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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
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
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.
Design, synthesis and structure-activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors.
Fernandez MC, Escribano A, Mateo AI, Parthasarathy S, Martin de la Nava EM, Wang X, Cockerham SL, Beyer TP, Schmidt RJ, Cao G, Zhang Y, Jones TM, Borel A, Sweetana SA, Cannady EA, Stephenson G, Frank S, Mantlo NB. Fernandez MC, et al. Among authors: zhang y. Bioorg Med Chem Lett. 2012 May 1;22(9):3056-62. doi: 10.1016/j.bmcl.2012.03.075. Epub 2012 Mar 28. Bioorg Med Chem Lett. 2012. PMID: 22497761
Design and synthesis of new tetrahydroquinolines derivatives as CETP inhibitors.
Escribano A, Mateo AI, Martin de la Nava EM, Mayhugh DR, Cockerham SL, Beyer TP, Schmidt RJ, Cao G, Zhang Y, Jones TM, Borel AG, Sweetana SA, Cannady EA, Mantlo NB. Escribano A, et al. Among authors: zhang y. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3671-5. doi: 10.1016/j.bmcl.2012.04.042. Epub 2012 Apr 13. Bioorg Med Chem Lett. 2012. PMID: 22543028
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