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Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers.
Peng SB, Henry JR, Kaufman MD, Lu WP, Smith BD, Vogeti S, Rutkoski TJ, Wise S, Chun L, Zhang Y, Van Horn RD, Yin T, Zhang X, Yadav V, Chen SH, Gong X, Ma X, Webster Y, Buchanan S, Mochalkin I, Huber L, Kays L, Donoho GP, Walgren J, McCann D, Patel P, Conti I, Plowman GD, Starling JJ, Flynn DL. Peng SB, et al. Among authors: zhang x, zhang y. Cancer Cell. 2015 Sep 14;28(3):384-98. doi: 10.1016/j.ccell.2015.08.002. Epub 2015 Sep 3. Cancer Cell. 2015. PMID: 26343583 Free article.
Mouse PDX Trial Suggests Synergy of Concurrent Inhibition of RAF and EGFR in Colorectal Cancer with BRAF or KRAS Mutations.
Yao YM, Donoho GP, Iversen PW, Zhang Y, Van Horn RD, Forest A, Novosiadly RD, Webster YW, Ebert P, Bray S, Ting JC, Aggarwal A, Henry JR, Tiu RV, Plowman GD, Peng SB. Yao YM, et al. Among authors: zhang y. Clin Cancer Res. 2017 Sep 15;23(18):5547-5560. doi: 10.1158/1078-0432.CCR-16-3250. Epub 2017 Jun 13. Clin Cancer Res. 2017. PMID: 28611205
Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.
Henry JR, Kaufman MD, Peng SB, Ahn YM, Caldwell TM, Vogeti L, Telikepalli H, Lu WP, Hood MM, Rutkoski TJ, Smith BD, Vogeti S, Miller D, Wise SC, Chun L, Zhang X, Zhang Y, Kays L, Hipskind PA, Wrobleski AD, Lobb KL, Clay JM, Cohen JD, Walgren JL, McCann D, Patel P, Clawson DK, Guo S, Manglicmot D, Groshong C, Logan C, Starling JJ, Flynn DL. Henry JR, et al. Among authors: zhang x, zhang y. J Med Chem. 2015 May 28;58(10):4165-79. doi: 10.1021/acs.jmedchem.5b00067. Epub 2015 May 12. J Med Chem. 2015. PMID: 25965804
Identification of druggable cancer driver genes amplified across TCGA datasets.
Chen Y, McGee J, Chen X, Doman TN, Gong X, Zhang Y, Hamm N, Ma X, Higgs RE, Bhagwat SV, Buchanan S, Peng SB, Staschke KA, Yadav V, Yue Y, Kouros-Mehr H. Chen Y, et al. Among authors: zhang y. PLoS One. 2014 May 29;9(5):e98293. doi: 10.1371/journal.pone.0098293. eCollection 2014. PLoS One. 2014. PMID: 24874471 Free PMC article.
Evacetrapib is a novel, potent, and selective inhibitor of cholesteryl ester transfer protein that elevates HDL cholesterol without inducing aldosterone or increasing blood pressure.
Cao G, Beyer TP, Zhang Y, Schmidt RJ, Chen YQ, Cockerham SL, Zimmerman KM, Karathanasis SK, Cannady EA, Fields T, Mantlo NB. Cao G, et al. Among authors: zhang y. J Lipid Res. 2011 Dec;52(12):2169-2176. doi: 10.1194/jlr.M018069. Epub 2011 Sep 25. J Lipid Res. 2011. PMID: 21957197 Free PMC article.
Coadministration of a liver X receptor agonist and a peroxisome proliferator activator receptor-alpha agonist in Mice: effects of nuclear receptor interplay on high-density lipoprotein and triglyceride metabolism in vivo.
Beyer TP, Schmidt RJ, Foxworthy P, Zhang Y, Dai J, Bensch WR, Kauffman RF, Gao H, Ryan TP, Jiang XC, Karathanasis SK, Eacho PI, Cao G. Beyer TP, et al. Among authors: zhang y. J Pharmacol Exp Ther. 2004 Jun;309(3):861-8. doi: 10.1124/jpet.103.064535. Epub 2004 Feb 11. J Pharmacol Exp Ther. 2004. PMID: 14960661
A natural product ligand of the oxysterol receptor, liver X receptor.
Bramlett KS, Houck KA, Borchert KM, Dowless MS, Kulanthaivel P, Zhang Y, Beyer TP, Schmidt R, Thomas JS, Michael LF, Barr R, Montrose C, Eacho PI, Cao G, Burris TP. Bramlett KS, et al. Among authors: zhang y. J Pharmacol Exp Ther. 2003 Oct;307(1):291-6. doi: 10.1124/jpet.103.052852. Epub 2003 Jul 31. J Pharmacol Exp Ther. 2003. PMID: 12893846
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