用于治疗类风湿性关节炎的CCR1拮抗剂BMS-817399的发现。
Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis.
作者信息
Santella Joseph B, Gardner Daniel S, Duncia John V, Wu Hong, Dhar Murali, Cavallaro Cullen, Tebben Andrew J, Carter Percy H, Barrish Joel C, Yarde Melissa, Briceno Stephanie W, Cvijic Mary Ellen, Grafstrom R Robert, Liu Richard, Patel Sima R, Watson Andrew J, Yang Guchen, Rose Anne V, Vickery Rodney D, Caceres-Cortes Janet, Caporuscio Christian, Camac Daniel M, Khan Javed A, An Yongmi, Foster William R, Davies Paul, Hynes John
机构信息
Bristol Myers Squibb Company , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States.
出版信息
J Med Chem. 2014 Sep 25;57(18):7550-64. doi: 10.1021/jm5003167. Epub 2014 Sep 3.
High-affinity, functionally potent, urea-based antagonists of CCR1 have been discovered. Modulation of PXR transactivation has revealed the selective and orally bioavailable CCR1 antagonist BMS-817399 (29), which entered clinical trials for the treatment of rheumatoid arthritis.
已发现对CCR1具有高亲和力、功能强效的基于尿素的拮抗剂。对孕烷X受体（PXR）反式激活的调节揭示了选择性且口服生物可利用的CCR1拮抗剂BMS-817399（29），该拮抗剂已进入治疗类风湿性关节炎的临床试验阶段。
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