocks BCR-ABL leukemogenesis in mice, and a dual PI3K/mTOR inhibitor prevents expansion of human BCR-ABL+ leukemia cells. J Clin Invest. 2008 Sep; 118(9):3038-50.

    (PMID 18704194) (PDF)

  • Johnson AW, Chen X, Crombag HS, Zhang C, Smith DR, Shokat KM, Gallagher M, Holland PC, Ginty DD. The brain-derived neurotrophic factor receptor TrkB is critical for the acquisition but not expression of conditioned incentive value. Eur J Neurosci. 2008 Sep; 28(5):997-1002.

    (PMID 18671735) (PDF)

  • Wang J, Knight ZA, Fiedler D, Williams O, Shokat KM, Pearce D. Activity of the p110-alpha subunit of phosphatidylinositol-3-kinase is required for activation of epithelial sodium transport. Am J Physiol Renal Physiol. 2008 Sep; 295(3):F843-50.

    (PMID 18653476) (PDF)

  • Park S, Chapuis N, Bardet V, Tamburini J, Gallay N, Willems L, Knight ZA, Shokat KM, Azar N, Viguié F, Ifrah N, Dreyfus F, Mayeux P, Lacombe C, Bouscary D. PI-103, a dual inhibitor of Class IA phosphatidylinositide 3-kinase and mTOR, has antileukemic activity in AML. Leukemia. 2008 Sep; 22(9):1698-706

    (PMID 18548104) (PDF)

  • Zunder ER, Knight ZA, Houseman BT, Apsel B, Shokat KM. Discovery of drug-resistant and drug-sensitizing mutations in the oncogenic PI3K isoform p110 alpha. Cancer Cell. 2008 Aug 12; 14(2):180-92.

    (PMID 18691552) (PDF)

  • Hoon S, Smith AM, Wallace IM, Suresh S, Miranda M, Fung E, Proctor M, Shokat KM, Zhang C, Davis RW, Giaever G, St Onge RP, StOnge RP, Nislow C. An integrated platform of genomic assays reveals small-molecule bioactivities. Nat Chem Biol. 2008 Aug; 4(8):498-506.

    (PMID 18622389) (PDF)

  • Tamgüney T, Zhang C, Fiedler D, Shokat K, Stokoe D. Analysis of 3-phosphoinositide-dependent kinase-1 signaling and function in ES cells. Exp Cell Res. 2008 Jul 01; 314(11-12):2299-312.

    (PMID 18514190) (PDF)

  • Kim HH, Abdelmohsen K, Lal A, Pullmann R, Yang X, Galban S, Srikantan S, Martindale JL, Blethrow J, Shokat KM, Gorospe M. Nuclear HuR accumulation through phosphorylation by Cdk1. Genes Dev. 2008 Jul 01; 22(13):1804-15.

    (PMID 18593881) (PDF)

  • Sauer S, Bruno L, Hertweck A, Finlay D, Leleu M, Spivakov M, Knight ZA, Cobb BS, Cantrell D, O’Connor E, Shokat KM, Fisher AG, Merkenschlager M. T cell receptor signaling controls Foxp3 expression via PI3K, Akt, and mTOR. Proc Natl Acad Sci U S A. 2008 Jun 03; 105(22):7797-802.

    (PMID 18509048) (PDF)

  • Levin SE, Zhang C, Kadlecek TA, Shokat KM, Weiss A. Inhibition of ZAP-70 kinase activity via an analog-sensitive allele blocks T cell receptor and CD28 superagonist signaling. J Biol Chem. 2008 May 30; 283(22):15419-30.

    (PMID 18378687) (PDF)

  • Chen JS, Zhou LJ, Entin-Meer M, Yang X, Donker M, Knight ZA, Weiss W, Shokat KM, Haas-Kogan D, Stokoe D. Characterization of structurally distinct, isoform-selective phosphoinositide 3’-kinase inhibitors in combination with radiation in the treatment of glioblastoma. Mol Cancer Ther. 2008 Apr; 7(4):841-50.

    (PMID 18413797) (PDF)

  • Balla A, Tuymetova G, Toth B, Szentpetery Z, Zhao X, Knight ZA, Shokat K, Steinbach PJ, Balla T. Design of drug-resistant alleles of type-III phosphatidylinositol 4-kinases using mutagenesis and molecular modeling. Biochemistry. 2008 Feb 12; 47(6):1599-607.

    (PMID 18205404) (PDF)

  • Blethrow JD, Glavy JS, Morgan DO, Shokat KM. Covalent capture of kinase-specific phosphopeptides reveals Cdk1-cyclin B substrates. Proc Natl Acad Sci U S A. 2008 Feb 05; 105(5):1442-7.

    (PMID 18234856) (PDF)

  • Wan L, Niu H, Futcher B, Zhang C, Shokat KM, Boulton SJ, Hollingsworth NM. Cdc28-Clb5 (CDK-S) and Cdc7-Dbf4 (DDK) collaborate to initiate meiotic recombination in yeast. Genes Dev. 2008 Feb 01; 22(3):386-97. View on PubMed

    (PMID 18245450) (PDF)

  • Balla A, Kim YJ, Varnai P, Szentpetery Z, Knight Z, Shokat KM, Balla T. Maintenance of hormone-sensitive phosphoinositide pools in the plasma membrane requires phosphatidylinositol 4-kinase III alpha. Mol Biol Cell. 2008 Feb; 19(2):711-21.

