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Page 1
Pharmacological Induction of RAS-GTP Confers RAF Inhibitor Sensitivity in KRAS Mutant Tumors.
Yen I, Shanahan F, Merchant M, Orr C, Hunsaker T, Durk M, La H, Zhang X, Martin SE, Lin E, Chan J, Yu Y, Amin D, Neve RM, Gustafson A, Venkatanarayan A, Foster SA, Rudolph J, Klijn C, Malek S. Yen I, et al. Among authors: malek s. Cancer Cell. 2018 Oct 8;34(4):611-625.e7. doi: 10.1016/j.ccell.2018.09.002. Cancer Cell. 2018. PMID: 30300582 Free article.
RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth.
Hatzivassiliou G, Song K, Yen I, Brandhuber BJ, Anderson DJ, Alvarado R, Ludlam MJ, Stokoe D, Gloor SL, Vigers G, Morales T, Aliagas I, Liu B, Sideris S, Hoeflich KP, Jaiswal BS, Seshagiri S, Koeppen H, Belvin M, Friedman LS, Malek S. Hatzivassiliou G, et al. Among authors: malek s. Nature. 2010 Mar 18;464(7287):431-5. doi: 10.1038/nature08833. Epub 2010 Feb 3. Nature. 2010. PMID: 20130576
Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity.
Maurer T, Garrenton LS, Oh A, Pitts K, Anderson DJ, Skelton NJ, Fauber BP, Pan B, Malek S, Stokoe D, Ludlam MJ, Bowman KK, Wu J, Giannetti AM, Starovasnik MA, Mellman I, Jackson PK, Rudolph J, Wang W, Fang G. Maurer T, et al. Among authors: malek s. Proc Natl Acad Sci U S A. 2012 Apr 3;109(14):5299-304. doi: 10.1073/pnas.1116510109. Epub 2012 Mar 19. Proc Natl Acad Sci U S A. 2012. PMID: 22431598 Free PMC article.
Noncovalent wild-type-sparing inhibitors of EGFR T790M.
Lee HJ, Schaefer G, Heffron TP, Shao L, Ye X, Sideris S, Malek S, Chan E, Merchant M, La H, Ubhayakar S, Yauch RL, Pirazzoli V, Politi K, Settleman J. Lee HJ, et al. Among authors: malek s. Cancer Discov. 2013 Feb;3(2):168-81. doi: 10.1158/2159-8290.CD-12-0357. Epub 2012 Dec 10. Cancer Discov. 2013. PMID: 23229345 Free PMC article.
Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase.
Dragovich PS, Fauber BP, Corson LB, Ding CZ, Eigenbrot C, Ge H, Giannetti AM, Hunsaker T, Labadie S, Liu Y, Malek S, Pan B, Peterson D, Pitts K, Purkey HE, Sideris S, Ultsch M, VanderPorten E, Wei B, Xu Q, Yen I, Yue Q, Zhang H, Zhang X. Dragovich PS, et al. Among authors: malek s. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3186-94. doi: 10.1016/j.bmcl.2013.04.001. Epub 2013 Apr 10. Bioorg Med Chem Lett. 2013. PMID: 23628333
Combination drug scheduling defines a "window of opportunity" for chemopotentiation of gemcitabine by an orally bioavailable, selective ChK1 inhibitor, GNE-900.
Blackwood E, Epler J, Yen I, Flagella M, O'Brien T, Evangelista M, Schmidt S, Xiao Y, Choi J, Kowanetz K, Ramiscal J, Wong K, Jakubiak D, Yee S, Cain G, Gazzard L, Williams K, Halladay J, Jackson PK, Malek S. Blackwood E, et al. Among authors: malek s. Mol Cancer Ther. 2013 Oct;12(10):1968-80. doi: 10.1158/1535-7163.MCT-12-1218. Epub 2013 Jul 19. Mol Cancer Ther. 2013. PMID: 23873850
Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers.
Hatzivassiliou G, Haling JR, Chen H, Song K, Price S, Heald R, Hewitt JF, Zak M, Peck A, Orr C, Merchant M, Hoeflich KP, Chan J, Luoh SM, Anderson DJ, Ludlam MJ, Wiesmann C, Ultsch M, Friedman LS, Malek S, Belvin M. Hatzivassiliou G, et al. Among authors: malek s. Nature. 2013 Sep 12;501(7466):232-6. doi: 10.1038/nature12441. Epub 2013 Aug 11. Nature. 2013. PMID: 23934108
Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase.
Fauber BP, Dragovich PS, Chen J, Corson LB, Ding CZ, Eigenbrot C, Giannetti AM, Hunsaker T, Labadie S, Liu Y, Liu Y, Malek S, Peterson D, Pitts K, Sideris S, Ultsch M, VanderPorten E, Wang J, Wei B, Yen I, Yue Q. Fauber BP, et al. Among authors: malek s. Bioorg Med Chem Lett. 2013 Oct 15;23(20):5533-9. doi: 10.1016/j.bmcl.2013.08.060. Epub 2013 Aug 22. Bioorg Med Chem Lett. 2013. PMID: 24012183
Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.
Dragovich PS, Fauber BP, Boggs J, Chen J, Corson LB, Ding CZ, Eigenbrot C, Ge H, Giannetti AM, Hunsaker T, Labadie S, Li C, Liu Y, Liu Y, Ma S, Malek S, Peterson D, Pitts KE, Purkey HE, Robarge K, Salphati L, Sideris S, Ultsch M, VanderPorten E, Wang J, Wei B, Xu Q, Yen I, Yue Q, Zhang H, Zhang X, Zhou A. Dragovich PS, et al. Among authors: malek s. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3764-71. doi: 10.1016/j.bmcl.2014.06.076. Epub 2014 Jul 1. Bioorg Med Chem Lett. 2014. PMID: 25037916
398 results