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Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor.
Janes MR, Zhang J, Li LS, Hansen R, Peters U, Guo X, Chen Y, Babbar A, Firdaus SJ, Darjania L, Feng J, Chen JH, Li S, Li S, Long YO, Thach C, Liu Y, Zarieh A, Ely T, Kucharski JM, Kessler LV, Wu T, Yu K, Wang Y, Yao Y, Deng X, Zarrinkar PP, Brehmer D, Dhanak D, Lorenzi MV, Hu-Lowe D, Patricelli MP, Ren P, Liu Y. Janes MR, et al. Among authors: zarrinkar pp. Cell. 2018 Jan 25;172(3):578-589.e17. doi: 10.1016/j.cell.2018.01.006. Cell. 2018. PMID: 29373830 Free article.
The reactivity-driven biochemical mechanism of covalent KRASG12C inhibitors.
Hansen R, Peters U, Babbar A, Chen Y, Feng J, Janes MR, Li LS, Ren P, Liu Y, Zarrinkar PP. Hansen R, et al. Among authors: zarrinkar pp. Nat Struct Mol Biol. 2018 Jun;25(6):454-462. doi: 10.1038/s41594-018-0061-5. Epub 2018 May 14. Nat Struct Mol Biol. 2018. PMID: 29760531
KRAS G12C NSCLC Models Are Sensitive to Direct Targeting of KRAS in Combination with PI3K Inhibition.
Misale S, Fatherree JP, Cortez E, Li C, Bilton S, Timonina D, Myers DT, Lee D, Gomez-Caraballo M, Greenberg M, Nangia V, Greninger P, Egan RK, McClanaghan J, Stein GT, Murchie E, Zarrinkar PP, Janes MR, Li LS, Liu Y, Hata AN, Benes CH. Misale S, et al. Among authors: zarrinkar pp. Clin Cancer Res. 2019 Jan 15;25(2):796-807. doi: 10.1158/1078-0432.CCR-18-0368. Epub 2018 Oct 16. Clin Cancer Res. 2019. PMID: 30327306
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.
Carter TA, Wodicka LM, Shah NP, Velasco AM, Fabian MA, Treiber DK, Milanov ZV, Atteridge CE, Biggs WH 3rd, Edeen PT, Floyd M, Ford JM, Grotzfeld RM, Herrgard S, Insko DE, Mehta SA, Patel HK, Pao W, Sawyers CL, Varmus H, Zarrinkar PP, Lockhart DJ. Carter TA, et al. Among authors: zarrinkar pp. Proc Natl Acad Sci U S A. 2005 Aug 2;102(31):11011-6. doi: 10.1073/pnas.0504952102. Epub 2005 Jul 26. Proc Natl Acad Sci U S A. 2005. PMID: 16046538 Free PMC article.
Comprehensive analysis of kinase inhibitor selectivity.
Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. Davis MI, et al. Among authors: zarrinkar pp. Nat Biotechnol. 2011 Oct 30;29(11):1046-51. doi: 10.1038/nbt.1990. Nat Biotechnol. 2011. PMID: 22037378
Discovery and optimization of a highly efficacious class of 5-aryl-2-aminopyridines as FMS-like tyrosine kinase 3 (FLT3) inhibitors.
Liu G, Abraham S, Liu X, Xu S, Rooks AM, Nepomuceno R, Dao A, Brigham D, Gitnick D, Insko DE, Gardner MF, Zarrinkar PP, Christopher R, Belli B, Armstrong RC, Holladay MW. Liu G, et al. Among authors: zarrinkar pp. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3436-41. doi: 10.1016/j.bmcl.2015.07.023. Epub 2015 Jul 14. Bioorg Med Chem Lett. 2015. PMID: 26208887
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