    (PMID 18077555) (PDF)

  • Rubenstein EM, McCartney RR, Zhang C, Shokat KM, Shirra MK, Arndt KM, Schmidt MC. Access denied: Snf1 activation loop phosphorylation is controlled by availability of the phosphorylated threonine 210 to the PP1 phosphatase. J Biol Chem. 2008 Jan 04; 283(1):222-30.

    (PMID 17991748) (PDF)

  • Weiss WA, Taylor SS, Shokat KM. Recognizing and exploiting differences between RNAi and small-molecule inhibitors. Nat Chem Biol. 2007 Dec; 3(12):739-44.

    (PMID 18007642) (PDF)

  • Lin JH, Li H, Yasumura D, Cohen HR, Zhang C, Panning B, Shokat KM, Lavail MM, Walter P. IRE1 signaling affects cell fate during the unfolded protein response. Science. 2007 Nov 09; 318(5852):944-9.

    (PMID 17991856) (PDF)

  • Qi ZH, Song M, Wallace MJ, Wang D, Newton PM, McMahon T, Chou WH, Zhang C, Shokat KM, Messing RO. Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits. J Biol Chem. 2007 Nov 09; 282(45):33052-63.

    (PMID 17875639) (PDF)

  • Snead JL, Sullivan M, Lowery DM, Cohen MS, Zhang C, Randle DH, Taunton J, Yaffe MB, Morgan DO, Shokat KM. A coupled chemical-genetic and bioinformatic approach to Polo-like kinase pathway exploration. Chem Biol. 2007 Nov; 14(11):1261-72.

    (PMID 18022565) (PDF)

  • Bateman R, Rauh D, Shokat KM. Glutathione traps formaldehyde by formation of a bicyclo[4.4.1]undecane adduct. Org Biomol Chem. 2007 Oct 21; 5(20):3363-7.

    (PMID 17912391) (PDF)

  • Estébanez-Perpiñá E, Arnold LA, Arnold AA, Nguyen P, Rodrigues ED, Mar E, Bateman R, Pallai P, Shokat KM, Baxter JD, Guy RK, Webb P, Fletterick RJ. A surface on the androgen receptor that allosterically regulates coactivator binding. Proc Natl Acad Sci U S A. 2007 Oct 09; 104(41):16074-9.

    (PMID 17911242) (PDF)

  • Das M, Jiang F, Sluss HK, Zhang C, Shokat KM, Flavell RA, Davis RJ. Suppression of p53-dependent senescence by the JNK signal transduction pathway. Proc Natl Acad Sci U S A. 2007 Oct 02; 104(40):15759-64.

    (PMID 17893331) (PDF)

  • Knight ZA, Garrison JL, Chan K, King DS, Shokat KM. A remodelled protease that cleaves phosphotyrosine substrates. J Am Chem Soc. 2007 Sep 26; 129(38):11672-3.

    (PMID 17803306) (PDF)

  • Fan QW, Cheng CK, Nicolaides TP, Hackett CS, Knight ZA, Shokat KM, Weiss WA. A dual phosphoinositide-3-kinase alpha/mTOR inhibitor cooperates with blockade of epidermal growth factor receptor in PTEN-mutant glioma. Cancer Res. 2007 Sep 01; 67(17):7960-5.

    (PMID 17804702) (PDF)

  • Allen JJ, Li M, Brinkworth CS, Paulson JL, Wang D, Hübner A, Chou WH, Davis RJ, Burlingame AL, Messing RO, Katayama CD, Hedrick SM, Shokat KM. A semisynthetic epitope for kinase substrates. Nat Methods. 2007 Jun; 4(6):511-6.

    (PMID 17486086) (PDF)

  • Hung CH, Thomas L, Ruby CE, Atkins KM, Morris NP, Knight ZA, Scholz I, Barklis E, Weinberg AD, Shokat KM, Thomas G. HIV-1 Nef assembles a Src family kinase-ZAP-70/Syk-PI3K cascade to downregulate cell-surface MHC-I. Cell Host Microbe. 2007 Apr 19; 1(2):121-33.

    (PMID 18005690) (PDF)

  • Kanin EI, Kipp RT, Kung C, Slattery M, Viale A, Hahn S, Shokat KM, Ansari AZ. Chemical inhibition of the TFIIH-associated kinase Cdk7/Kin28 does not impair global mRNA synthesis. Proc Natl Acad Sci U S A. 2007 Apr 03; 104(14):5812-7.

    (PMID 17392431) (PDF)

  • Knight ZA, Shokat KM. Chemically targeting the PI3K family. Biochem Soc Trans. 2007 Apr; 35(Pt 2):245-9.

    (PMID 17371250) (PDF)

  • Blair JA, Rauh D, Kung C, Yun CH, Fan QW, Rode H, Zhang C, Eck MJ, Weiss WA, Shokat KM. Structure-guided development of affinity probes for tyrosine kinases using chemical genetics. Nat Chem Biol. 2007 Apr; 3(4):229-38.

    (PMID 17334377) (PDF)

  • Larochelle S, Merrick KA, Terret ME, Wohlbold L, Barboza NM, Zhang C, Shokat KM, Jallepalli PV, Fisher RP. Requirements for Cdk7 in the assembly of Cdk1/cyclin B and activation of Cdk2 revealed by chemical genetics in human cells. Mol Cell. 2007 Mar 23; 25(6):839-50.

