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Items: 1 to 50 of 299

1.

Disease-Causing Mutations in the G Protein Gαs Subvert the Roles of GDP and GTP.

Hu Q, Shokat KM.

Cell. 2018 Apr 1. pii: S0092-8674(18)30298-8. doi: 10.1016/j.cell.2018.03.018. [Epub ahead of print]

PMID:
29628140
2.

Novel K-Ras G12C Switch-II Covalent Binders Destabilize Ras and Accelerate Nucleotide Exchange.

Nnadi CI, Jenkins ML, Gentile DR, Bateman LA, Zaidman D, Balius TE, Nomura DK, Burke JE, Shokat KM, London N.

J Chem Inf Model. 2018 Feb 26;58(2):464-471. doi: 10.1021/acs.jcim.7b00399. Epub 2018 Jan 31.

PMID:
29320178
3.

Stepwise processing analyses of the single-turnover PCSK9 protease reveal its substrate sequence specificity and link clinical genotype to lipid phenotype.

Chorba JS, Galvan AM, Shokat KM.

J Biol Chem. 2018 Feb 9;293(6):1875-1886. doi: 10.1074/jbc.RA117.000754. Epub 2017 Dec 19.

PMID:
29259136
4.

Ras Binder Induces a Modified Switch-II Pocket in GTP and GDP States.

Gentile DR, Rathinaswamy MK, Jenkins ML, Moss SM, Siempelkamp BD, Renslo AR, Burke JE, Shokat KM.

Cell Chem Biol. 2017 Dec 21;24(12):1455-1466.e14. doi: 10.1016/j.chembiol.2017.08.025. Epub 2017 Oct 12.

PMID:
29033317
5.

Inhibition of Calcium Dependent Protein Kinase 1 (CDPK1) by Pyrazolopyrimidine Analogs Decreases Establishment and Reoccurrence of Central Nervous System Disease by Toxoplasma gondii.

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.

J Med Chem. 2017 Dec 28;60(24):9976-9989. doi: 10.1021/acs.jmedchem.7b01192. Epub 2017 Oct 9.

PMID:
28933846
6.

A new generation of mTORC1 inhibitor attenuates alcohol intake and reward in mice.

Morisot N, Novotny CJ, Shokat KM, Ron D.

Addict Biol. 2018 Mar;23(2):713-722. doi: 10.1111/adb.12528. Epub 2017 Jul 6.

PMID:
28681511
7.

Drugging the 'undruggable' cancer targets.

Dang CV, Reddy EP, Shokat KM, Soucek L.

Nat Rev Cancer. 2017 Aug;17(8):502-508. doi: 10.1038/nrc.2017.36. Epub 2017 Jun 23. Review.

PMID:
28643779
8.

Expanding the Scope of Electrophiles Capable of Targeting K-Ras Oncogenes.

McGregor LM, Jenkins ML, Kerwin C, Burke JE, Shokat KM.

Biochemistry. 2017 Jun 27;56(25):3178-3183. doi: 10.1021/acs.biochem.7b00271. Epub 2017 Jun 16.

9.

Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors.

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.

Sci Transl Med. 2017 Jun 14;9(394). pii: eaah6144. doi: 10.1126/scitranslmed.aah6144.

10.

Site-specific incorporation of phosphotyrosine using an expanded genetic code.

Hoppmann C, Wong A, Yang B, Li S, Hunter T, Shokat KM, Wang L.

Nat Chem Biol. 2017 Aug;13(8):842-844. doi: 10.1038/nchembio.2406. Epub 2017 Jun 12.

11.

Ablation of PI3K blocks BCR-ABL leukemogenesis in mice, and a dual PI3K/mTOR inhibitor prevents expansion of human BCR-ABL+ leukemia cells.

Kharas MG, Janes MR, Scarfone VM, Lilly MB, Knight ZA, Shokat KM, Fruman DA.

J Clin Invest. 2017 Jun 1;127(6):2438. doi: 10.1172/JCI95182. Epub 2017 Jun 1. No abstract available.

12.

Farnesyltransferase-Mediated Delivery of a Covalent Inhibitor Overcomes Alternative Prenylation to Mislocalize K-Ras.

Novotny CJ, Hamilton GL, McCormick F, Shokat KM.

