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GDC-0449-a potent inhibitor of the hedgehog pathway.
Robarge KD, Brunton SA, Castanedo GM, Cui Y, Dina MS, Goldsmith R, Gould SE, Guichert O, Gunzner JL, Halladay J, Jia W, Khojasteh C, Koehler MF, Kotkow K, La H, Lalonde RL, Lau K, Lee L, Marshall D, Marsters JC Jr, Murray LJ, Qian C, Rubin LL, Salphati L, Stanley MS, Stibbard JH, Sutherlin DP, Ubhayaker S, Wang S, Wong S, Xie M. Robarge KD, et al. Among authors: wong s. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5576-81. doi: 10.1016/j.bmcl.2009.08.049. Epub 2009 Aug 15. Bioorg Med Chem Lett. 2009. PMID: 19716296
Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor.
Wong H, Chen JZ, Chou B, Halladay JS, Kenny JR, La H, Marsters JC Jr, Plise E, Rudewicz PJ, Robarge K, Shin Y, Wong S, Zhang C, Khojasteh SC. Wong H, et al. Among authors: wong s. Xenobiotica. 2009 Nov;39(11):850-61. doi: 10.3109/00498250903180289. Xenobiotica. 2009. PMID: 19845436
Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.
Sutherlin DP, Sampath D, Berry M, Castanedo G, Chang Z, Chuckowree I, Dotson J, Folkes A, Friedman L, Goldsmith R, Heffron T, Lee L, Lesnick J, Lewis C, Mathieu S, Nonomiya J, Olivero A, Pang J, Prior WW, Salphati L, Sideris S, Tian Q, Tsui V, Wan NC, Wang S, Wiesmann C, Wong S, Zhu BY. Sutherlin DP, et al. Among authors: wong s. J Med Chem. 2010 Feb 11;53(3):1086-97. doi: 10.1021/jm901284w. J Med Chem. 2010. PMID: 20050669
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.
Heffron TP, Berry M, Castanedo G, Chang C, Chuckowree I, Dotson J, Folkes A, Gunzner J, Lesnick JD, Lewis C, Mathieu S, Nonomiya J, Olivero A, Pang J, Peterson D, Salphati L, Sampath D, Sideris S, Sutherlin DP, Tsui V, Wan NC, Wang S, Wong S, Zhu BY. Heffron TP, et al. Among authors: wong s. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2408-11. doi: 10.1016/j.bmcl.2010.03.046. Epub 2010 Mar 12. Bioorg Med Chem Lett. 2010. PMID: 20346656
Second generation 2-pyridyl biphenyl amide inhibitors of the hedgehog pathway.
Castanedo GM, Wang S, Robarge KD, Blackwood E, Burdick D, Chang C, Dijkgraaf GJ, Gould S, Gunzner J, Guichert O, Halladay J, Khojasteh C, Lee L, Marsters JC Jr, Murray L, Peterson D, Plise E, Salphati L, de Sauvage FJ, Wong S, Sutherlin DP. Castanedo GM, et al. Among authors: wong s. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6748-53. doi: 10.1016/j.bmcl.2010.08.134. Epub 2010 Sep 15. Bioorg Med Chem Lett. 2010. PMID: 20875741
Significant species difference in amide hydrolysis of GDC-0834, a novel potent and selective Bruton's tyrosine kinase inhibitor.
Liu L, Halladay JS, Shin Y, Wong S, Coraggio M, La H, Baumgardner M, Le H, Gopaul S, Boggs J, Kuebler P, Davis JC Jr, Liao XC, Lubach JW, Deese A, Sowell CG, Currie KS, Young WB, Khojasteh SC, Hop CE, Wong H. Liu L, et al. Among authors: wong s, wong h. Drug Metab Dispos. 2011 Oct;39(10):1840-9. doi: 10.1124/dmd.111.040840. Epub 2011 Jul 8. Drug Metab Dispos. 2011. PMID: 21742900
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