    (PMID 17386261) (PDF)

  • Burkard ME, Randall CL, Larochelle S, Zhang C, Shokat KM, Fisher RP, Jallepalli PV. Chemical genetics reveals the requirement for Polo-like kinase 1 activity in positioning RhoA and triggering cytokinesis in human cells. Proc Natl Acad Sci U S A. 2007 Mar 13; 104(11):4383-8.

    (PMID 17360533) (PDF)

  • Simon MD, Chu F, Racki LR, de la Cruz CC, Burlingame AL, Panning B, Narlikar GJ, Shokat KM. The site-specific installation of methyl-lysine analogs into recombinant histones. Cell. 2007 Mar 09; 128(5):1003-12.

    (PMID 17350582) (PDF)

  • Knight ZA, Shokat KM. Chemical genetics: where genetics and pharmacology meet. Cell. 2007 Feb 09; 128(3):425-30.

    (PMID 17289560) (PDF)

  • Sergina NV, Rausch M, Wang D, Blair J, Hann B, Shokat KM, Moasser MM. Escape from HER-family tyrosine kinase inhibitor therapy by the kinase-inactive HER3. Nature. 2007 Jan 25; 445(7126):437-41.

    (PMID 17206155) (PDF)

  • Knight ZA, Feldman ME, Balla A, Balla T, Shokat KM. A membrane capture assay for lipid kinase activity. Nat Protoc. 2007; 2(10):2459-66.

    (PMID 17947987) (PDF)

  • Gregan J, Zhang C, Rumpf C, Cipak L, Li Z, Uluocak P, Nasmyth K, Shokat KM. Construction of conditional analog-sensitive kinase alleles in the fission yeast Schizosaccharomyces pombe. Nat Protoc. 2007; 2(11):2996-3000.

    (PMID 18007635) (PDF)

  • Simon MD, Feldman ME, Rauh D, Maris AE, Wemmer DE, Shokat KM. Structure and properties of a re-engineered homeodomain protein-DNA interface. ACS Chem Biol. 2006 Dec 15; 1(12):755-60.

    (PMID 17240973) (PDF)

  • Wan L, Zhang C, Shokat KM, Hollingsworth NM. Chemical inactivation of cdc7 kinase in budding yeast results in a reversible arrest that allows efficient cell synchronization prior to meiotic recombination. Genetics. 2006 Dec; 174(4):1767-74.

    (PMID 17057233) (PDF)

  • Tóth B, Balla A, Ma H, Knight ZA, Shokat KM, Balla T. Phosphatidylinositol 4-kinase IIIbeta regulates the transport of ceramide between the endoplasmic reticulum and Golgi. J Biol Chem. 2006 Nov 24; 281(47):36369-77.

    (PMID 17003043) (PDF)

  • Jaeschke A, Karasarides M, Ventura JJ, Ehrhardt A, Zhang C, Flavell RA, Shokat KM, Davis RJ. JNK2 is a positive regulator of the cJun transcription factor. Mol Cell. 2006 Sep 15; 23(6):899-911.

    (PMID 16973441) (PDF)

  • Brodersen P, Petersen M, Bjørn Nielsen H, Zhu S, Newman MA, Shokat KM, Rietz S, Parker J, Mundy J. Arabidopsis MAP kinase 4 regulates salicylic acid- and jasmonic acid/ethylene-dependent responses via EDS1 and PAD4. Plant J. 2006 Aug; 47(4):532-46.

    (PMID 16813576) (PDF)

  • Van Keymeulen A, Wong K, Knight ZA, Govaerts C, Hahn KM, Shokat KM, Bourne HR. To stabilize neutrophil polarity, PIP3 and Cdc42 augment RhoA activity at the back as well as signals at the front. J Cell Biol. 2006 Jul 31; 174(3):437-45.

    (PMID 16864657) (PDF)

  • Wei F, Wang GD, Zhang C, Shokat KM, Wang H, Tsien JZ, Liauw J, Zhuo M. Forebrain overexpression of CaMKII abolishes cingulate long term depression and reduces mechanical allodynia and thermal hyperalgesia. Mol Pain. 2006 Jun 15; 2:21.

    (PMID 16776832) (PDF)

  • Knight ZA, Gonzalez B, Feldman ME, Zunder ER, Goldenberg DD, Williams O, Loewith R, Stokoe D, Balla A, Toth B, Balla T, Weiss WA, Williams RL, Shokat KM. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19; 125(4):733-47.

    (PMID 16647110) (PDF)

  • Fan QW, Knight ZA, Goldenberg DD, Yu W, Mostov KE, Stokoe D, Shokat KM, Weiss WA. A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer Cell. 2006 May; 9(5):341-9.

    (PMID 16697955) (PDF)

  • Allen JJ, Shokat KM. Chemical genomics: dialed in transcriptional network control with non-steroidal glucocorticoid receptor modulators. ACS Chem Biol. 2006 Apr 25; 1(3):139-40.

    (PMID 17163659) (PDF)

  • Sturgeon CM, Knight ZA, Shokat KM, Roberge M. Effect of combined DNA repair inhibition and G2 checkpoint inhibition on cell cycle progression after DNA damage. Mol Cancer Ther. 2006 Apr; 5(4):885-92.

