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Discovery of potent and selective covalent inhibitors of JNK.
Zhang T, Inesta-Vaquera F, Niepel M, Zhang J, Ficarro SB, Machleidt T, Xie T, Marto JA, Kim N, Sim T, Laughlin JD, Park H, LoGrasso PV, Patricelli M, Nomanbhoy TK, Sorger PK, Alessi DR, Gray NS. Zhang T, et al. Chem Biol. 2012 Jan 27;19(1):140-54. doi: 10.1016/j.chembiol.2011.11.010. Chem Biol. 2012. PMID: 22284361 Free PMC article.
Therapeutic targeting of oncogenic K-Ras by a covalent catalytic site inhibitor.
Lim SM, Westover KD, Ficarro SB, Harrison RA, Choi HG, Pacold ME, Carrasco M, Hunter J, Kim ND, Xie T, Sim T, Jänne PA, Meyerson M, Marto JA, Engen JR, Gray NS. Lim SM, et al. Among authors: kim nd. Angew Chem Int Ed Engl. 2014 Jan 3;53(1):199-204. doi: 10.1002/anie.201307387. Epub 2013 Nov 20. Angew Chem Int Ed Engl. 2014. PMID: 24259466 Free PMC article.
Targeting transcription regulation in cancer with a covalent CDK7 inhibitor.
Kwiatkowski N, Zhang T, Rahl PB, Abraham BJ, Reddy J, Ficarro SB, Dastur A, Amzallag A, Ramaswamy S, Tesar B, Jenkins CE, Hannett NM, McMillin D, Sanda T, Sim T, Kim ND, Look T, Mitsiades CS, Weng AP, Brown JR, Benes CH, Marto JA, Young RA, Gray NS. Kwiatkowski N, et al. Among authors: kim nd. Nature. 2014 Jul 31;511(7511):616-20. doi: 10.1038/nature13393. Epub 2014 Jun 22. Nature. 2014. PMID: 25043025 Free PMC article.
Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors.
Tan L, Wang J, Tanizaki J, Huang Z, Aref AR, Rusan M, Zhu SJ, Zhang Y, Ercan D, Liao RG, Capelletti M, Zhou W, Hur W, Kim N, Sim T, Gaudet S, Barbie DA, Yeh JR, Yun CH, Hammerman PS, Mohammadi M, Jänne PA, Gray NS. Tan L, et al. Proc Natl Acad Sci U S A. 2014 Nov 11;111(45):E4869-77. doi: 10.1073/pnas.1403438111. Epub 2014 Oct 27. Proc Natl Acad Sci U S A. 2014. PMID: 25349422 Free PMC article.
416 results