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Kinome-wide selectivity profiling of ATP-competitive mammalian target of rapamycin (mTOR) inhibitors and characterization of their binding kinetics.
Liu Q, Kirubakaran S, Hur W, Niepel M, Westover K, Thoreen CC, Wang J, Ni J, Patricelli MP, Vogel K, Riddle S, Waller DL, Traynor R, Sanda T, Zhao Z, Kang SA, Zhao J, Look AT, Sorger PK, Sabatini DM, Gray NS. Liu Q, et al. J Biol Chem. 2012 Mar 23;287(13):9742-9752. doi: 10.1074/jbc.M111.304485. Epub 2012 Jan 5. J Biol Chem. 2012. PMID: 22223645 Free PMC article.
Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2).
Tan L, Nomanbhoy T, Gurbani D, Patricelli M, Hunter J, Geng J, Herhaus L, Zhang J, Pauls E, Ham Y, Choi HG, Xie T, Deng X, Buhrlage SJ, Sim T, Cohen P, Sapkota G, Westover KD, Gray NS. Tan L, et al. Among authors: westover kd. J Med Chem. 2015 Jan 8;58(1):183-96. doi: 10.1021/jm500480k. Epub 2014 Jul 30. J Med Chem. 2015. PMID: 25075558 Free PMC article.
Pharmacological targeting of the pseudokinase Her3.
Xie T, Lim SM, Westover KD, Dodge ME, Ercan D, Ficarro SB, Udayakumar D, Gurbani D, Tae HS, Riddle SM, Sim T, Marto JA, Jänne PA, Crews CM, Gray NS. Xie T, et al. Among authors: westover kd. Nat Chem Biol. 2014 Dec;10(12):1006-12. doi: 10.1038/nchembio.1658. Epub 2014 Oct 19. Nat Chem Biol. 2014. PMID: 25326665 Free PMC article.
Development of small molecules targeting the pseudokinase Her3.
Lim SM, Xie T, Westover KD, Ficarro SB, Tae HS, Gurbani D, Sim T, Marto JA, Jänne PA, Crews CM, Gray NS. Lim SM, et al. Among authors: westover kd. Bioorg Med Chem Lett. 2015 Aug 15;25(16):3382-9. doi: 10.1016/j.bmcl.2015.04.103. Epub 2015 May 11. Bioorg Med Chem Lett. 2015. PMID: 26094118 Free PMC article.
Structural dataset for the fast-exchanging KRAS G13D.
Lu J, Hunter J, Manandhar A, Gurbani D, Westover KD. Lu J, et al. Among authors: westover kd. Data Brief. 2015 Oct 17;5:572-8. doi: 10.1016/j.dib.2015.10.001. eCollection 2015 Dec. Data Brief. 2015. PMID: 26958611 Free PMC article.
Structure-guided development of covalent TAK1 inhibitors.
Tan L, Gurbani D, Weisberg EL, Hunter JC, Li L, Jones DS, Ficarro SB, Mowafy S, Tam CP, Rao S, Du G, Griffin JD, Sorger PK, Marto JA, Westover KD, Gray NS. Tan L, et al. Among authors: westover kd. Bioorg Med Chem. 2017 Feb 1;25(3):838-846. doi: 10.1016/j.bmc.2016.11.035. Epub 2016 Dec 9. Bioorg Med Chem. 2017. PMID: 28011204 Free PMC article.
112 results