    (PMID 16648558) (PDF)

  • Kung C, Kenski DM, Krukenberg K, Madhani HD, Shokat KM. Selective kinase inhibition by exploiting differential pathway sensitivity. Chem Biol. 2006 Apr; 13(4):399-407.

    (PMID 16632252) (PDF)

  • Ventura JJ, Hübner A, Zhang C, Flavell RA, Shokat KM, Davis RJ. Chemical genetic analysis of the time course of signal transduction by JNK. Mol Cell. 2006 Mar 03; 21(5):701-10.

    (PMID 16507367) (PDF)

  • Wohlbold L, Larochelle S, Liao JC, Livshits G, Singer J, Shokat KM, Fisher RP. The cyclin-dependent kinase (CDK) family member PNQALRE/CCRK supports cell proliferation but has no intrinsic CDK-activating kinase (CAK) activity. Cell Cycle. 2006 Mar; 5(5):546-54.

    (PMID 16552187) (PDF)

  • Juris SJ, Shah K, Shokat K, Dixon JE, Vacratsis PO. Identification of otubain 1 as a novel substrate for the Yersinia protein kinase using chemical genetics and mass spectrometry. FEBS Lett. 2006 Jan 09; 580(1):179-83.

    (PMID 16364312) (PDF)

  • Larochelle S, Batliner J, Gamble MJ, Barboza NM, Kraybill BC, Blethrow JD, Shokat KM, Fisher RP. Dichotomous but stringent substrate selection by the dual-function Cdk7 complex revealed by chemical genetics. Nat Struct Mol Biol. 2006 Jan; 13(1):55-62.

    (PMID 16327805) (PDF)

  • Pinsky BA, Kung C, Shokat KM, Biggins S. The Ipl1-Aurora protein kinase activates the spindle checkpoint by creating unattached kinetochores. Nat Cell Biol. 2006 Jan; 8(1):78-83.

    (PMID 16327780) (PDF)

  • Dephoure N, Howson RW, Blethrow JD, Shokat KM, O’Shea EK. Combining chemical genetics and proteomics to identify protein kinase substrates. Proc Natl Acad Sci U S A. 2005 Dec 13; 102(50):17940-5.

    (PMID 16330754) (PDF)

  • Kenski DM, Zhang C, von Zastrow M, Shokat KM. Chemical genetic engineering of G protein-coupled receptor kinase 2. J Biol Chem. 2005 Oct 14; 280(41):35051-61.

    (PMID 16081410) (PDF)

  • D’Aquino KE, Monje-Casas F, Paulson J, Reiser V, Charles GM, Lai L, Shokat KM, Amon A. The protein kinase Kin4 inhibits exit from mitosis in response to spindle position defects. Mol Cell. 2005 Jul 22; 19(2):223-34.

    (PMID 16039591) (PDF)

  • Zhang C, Kenski DM, Paulson JL, Bonshtien A, Sessa G, Cross JV, Templeton DJ, Shokat KM. A second-site suppressor strategy for chemical genetic analysis of diverse protein kinases. Nat Methods. 2005 Jun; 2(6):435-41.

    (PMID 15908922) (PDF)

  • Knight ZA, Shokat KM. Features of selective kinase inhibitors. Chem Biol. 2005 Jun; 12(6):621-37.

    (PMID 15975507) (PDF)

  • Cohen MS, Zhang C, Shokat KM, Taunton J. Structural bioinformatics-based design of selective, irreversible kinase inhibitors. Science. 2005 May 27; 308(5726):1318-21.

    (PMID 15919995) (PDF)

  • Tanaka M, Bateman R, Rauh D, Vaisberg E, Ramachandani S, Zhang C, Hansen KC, Burlingame AL, Trautman JK, Shokat KM, Adams CL. An unbiased cell morphology-based screen for new, biologically active small molecules. PLoS Biol. 2005 May; 3(5):e128.

    (PMID 15799708) (PDF)

  • Shokat KM. Chemicals call bacteria, and a new membrane protein machine answers. Cell. 2005 Apr 22; 121(2):163-6.

    (PMID 15851024) (PDF)

  • Allen JJ, Lazerwith SE, Shokat KM. Bio-orthogonal affinity purification of direct kinase substrates. J Am Chem Soc. 2005 Apr 20; 127(15):5288-9.

    (PMID 15826144) (PDF)

  • Alaimo PJ, Knight ZA, Shokat KM. Targeting the gatekeeper residue in phosphoinositide 3-kinases. Bioorg Med Chem. 2005 Apr 15; 13(8):2825-36.

    (PMID 15781393) (PDF)

  • Chen X, Ye H, Kuruvilla R, Ramanan N, Scangos KW, Zhang C, Johnson NM, England PM, Shokat KM, Ginty DD. A chemical-genetic approach to studying neurotrophin signaling. Neuron. 2005 Apr 07; 46(1):13-21.

    (PMID 15820690) (PDF)

  • Muratani M, Kung C, Shokat KM, Tansey WP. The F box protein Dsg1/Mdm30 is a transcriptional coactivator that stimulates Gal4 turnover and cotranscriptional mRNA processing. Cell. 2005 Mar 25; 120(6):887-99.

    (PMID 15797387) (PDF)

  • Kung C, Kenski DM, Dickerson SH, Howson RW, Kuyper LF, Madhani HD, Shokat KM. Chemical genomic profiling to identify intracellular targets of a multiplex kinase inhibitor. Proc Natl Acad Sci U S A. 2005 Mar 08; 102(10):3587-92.

