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Coordinating Tissue Regeneration Through Transforming Growth Factor-β Activated Kinase 1 Inactivation and Reactivation.
Hsieh HHS, Agarwal S, Cholok DJ, Loder SJ, Kaneko K, Huber A, Chung MT, Ranganathan K, Habbouche J, Li J, Butts J, Reimer J, Kaura A, Drake J, Breuler C, Priest CR, Nguyen J, Brownley C, Peterson J, Ozgurel SU, Niknafs YS, Li S, Inagaki M, Scott G, Krebsbach PH, Longaker MT, Westover K, Gray N, Ninomiya-Tsuji J, Mishina Y, Levi B. Hsieh HHS, et al. Among authors: westover k. Stem Cells. 2019 Jun;37(6):766-778. doi: 10.1002/stem.2991. Epub 2019 Mar 14. Stem Cells. 2019. PMID: 30786091 Free PMC article.
Characterization of Torin2, an ATP-competitive inhibitor of mTOR, ATM, and ATR.
Liu Q, Xu C, Kirubakaran S, Zhang X, Hur W, Liu Y, Kwiatkowski NP, Wang J, Westover KD, Gao P, Ercan D, Niepel M, Thoreen CC, Kang SA, Patricelli MP, Wang Y, Tupper T, Altabef A, Kawamura H, Held KD, Chou DM, Elledge SJ, Janne PA, Wong KK, Sabatini DM, Gray NS. Liu Q, et al. Cancer Res. 2013 Apr 15;73(8):2574-86. doi: 10.1158/0008-5472.CAN-12-1702. Epub 2013 Feb 22. Cancer Res. 2013. PMID: 23436801 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. 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. 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.
Progress on Covalent Inhibition of KRAS(G12C).
Westover KD, Jänne PA, Gray NS. Westover KD, et al. Cancer Discov. 2016 Mar;6(3):233-4. doi: 10.1158/2159-8290.CD-16-0092. Cancer Discov. 2016. PMID: 26951837
Torin2 Suppresses Ionizing Radiation-Induced DNA Damage Repair.
Udayakumar D, Pandita RK, Horikoshi N, Liu Y, Liu Q, Wong KK, Hunt CR, Gray NS, Minna JD, Pandita TK, Westover KD. Udayakumar D, et al. Among authors: westover kd. Radiat Res. 2016 May;185(5):527-38. doi: 10.1667/RR14373.1. Epub 2016 May 2. Radiat Res. 2016. PMID: 27135971 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.
Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors.
Tan L, Gurbani D, Weisberg EL, Jones DS, Rao S, Singer WD, Bernard FM, Mowafy S, Jenney A, Du G, Nonami A, Griffin JD, Lauffenburger DA, Westover KD, Sorger PK, Gray NS. Tan L, et al. Among authors: westover kd. Bioorg Med Chem. 2017 Feb 15;25(4):1320-1328. doi: 10.1016/j.bmc.2016.11.034. Epub 2016 Dec 7. Bioorg Med Chem. 2017. PMID: 28038940 Free PMC article.
Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype.
Olson CM, Liang Y, Leggett A, Park WD, Li L, Mills CE, Elsarrag SZ, Ficarro SB, Zhang T, Düster R, Geyer M, Sim T, Marto JA, Sorger PK, Westover KD, Lin CY, Kwiatkowski N, Gray NS. Olson CM, et al. Among authors: westover kd. Cell Chem Biol. 2019 Jun 20;26(6):792-803.e10. doi: 10.1016/j.chembiol.2019.02.012. Epub 2019 Mar 21. Cell Chem Biol. 2019. PMID: 30905681 Free PMC article.
133 results