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.
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.
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。
Zotero 插件