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Identification of a novel series of BET family bromodomain inhibitors: Binding mode and profile of I-BET151 (GSK1210151A)

作者	Seal, J; Lamotte, Y; Donche, F; Bouillot, A; Mirguet, O; Gellibert, F; Nicodeme, E; Krysa, G; Kirilovsky, J; Beinke, S; McCleary, S; Rioja, I; Bamborough, P; Chung, CW; Gordon, L; Lewis, T; Walker, AL; Cutler, L; Lugo, D; Wilson, DM; Witherington, J; Lee, K; Prinjha, RK

选自	期刊 Bioorganic & Medicinal Chemistry Letters; 卷期 2012年22-8; 页码 2968-2972

关联知识点

[摘要]：A novel series of quinoline isoxazole BET family bromodomain inhibitors are discussed. Crystallography is used to illustrate binding modes and rationalize their SAR. One member, I-BET151 (GSK1210151A), shows good oral bioavailability in both the rat and minipig as well as demonstrating efficient suppression of bacterial induced inflammation and sepsis in a murine in vivo endotoxaemia model. (C) 2012 Elsevier Ltd. All rights reserved.
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