ACS Chem Biol. 2017 Jul 21;12(7):1956-1962. doi: 10.1021/acschembio.7b00374. Epub 2017 Jun 19.

PMID:
28530791
13.

Long-term oral kinetin does not protect against α-synuclein-induced neurodegeneration in rodent models of Parkinson's disease.

Orr AL, Rutaganira FU, de Roulet D, Huang EJ, Hertz NT, Shokat KM, Nakamura K.

Neurochem Int. 2017 Oct;109:106-116. doi: 10.1016/j.neuint.2017.04.006. Epub 2017 Apr 20.

PMID:
28434973
14.

A Kinase Inhibitor Targeted to mTORC1 Drives Regression in Glioblastoma.

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.

Cancer Cell. 2017 Mar 13;31(3):424-435. doi: 10.1016/j.ccell.2017.01.014.

15.

INPP4B and PTEN Loss Leads to PI-3,4-P2 Accumulation and Inhibition of PI3K in TNBC.

Reed DE, Shokat KM.

Mol Cancer Res. 2017 Jun;15(6):765-775. doi: 10.1158/1541-7786.MCR-16-0183. Epub 2017 Feb 14.

PMID:
28196852
16.

An Optimized Chromatographic Strategy for Multiplexing In Parallel Reaction Monitoring Mass Spectrometry: Insights from Quantitation of Activated Kinases.

Urisman A, Levin RS, Gordan JD, Webber JT, Hernandez H, Ishihama Y, Shokat KM, Burlingame AL.

Mol Cell Proteomics. 2017 Feb;16(2):265-277. doi: 10.1074/mcp.M116.058172. Epub 2016 Dec 11.

17.

Endosomal Phosphatidylinositol 3-Kinase Is Essential for Canonical GPCR Signaling.

Uchida Y, Rutaganira FU, Jullié D, Shokat KM, von Zastrow M.

Mol Pharmacol. 2017 Jan;91(1):65-73. Epub 2016 Nov 7.

18.

Discovery of new substrates of the elongation factor-2 kinase suggests a broader role in the cellular nutrient response.

Lazarus MB, Levin RS, Shokat KM.

Cell Signal. 2017 Jan;29:78-83. doi: 10.1016/j.cellsig.2016.10.006. Epub 2016 Oct 17.

19.

Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design.

Ostrem JM, Shokat KM.

Nat Rev Drug Discov. 2016 Nov;15(11):771-785. doi: 10.1038/nrd.2016.139. Epub 2016 Jul 29. Review.

PMID:
27469033
20.

Overcoming resistance to HER2 inhibitors through state-specific kinase binding.

Novotny CJ, Pollari S, Park JH, Lemmon MA, Shen W, Shokat KM.

Nat Chem Biol. 2016 Nov;12(11):923-930. doi: 10.1038/nchembio.2171. Epub 2016 Sep 5.

21.

Innate immunity kinase TAK1 phosphorylates Rab1 on a hotspot for posttranslational modifications by host and pathogen.

Levin RS, Hertz NT, Burlingame AL, Shokat KM, Mukherjee S.

Proc Natl Acad Sci U S A. 2016 Aug 16;113(33):E4776-83. doi: 10.1073/pnas.1608355113. Epub 2016 Aug 1.

22.

Synthetic Lethal Targeting of ARID1A-Mutant Ovarian Clear Cell Tumors with Dasatinib.

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.

Mol Cancer Ther. 2016 Jul;15(7):1472-84. doi: 10.1158/1535-7163.MCT-15-0554. Epub 2016 Jun 30.

23.

Inhibition of Carbonyl Reductase 1 Safely Improves the Efficacy of Doxorubicin in Breast Cancer Treatment.

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.

Antioxid Redox Signal. 2017 Jan 10;26(2):70-83. doi: 10.1089/ars.2015.6457. Epub 2016 Aug 5.

PMID:
27357096
24.

Overcoming mTOR resistance mutations with a new-generation mTOR inhibitor.

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.

Nature. 2016 Jun 9;534(7606):272-6. doi: 10.1038/nature17963. Epub 2016 May 18.

25.

Isocitrate Dehydrogenase Mutations Confer Dasatinib Hypersensitivity and SRC Dependence in Intrahepatic Cholangiocarcinoma.

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.