    (PMID 15738404) (PDF)

  • Kung C, Shokat KM. Small-molecule kinase-inhibitor target assessment. Chembiochem. 2005 Mar; 6(3):523-6.

    (PMID 15696508) (PDF)

  • Jones MH, Huneycutt BJ, Pearson CG, Zhang C, Morgan G, Shokat K, Bloom K, Winey M. Chemical genetics reveals a role for Mps1 kinase in kinetochore attachment during mitosis. Curr Biol. 2005 Jan 26; 15(2):160-5.

    (PMID 15668173) (PDF)

  • Wong S, McLaughlin J, Cheng D, Zhang C, Shokat KM, Witte ON. Sole BCR-ABL inhibition is insufficient to eliminate all myeloproliferative disorder cell populations. Proc Natl Acad Sci U S A. 2004 Dec 14; 101(50):17456-61.

    (PMID 15505216) (PDF)

  • Knight ZA, Chiang GG, Alaimo PJ, Kenski DM, Ho CB, Coan K, Abraham RT, Shokat KM. Isoform-specific phosphoinositide 3-kinase inhibitors from an arylmorpholine scaffold. Bioorg Med Chem. 2004 Sep 01; 12(17):4749-59.

    (PMID 15358300) (PDF)

  • Maly DJ, Allen JA, Shokat KM. A mechanism-based cross-linker for the identification of kinase-substrate pairs. J Am Chem Soc. 2004 Aug 04; 126(30):9160-1.

    (PMID 15281787) (PDF)

  • Kunkel EJ, Plavec I, Nguyen D, Melrose J, Rosler ES, Kao LT, Wang Y, Hytopoulos E, Bishop AC, Bateman R, Shokat KM, Butcher EC, Berg EL. Rapid structure-activity and selectivity analysis of kinase inhibitors by BioMAP analysis in complex human primary cell-based models. Assay Drug Dev Technol. 2004 Aug; 2(4):431-41.

    (PMID 15357924) (PDF)

  • Simon MD, Sato K, Weiss GA, Shokat KM. A phage display selection of engrailed homeodomain mutants and the importance of residue Q50. Nucleic Acids Res. 2004 Jul 9; 32(12):3623-31.

    (PMID 15247345) (PDF)

  • Simon MD, Shokat KM. Adaptability at a protein-DNA interface: re-engineering the engrailed homeodomain to recognize an unnatural nucleotide. J Am Chem Soc. 2004 Jul 07; 126(26):8078-9.

    (PMID 15225024) (PDF)

  • Sato K, Simon MD, Levin AM, Shokat KM, Weiss GA. Dissecting the Engrailed homeodomain-DNA interaction by phage-displayed shotgun scanning. Chem Biol. 2004 Jul; 11(7):1017-23.

    (PMID 15271360) (PDF)

  • Blethrow J, Zhang C, Shokat KM, Weiss EL. Design and use of analog-sensitive protein kinases. Curr Protoc Mol Biol. 2004 May; Chapter 18:Unit 18.11.

    (PMID 18265343) (PDF)

  • Provance DW, Gourley CR, Silan CM, Cameron LC, Shokat KM, Goldenring JR, Shah K, Gillespie PG, Mercer JA. Chemical-genetic inhibition of a sensitized mutant myosin Vb demonstrates a role in peripheral-pericentriolar membrane traffic. Proc Natl Acad Sci U S A. 2004 Feb 17; 101(7):1868-73.

    (PMID 14766983) (PDF)

  • Liu Y, Kung C, Fishburn J, Ansari AZ, Shokat KM, Hahn S. Two cyclin-dependent kinases promote RNA polymerase II transcription and formation of the scaffold complex. Mol Cell Biol. 2004 Feb; 24(4):1721-35.

    (PMID 14749387) (PDF)

  • Hindley AD, Park S, Wang L, Shah K, Wang Y, Hu X, Shokat KM, Kolch W, Sedivy JM, Yeung KC. Engineering the serine/threonine protein kinase Raf-1 to utilise an orthogonal analogue of ATP substituted at the N6 position. FEBS Lett. 2004 Jan 02; 556(1-3):26-34.

    (PMID 14706820) (PDF)

  • Wan L, de los Santos T, Zhang C, Shokat K, Hollingsworth NM. Mek1 kinase activity functions downstream of RED1 in the regulation of meiotic double strand break repair in budding yeast. Mol Biol Cell. 2004 Jan; 15(1):11-23.

    (PMID 14595109) (PDF)

  • Fan QW, Specht KM, Zhang C, Goldenberg DD, Shokat KM, Weiss WA. Combinatorial efficacy achieved through two-point blockade within a signaling pathway-a chemical genetic approach. Cancer Res. 2003 Dec 15; 63(24):8930-8.

    (PMID 14695210) (PDF)

  • Papa FR, Zhang C, Shokat K, Walter P. Bypassing a kinase activity with an ATP-competitive drug. Science. 2003 Nov 28; 302(5650):1533-7.

    (PMID 14564015) (PDF)

  • Ubersax JA, Woodbury EL, Quang PN, Paraz M, Blethrow JD, Shah K, Shokat KM, Morgan DO. Targets of the cyclin-dependent kinase Cdk1. Nature. 2003 Oct 23; 425(6960):859-64.

