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106 results

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Page 1
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: henry jr. 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
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: henry jr. 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.
Aurora A Kinase Inhibition Is Synthetic Lethal with Loss of the RB1 Tumor Suppressor Gene.
Gong X, Du J, Parsons SH, Merzoug FF, Webster Y, Iversen PW, Chio LC, Van Horn RD, Lin X, Blosser W, Han B, Jin S, Yao S, Bian H, Ficklin C, Fan L, Kapoor A, Antonysamy S, Mc Nulty AM, Froning K, Manglicmot D, Pustilnik A, Weichert K, Wasserman SR, Dowless M, Marugán C, Baquero C, Lallena MJ, Eastman SW, Hui YH, Dieter MZ, Doman T, Chu S, Qian HR, Ye XS, Barda DA, Plowman GD, Reinhard C, Campbell RM, Henry JR, Buchanan SG. Gong X, et al. Among authors: henry jr. Cancer Discov. 2019 Feb;9(2):248-263. doi: 10.1158/2159-8290.CD-18-0469. Epub 2018 Oct 29. Cancer Discov. 2019. PMID: 30373917
Aurora A-Selective Inhibitor LY3295668 Leads to Dominant Mitotic Arrest, Apoptosis in Cancer Cells, and Shows Potent Preclinical Antitumor Efficacy.
Du J, Yan L, Torres R, Gong X, Bian H, Marugán C, Boehnke K, Baquero C, Hui YH, Chapman SC, Yang Y, Zeng Y, Bogner SM, Foreman RT, Capen A, Donoho GP, Van Horn RD, Barnard DS, Dempsey JA, Beckmann RP, Marshall MS, Chio LC, Qian Y, Webster YW, Aggarwal A, Chu S, Bhattachar S, Stancato LF, Dowless MS, Iversen PW, Manro JR, Walgren JL, Halstead BW, Dieter MZ, Martinez R, Bhagwat SV, Kreklau EL, Lallena MJ, Ye XS, Patel BKR, Reinhard C, Plowman GD, Barda DA, Henry JR, Buchanan SG, Campbell RM. Du J, et al. Among authors: henry jr. Mol Cancer Ther. 2019 Dec;18(12):2207-2219. doi: 10.1158/1535-7163.MCT-18-0529. Epub 2019 Sep 17. Mol Cancer Ther. 2019. PMID: 31530649
A Phase I Study of LY3009120, a Pan-RAF Inhibitor, in Patients with Advanced or Metastatic Cancer.
Sullivan RJ, Hollebecque A, Flaherty KT, Shapiro GI, Rodon Ahnert J, Millward MJ, Zhang W, Gao L, Sykes A, Willard MD, Yu D, Schade AE, Crowe K, Flynn DL, Kaufman MD, Henry JR, Peng SB, Benhadji KA, Conti I, Gordon MS, Tiu RV, Hong DS. Sullivan RJ, et al. Among authors: henry jr. Mol Cancer Ther. 2020 Feb;19(2):460-467. doi: 10.1158/1535-7163.MCT-19-0681. Epub 2019 Oct 23. Mol Cancer Ther. 2020. PMID: 31645440 Clinical Trial.
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. 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
Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.
Engler TA, Henry JR, Malhotra S, Cunningham B, Furness K, Brozinick J, Burkholder TP, Clay MP, Clayton J, Diefenbacher C, Hawkins E, Iversen PW, Li Y, Lindstrom TD, Marquart AL, McLean J, Mendel D, Misener E, Briere D, O'Toole JC, Porter WJ, Queener S, Reel JK, Owens RA, Brier RA, Eessalu TE, Wagner JR, Campbell RM, Vaughn R. Engler TA, et al. Among authors: henry jr. J Med Chem. 2004 Jul 29;47(16):3934-7. doi: 10.1021/jm049768a. J Med Chem. 2004. PMID: 15267232
106 results