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发现JAK3的高效、选择性共价抑制剂。

Discovery of highly potent, selective, covalent inhibitors of JAK3.

作者信息

Kempson James, Ovalle Damaso, Guo Junqing, Wrobleski Stephen T, Lin Shuqun, Spergel Steven H, Duan James J-W, Jiang Bin, Lu Zhonghui, Das Jagabandhu, Yang Bingwei V, Hynes John, Wu Hong, Tokarski John, Sack John S, Khan Javed, Schieven Gary, Blatt Yuval, Chaudhry Charu, Salter-Cid Luisa M, Fura Aberra, Barrish Joel C, Carter Percy H, Pitts William J

机构信息

Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.

Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.

出版信息

Bioorg Med Chem Lett. 2017 Oct 15;27(20):4622-4625. doi: 10.1016/j.bmcl.2017.09.023. Epub 2017 Sep 11.

DOI:10.1016/j.bmcl.2017.09.023
PMID:28927786
Abstract

A useful and novel set of tool molecules have been identified which bind irreversibly to the JAK3 active site cysteine residue. The design was based on crystal structure information and a comparative study of several electrophilic warheads.

摘要

已经鉴定出一组有用且新颖的工具分子,它们与JAK3活性位点的半胱氨酸残基不可逆地结合。该设计基于晶体结构信息和对几种亲电弹头的比较研究。

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