    (PMID 14574415) (PDF)

  • Sekiya-Kawasaki M, Groen AC, Cope MJ, Kaksonen M, Watson HA, Zhang C, Shokat KM, Wendland B, McDonald KL, McCaffery JM, Drubin DG. Dynamic phosphoregulation of the cortical actin cytoskeleton and endocytic machinery revealed by real-time chemical genetic analysis. J Cell Biol. 2003 Sep 01; 162(5):765-72.

    (PMID 12952930) (PDF)

  • Sreenivasan A, Bishop AC, Shokat KM, Kellogg DR. Specific inhibition of Elm1 kinase activity reveals functions required for early G1 events. Mol Cell Biol. 2003 Sep; 23(17):6327-37.

    (PMID 12917352) (PDF)

  • Knight ZA, Schilling B, Row RH, Kenski DM, Gibson BW, Shokat KM. Phosphospecific proteolysis for mapping sites of protein phosphorylation. Nat Biotechnol. 2003 Sep; 21(9):1047-54.

    (PMID 12923550) (PDF)

  • Denzel A, Hare KJ, Zhang C, Shokat K, Jenkinson EJ, Anderson G, Hayday A. Cutting edge: a chemical genetic system for the analysis of kinases regulating T cell development. J Immunol. 2003 Jul 15; 171(2):519-23.

    (PMID 12847211) (PDF)

  • Ulrich SM, Kenski DM, Shokat KM. Engineering a “methionine clamp” into Src family kinases enhances specificity toward unnatural ATP analogues. Biochemistry. 2003 Jul 08; 42(26):7915-21.

    (PMID 12834343) (PDF)

  • Benjamin KR, Zhang C, Shokat KM, Herskowitz I. Control of landmark events in meiosis by the CDK Cdc28 and the meiosis-specific kinase Ime2. Genes Dev. 2003 Jun 15; 17(12):1524-39.

    (PMID 12783856) (PDF)

  • Eblen ST, Kumar NV, Shah K, Henderson MJ, Watts CK, Shokat KM, Weber MJ. Identification of novel ERK2 substrates through use of an engineered kinase and ATP analogs. J Biol Chem. 2003 Apr 25; 278(17):14926-35.

    (PMID 12594221) (PDF)

  • Wang H, Shimizu E, Tang YP, Cho M, Kyin M, Zuo W, Robinson DA, Alaimo PJ, Zhang C, Morimoto H, Zhuo M, Feng R, Shokat KM, Tsien JZ. Inducible protein knockout reveals temporal requirement of CaMKII reactivation for memory consolidation in the brain. Proc Natl Acad Sci U S A. 2003 Apr 01; 100(7):4287-92.

    (PMID 12646704) (PDF)

  • Abeliovich H, Zhang C, Dunn WA, Shokat KM, Klionsky DJ. Chemical genetic analysis of Apg1 reveals a non-kinase role in the induction of autophagy. Mol Biol Cell. 2003 Feb; 14(2):477-90.

    (PMID 12589048) (PDF)

  • Shah K, Shokat KM. A chemical genetic approach for the identification of direct substrates of protein kinases. Methods Mol Biol. 2003; 233:253-71.

    (PMID 12840513) (PDF)

  • Ulrich SM, Sallee NA, Shokat KM. Conformational restraint is a critical determinant of unnatural nucleotide recognition by protein kinases. Bioorg Med Chem Lett. 2002 Nov 04; 12(21):3223-7.

    (PMID 12372539) (PDF)

  • Kraybill BC, Elkin LL, Blethrow JD, Morgan DO, Shokat KM. Inhibitor scaffolds as new allele specific kinase substrates. J Am Chem Soc. 2002 Oct 16; 124(41):12118-28.

    (PMID 12371851) (PDF)

  • Buzko O, Shokat KM. A kinase sequence database: sequence alignments and family assignment. Bioinformatics. 2002 Sep; 18(9):1274-5.

    (PMID 12217924) (PDF)

  • Weiss EL, Kurischko C, Zhang C, Shokat K, Drubin DG, Luca FC. The Saccharomyces cerevisiae Mob2p-Cbk1p kinase complex promotes polarized growth and acts with the mitotic exit network to facilitate daughter cell-specific localization of Ace2p transcription factor. J Cell Biol. 2002 Sep 02; 158(5):885-900.

    (PMID 12196508) (PDF)

  • Fan QW, Zhang C, Shokat KM, Weiss WA. Chemical genetic blockade of transformation reveals dependence on aberrant oncogenic signaling. Curr Biol. 2002 Aug 20; 12(16):1386-94.

    (PMID 12194819) (PDF)

  • Shokat K, Velleca M. Novel chemical genetic approaches to the discovery of signal transduction inhibitors. Drug Discov Today. 2002 Aug 15; 7(16):872-9.

    (PMID 12546954) (PDF)

  • Niswender CM, Ishihara RW, Judge LM, Zhang C, Shokat KM, McKnight GS. Protein engineering of protein kinase A catalytic subunits results in the acquisition of novel inhibitor sensitivity. J Biol Chem. 2002 Aug 09; 277(32):28916-22.

    (PMID 12034735) (PDF)

  • Specht KM, Shokat KM. The emerging power of chemical genetics. Curr Opin Cell Biol. 2002 Apr; 14(2):155-9.