Cancer Discov. 2016 Jul;6(7):727-39. doi: 10.1158/2159-8290.CD-15-1442. Epub 2016 May 26.

26.

Multistep Compositional Remodeling of Supported Lipid Membranes by Interfacially Active Phosphatidylinositol Kinases.

Tabaei SR, Guo F, Rutaganira FU, Vafaei S, Choong I, Shokat KM, Glenn JS, Cho NJ.

Anal Chem. 2016 May 17;88(10):5042-5. doi: 10.1021/acs.analchem.6b01293. Epub 2016 Apr 28.

27.

N-Myc Drives Neuroendocrine Prostate Cancer Initiated from Human Prostate Epithelial Cells.

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.

Cancer Cell. 2016 Apr 11;29(4):536-547. doi: 10.1016/j.ccell.2016.03.001. Epub 2016 Mar 31.

28.

Design and Structural Characterization of Potent and Selective Inhibitors of Phosphatidylinositol 4 Kinase IIIβ.

Rutaganira FU, Fowler ML, McPhail JA, Gelman MA, Nguyen K, Xiong A, Dornan GL, Tavshanjian B, Glenn JS, Shokat KM, Burke JE.

J Med Chem. 2016 Mar 10;59(5):1830-9. doi: 10.1021/acs.jmedchem.5b01311. Epub 2016 Feb 26.

29.

Using hydrogen deuterium exchange mass spectrometry to engineer optimized constructs for crystallization of protein complexes: Case study of PI4KIIIβ with Rab11.

Fowler ML, McPhail JA, Jenkins ML, Masson GR, Rutaganira FU, Shokat KM, Williams RL, Burke JE.

Protein Sci. 2016 Apr;25(4):826-39. doi: 10.1002/pro.2879. Epub 2016 Feb 1.

30.

P-TEFb regulation of transcription termination factor Xrn2 revealed by a chemical genetic screen for Cdk9 substrates.

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.

Genes Dev. 2016 Jan 1;30(1):117-31. doi: 10.1101/gad.269589.115.

31.

Analog sensitive chemical inhibition of the DEAD-box protein DDX3.

Floor SN, Barkovich KJ, Condon KJ, Shokat KM, Doudna JA.

Protein Sci. 2016 Mar;25(3):638-49. doi: 10.1002/pro.2857. Epub 2015 Dec 26.

32.

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.

Kuhlenschmidt TB, Rutaganira FU, Long S, Tang K, Shokat KM, Kuhlenschmidt MS, Sibley LD.

Antimicrob Agents Chemother. 2015 Nov 9;60(1):570-9. doi: 10.1128/AAC.01915-15. Print 2016 Jan.

33.

Discovery and functional characterization of a neomorphic PTEN mutation.

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.

Proc Natl Acad Sci U S A. 2015 Nov 10;112(45):13976-81. doi: 10.1073/pnas.1422504112. Epub 2015 Oct 26.

34.

Identification of AMPK Phosphorylation Sites Reveals a Network of Proteins Involved in Cell Invasion and Facilitates Large-Scale Substrate Prediction.

Schaffer BE, Levin RS, Hertz NT, Maures TJ, Schoof ML, Hollstein PE, Benayoun BA, Banko MR, Shaw RJ, Shokat KM, Brunet A.

Cell Metab. 2015 Nov 3;22(5):907-21. doi: 10.1016/j.cmet.2015.09.009. Epub 2015 Oct 8.

35.

Small molecule inhibition of Csk alters affinity recognition by T cells.

Manz BN, Tan YX, Courtney AH, Rutaganira F, Palmer E, Shokat KM, Weiss A.

Elife. 2015 Aug 24;4. doi: 10.7554/eLife.08088.

36.

Discovery and structure of a new inhibitor scaffold of the autophagy initiating kinase ULK1.

Lazarus MB, Shokat KM.

Bioorg Med Chem. 2015 Sep 1;23(17):5483-8. doi: 10.1016/j.bmc.2015.07.034. Epub 2015 Jul 26.

37.

SR protein kinases promote splicing of nonconsensus introns.

Lipp JJ, Marvin MC, Shokat KM, Guthrie C.

Nat Struct Mol Biol. 2015 Aug;22(8):611-7. doi: 10.1038/nsmb.3057. Epub 2015 Jul 13.

PMID:
26167880
38.

