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Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors.
Ashwell MA, Lapierre JM, Brassard C, Bresciano K, Bull C, Cornell-Kennon S, Eathiraj S, France DS, Hall T, Hill J, Kelleher E, Khanapurkar S, Kizer D, Koerner S, Link J, Liu Y, Makhija S, Moussa M, Namdev N, Nguyen K, Nicewonger R, Palma R, Szwaya J, Tandon M, Uppalapati U, Vensel D, Volak LP, Volckova E, Westlund N, Wu H, Yang RY, Chan TC. Ashwell MA, et al. Among authors: france ds. J Med Chem. 2012 Jun 14;55(11):5291-310. doi: 10.1021/jm300276x. Epub 2012 May 31. J Med Chem. 2012. PMID: 22533986
Discovery of a novel mode of protein kinase inhibition characterized by the mechanism of inhibition of human mesenchymal-epithelial transition factor (c-Met) protein autophosphorylation by ARQ 197.
Eathiraj S, Palma R, Volckova E, Hirschi M, France DS, Ashwell MA, Chan TC. Eathiraj S, et al. Among authors: france ds. J Biol Chem. 2011 Jun 10;286(23):20666-76. doi: 10.1074/jbc.M110.213801. Epub 2011 Mar 24. J Biol Chem. 2011. PMID: 21454604 Free PMC article.
A novel mode of protein kinase inhibition exploiting hydrophobic motifs of autoinhibited kinases: discovery of ATP-independent inhibitors of fibroblast growth factor receptor.
Eathiraj S, Palma R, Hirschi M, Volckova E, Nakuci E, Castro J, Chen CR, Chan TC, France DS, Ashwell MA. Eathiraj S, et al. Among authors: france ds. J Biol Chem. 2011 Jun 10;286(23):20677-87. doi: 10.1074/jbc.M110.213736. Epub 2011 Mar 24. J Biol Chem. 2011. PMID: 21454610 Free PMC article.
N-hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activity: discovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824).
Remiszewski SW, Sambucetti LC, Bair KW, Bontempo J, Cesarz D, Chandramouli N, Chen R, Cheung M, Cornell-Kennon S, Dean K, Diamantidis G, France D, Green MA, Howell KL, Kashi R, Kwon P, Lassota P, Martin MS, Mou Y, Perez LB, Sharma S, Smith T, Sorensen E, Taplin F, Trogani N, Versace R, Walker H, Weltchek-Engler S, Wood A, Wu A, Atadja P. Remiszewski SW, et al. J Med Chem. 2003 Oct 9;46(21):4609-24. doi: 10.1021/jm030235w. J Med Chem. 2003. PMID: 14521422
Oncology drug discovery applications using the FMAT 8100 HTS system.
Lee JY, Miraglia S, Yan X, Swartzman E, Cornell-Kennon S, Mellentin-Michelotti J, Bruseo C, France DS. Lee JY, et al. Among authors: france ds. J Biomol Screen. 2003 Feb;8(1):81-8. doi: 10.1177/1087057102239668. J Biomol Screen. 2003. PMID: 12855001
35 results