    (PMID 11891113) (PDF)

  • Holt JR, Gillespie SK, Provance DW, Shah K, Shokat KM, Corey DP, Mercer JA, Gillespie PG. A chemical-genetic strategy implicates myosin-1c in adaptation by hair cells. Cell. 2002 Feb 08; 108(3):371-81.

    (PMID 11853671) (PDF)

  • Alaimo PJ, Shogren-Knaak MA, Shokat KM. Chemical genetic analysis of protein kinase cascades. ScientificWorldJournal. 2002 Feb 5; 2:108-110.

    (PMID 29973826) (PDF)

  • Buzko OV, Bishop AC, Shokat KM. Modified AutoDock for accurate docking of protein kinase inhibitors. J Comput Aided Mol Des. 2002 Feb; 16(2):113-27.

    (PMID 12188021) (PDF)

  • Shah K, Shokat KM. A chemical genetic screen for direct v-Src substrates reveals ordered assembly of a retrograde signaling pathway. Chem Biol. 2002 Jan; 9(1):35-47.

    (PMID 11841937) (PDF)

  • Witucki LA, Huang X, Shah K, Liu Y, Kyin S, Eck MJ, Shokat KM. Mutant tyrosine kinases with unnatural nucleotide specificity retain the structure and phospho-acceptor specificity of the wild-type enzyme. Chem Biol. 2002 Jan; 9(1):25-33.

    (PMID 11841936) (PDF)

  • Ulrich S, Shokat K. Green fluorescent protein-based protein kinase biosensor substrates. Methods Mol Biol. 2002; 183:275-85.

    (PMID 12136762) (PDF)

  • Carroll AS, Bishop AC, DeRisi JL, Shokat KM, O’Shea EK. Chemical inhibition of the Pho85 cyclin-dependent kinase reveals a role in the environmental stress response. Proc Natl Acad Sci U S A. 2001 Oct 23; 98(22):12578-83.

    (PMID 11675494) (PDF)

  • Alaimo PJ, Shogren-Knaak MA, Shokat KM. Chemical genetic approaches for the elucidation of signaling pathways. Curr Opin Chem Biol. 2001 Aug; 5(4):360-7.

    (PMID 11470597) (PDF)

  • Schauder S, Shokat K, Surette MG, Bassler BL. The LuxS family of bacterial autoinducers: biosynthesis of a novel quorum-sensing signal molecule. Mol Microbiol. 2001 Jul; 41(2):463-76.

    (PMID 11489131) (PDF)

  • Habelhah H, Shah K, Huang L, Burlingame AL, Shokat KM, Ronai Z. Identification of new JNK substrate using ATP pocket mutant JNK and a corresponding ATP analogue. J Biol Chem. 2001 May 25; 276(21):18090-5.

    (PMID 11259409) (PDF)

  • Bishop AC, Buzko O, Shokat KM. Magic bullets for protein kinases. Trends Cell Biol. 2001 Apr; 11(4):167-72.

    (PMID 11306297) (PDF)

  • Habelhah H, Shah K, Huang L, Ostareck-Lederer A, Burlingame AL, Shokat KM, Hentze MW, Ronai Z. ERK phosphorylation drives cytoplasmic accumulation of hnRNP-K and inhibition of mRNA translation. Nat Cell Biol. 2001 Mar; 3(3):325-30.

    (PMID 11231586) (PDF)

  • Ting AY, Witte K, Shah K, Kraybill B, Shokat KM, Schultz PG. Phage-display evolution of tyrosine kinases with altered nucleotide specificity. Biopolymers. 2001; 60(3):220-8. View on PubMed

    (PMID 11774228) (PDF)

  • Shogren-Knaak MA, Alaimo PJ, Shokat KM. Recent advances in chemical approaches to the study of biological systems. Annu Rev Cell Dev Biol. 2001; 17:405-33.

    (PMID 11687495) (PDF)

  • Liu Y, Witucki LA, Shah K, Bishop AC, Shokat KM. Src-Abl tyrosine kinase chimeras: replacement of the adenine binding pocket of c-Abl with v-Src to swap nucleotide and inhibitor specificities. Biochemistry. 2000 Nov 28; 39(47):14400-8.

    (PMID 11087392) (PDF)

  • Weiss EL, Bishop AC, Shokat KM, Drubin DG. Chemical genetic analysis of the budding-yeast p21-activated kinase Cla4p. Nat Cell Biol. 2000 Oct; 2(10):677-85.

    (PMID 11025657) (PDF)

  • Bishop AC, Ubersax JA, Petsch DT, Matheos DP, Gray NS, Blethrow J, Shimizu E, Tsien JZ, Schultz PG, Rose MD, Wood JL, Morgan DO, Shokat KM. A chemical switch for inhibitor-sensitive alleles of any protein kinase. Nature. 2000 Sep 21; 407(6802):395-401.

    (PMID 11014197) (PDF)

  • Weintraub BC, Jun JE, Bishop AC, Shokat KM, Thomas ML, Goodnow CC. Entry of B cell receptor into signaling domains is inhibited in tolerant B cells. J Exp Med. 2000 Apr 17; 191(8):1443-8.

    (PMID 10770810) (PDF)

  • Bishop A, Buzko O, Heyeck-Dumas S, Jung I, Kraybill B, Liu Y, Shah K, Ulrich S, Witucki L, Yang F, Zhang C, Shokat KM. Unnatural ligands for engineered proteins: new tools for chemical genetics. Annu Rev Biophys Biomol Struct. 2000; 29:577-606.