WNK1-regulated inhibitory phosphorylation of the KCC2 cotransporter maintains the depolarizing action of GABA in immature neurons.

Friedel P, Kahle KT, Zhang J, Hertz N, Pisella LI, Buhler E, Schaller F, Duan J, Khanna AR, Bishop PN, Shokat KM, Medina I.

Sci Signal. 2015 Jun 30;8(383):ra65. doi: 10.1126/scisignal.aaa0354.

PMID:
26126716
39.

Endoplasmic reticulum stress-independent activation of unfolded protein response kinases by a small molecule ATP-mimic.

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.

Elife. 2015 May 19;4. doi: 10.7554/eLife.05434.

40.

Differential genetic interactions of yeast stress response MAPK pathways.

Martin H, Shales M, Fernandez-Piñar P, Wei P, Molina M, Fiedler D, Shokat KM, Beltrao P, Lim W, Krogan NJ.

Mol Syst Biol. 2015 Apr 17;11(4):800. doi: 10.15252/msb.20145606.

41.

The Tribbles 2 (TRB2) pseudokinase binds to ATP and autophosphorylates in a metal-independent manner.

Bailey FP, Byrne DP, Oruganty K, Eyers CE, Novotny CJ, Shokat KM, Kannan N, Eyers PA.

Biochem J. 2015 Apr 1;467(1):47-62. doi: 10.1042/BJ20141441.

42.

Structure of the human autophagy initiating kinase ULK1 in complex with potent inhibitors.

Lazarus MB, Novotny CJ, Shokat KM.

ACS Chem Biol. 2015 Jan 16;10(1):257-61. doi: 10.1021/cb500835z. Epub 2015 Jan 6.

43.

Overcoming myelosuppression due to synthetic lethal toxicity for FLT3-targeted acute myeloid leukemia therapy.

Warkentin AA, Lopez MS, Lasater EA, Lin K, He BL, Leung AY, Smith CC, Shah NP, Shokat KM.

Elife. 2014 Dec 22;3. doi: 10.7554/eLife.03445.

44.

Radiotherapy followed by aurora kinase inhibition targets tumor-propagating cells in human glioblastoma.

Li N, Maly DJ, Chanthery YH, Sirkis DW, Nakamura JL, Berger MS, James CD, Shokat KM, Weiss WA, Persson AI.

Mol Cancer Ther. 2015 Feb;14(2):419-28. doi: 10.1158/1535-7163.MCT-14-0526. Epub 2014 Dec 18.

45.

Targeting osteosarcoma.

Reed DE, Shokat KM.

Proc Natl Acad Sci U S A. 2014 Dec 23;111(51):18100-1. doi: 10.1073/pnas.1420596111. Epub 2014 Dec 15. No abstract available.

46.

Linking tumor mutations to drug responses via a quantitative chemical-genetic interaction map.

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.

Cancer Discov. 2015 Feb;5(2):154-67. doi: 10.1158/2159-8290.CD-14-0552. Epub 2014 Dec 12.

47.

MST3 kinase phosphorylates TAO1/2 to enable Myosin Va function in promoting spine synapse development.

Ultanir SK, Yadav S, Hertz NT, Oses-Prieto JA, Claxton S, Burlingame AL, Shokat KM, Jan LY, Jan YN.

Neuron. 2014 Dec 3;84(5):968-82. doi: 10.1016/j.neuron.2014.10.025. Epub 2014 Nov 13.

48.

Methods in Enzymology. Protein kinase inhibitors in research and medicine. Preface.

Shokat KM.

Methods Enzymol. 2014;548:xi-xii. doi: 10.1016/B978-0-12-397918-6.09986-9. No abstract available.

PMID:
25399648
49.

The logic and design of analog-sensitive kinases and their small molecule inhibitors.

Lopez MS, Kliegman JI, Shokat KM.

Methods Enzymol. 2014;548:189-213. doi: 10.1016/B978-0-12-397918-6.00008-2. Review.

PMID:
25399647
50.

The proprotein convertase subtilisin/kexin type 9 (PCSK9) active site and cleavage sequence differentially regulate protein secretion from proteolysis.

Chorba JS, Shokat KM.

J Biol Chem. 2014 Oct 17;289(42):29030-43. doi: 10.1074/jbc.M114.594861. Epub 2014 Sep 10.

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