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Discovery of highly potent, selective, covalent inhibitors of JAK3
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2017-09-11 , DOI: 10.1016/j.bmcl.2017.09.023
James Kempson , Damaso Ovalle , Junqing Guo , Stephen T. Wrobleski , Shuqun Lin , Steven H. Spergel , James J.-W. Duan , Bin Jiang , Zhonghui Lu , Jagabandhu Das , Bingwei V. Yang , John Hynes , Hong Wu , John Tokarski , John S. Sack , Javed Khan , Gary Schieven , Yuval Blatt , Charu Chaudhry , Luisa M. Salter-Cid , Aberra Fura , Joel C. Barrish , Percy H. Carter , William J. Pitts

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.



中文翻译:

发现高效,选择性,共价的JAK3抑制剂

已经鉴定了一组有用且新颖的工具分子,其与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几种亲电子弹头的比较研究。

更新日期:2017-09-11
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