    (PMID 10940260) (PDF)

  • Gillespie PG, Gillespie SK, Mercer JA, Shah K, Shokat KM. Engineering of the myosin-ibeta nucleotide-binding pocket to create selective sensitivity to N(6)-modified ADP analogs. J Biol Chem. 1999 Oct 29; 274(44):31373-81.

    (PMID 10531338) (PDF)

  • Buzko OV, Shokat KM. Blocking HIV entry. Nat Struct Biol. 1999 Oct; 6(10):906-8. View on PubMed

    (PMID 10504719) (PDF)

  • Liu Y, Bishop A, Witucki L, Kraybill B, Shimizu E, Tsien J, Ubersax J, Blethrow J, Morgan DO, Shokat KM. Structural basis for selective inhibition of Src family kinases by PP1. Chem Biol. 1999 Sep; 6(9):671-8.

    (PMID 10467133) (PDF)

  • Bishop AC, Shokat KM. Acquisition of inhibitor-sensitive protein kinases through protein design. Pharmacol Ther. 1999 May-Jun; 82(2-3):337-46.

    (PMID 10454210) (PDF)

  • Yang F, Liu Y, Bixby SD, Friedman JD, Shokat KM. Highly efficient green fluorescent protein-based kinase substrates. Anal Biochem. 1999 Jan 15; 266(2):167-73.

    (PMID 9888972) (PDF)

  • Liu Y, Shah K, Yang F, Witucki L, Shokat KM. A molecular gate which controls unnatural ATP analogue recognition by the tyrosine kinase v-Src. Bioorg Med Chem. 1998 Aug; 6(8):1219-26.

    (PMID 9784863) (PDF)

  • Surrey T, Elowitz MB, Wolf PE, Yang F, Nédélec F, Shokat K, Leibler S. Chromophore-assisted light inactivation and self-organization of microtubules and motors. Proc Natl Acad Sci U S A. 1998 Apr 14; 95(8):4293-8.

    (PMID 9539730) (PDF)

  • Bishop AC, Shah K, Liu Y, Witucki L, Kung C, Shokat KM. Design of allele-specific inhibitors to probe protein kinase signaling. Curr Biol. 1998 Feb 26; 8(5):257-66.

    (PMID 9501066) (PDF)

  • Liu Y, Shah K, Yang F, Witucki L, Shokat KM. Engineering Src family protein kinases with unnatural nucleotide specificity. Chem Biol. 1998 Feb; 5(2):91-101.

    (PMID 9495830) (PDF)

  • Shah K, Liu Y, Deirmengian C, Shokat KM. Engineering unnatural nucleotide specificity for Rous sarcoma virus tyrosine kinase to uniquely label its direct substrates. Proc Natl Acad Sci U S A. 1997 Apr 15; 94(8):3565-70.

    (PMID 9108016) (PDF)

  • Liblau RS, Tisch R, Shokat K, Yang X, Dumont N, Goodnow CC, McDevitt HO. Intravenous injection of soluble antigen induces thymic and peripheral T-cells apoptosis. Proc Natl Acad Sci U S A. 1996 Apr 02; 93(7):3031-6.

    (PMID 8610163) (PDF)

  • Shokat KM. Tyrosine kinases: modular signaling enzymes with tunable specificities. Chem Biol. 1995 Aug; 2(8):509-14.

    (PMID 9383454) (PDF)

  • Shokat KM, Goodnow CC. Antigen-induced B-cell death and elimination during germinal-centre immune responses. Nature. 1995 May 25; 375(6529):334-8.

    (PMID 7753200) (PDF)

  • Liblau RS, Pearson CI, Shokat K, Tisch R, Yang XD, McDevitt HO. High-dose soluble antigen: peripheral T-cell proliferation or apoptosis. Immunol Rev. 1994 Dec; 142:193-208.

    (PMID 7698794) (PDF)

  • Cooke MP, Heath AW, Shokat KM, Zeng Y, Finkelman FD, Linsley PS, Howard M, Goodnow CC. Immunoglobulin signal transduction guides the specificity of B cell-T cell interactions and is blocked in tolerant self-reactive B cells. J Exp Med. 1994 Feb 01; 179(2):425-38.

    (PMID 8294858) (PDF)

  • Shokat KM, Schultz PG. Catalytic antibodies. Methods Enzymol. 1991; 203:327-51.

    (PMID 1762563) (PDF)

  • Shokat KM, Schultz PG. The generation of antibody combining sites containing catalytic residues. Ciba Found Symp. 1991; 159:118-28; discussion 128-34.

    (PMID 1959444)

  • Shokat KM, Schultz PG. Catalytic antibodies. Annu Rev Immunol. 1990; 8:335-63.

    (PMID 2188666) (PDF)

  • Shokat KM, Leumann CJ, Sugasawara R, Schultz PG. A new strategy for the generation of catalytic antibodies. Nature. 1989 Mar 16; 338(6212):269-71.

    (PMID 2922053) (PDF)

  • McClard RW, Shokat KM. Does the bifunctional uridylate synthase channel orotidine 5’-phosphate? Kinetics of orotate phosphoribosyltransferase and orotidylate decarboxylase activities fit a noninteracting sites model. Biochemistry. 1987 Jun 16; 26(12):3378-84.

    (PMID 3651388) (PDF)