Literature DB >> 28927786

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

James Kempson1, Damaso Ovalle2, Junqing Guo2, Stephen T Wrobleski2, Shuqun Lin2, Steven H Spergel2, James J-W Duan2, Bin Jiang2, Zhonghui Lu2, Jagabandhu Das2, Bingwei V Yang2, John Hynes2, Hong Wu2, John Tokarski2, John S Sack2, Javed Khan2, Gary Schieven2, Yuval Blatt2, Charu Chaudhry2, Luisa M Salter-Cid2, Aberra Fura2, Joel C Barrish2, Percy H Carter2, William J Pitts2.   

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.
Copyright © 2017 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Covalent; Irreversible inhibitor; JAK3

Mesh：

Substances：

Year:  2017        PMID： 28927786     DOI： 10.1016/j.bmcl.2017.09.023

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

1.  Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.

Authors:  Steven H Spergel; Michael E Mertzman; James Kempson; Junqing Guo; Sylwia Stachura; Lauren Haque; Jonathan S Lippy; Rosemary F Zhang; Michael Galella; Sidney Pitt; Guoxiang Shen; Aberra Fura; Kathleen Gillooly; Kim W McIntyre; Vicky Tang; John Tokarski; John S Sack; Javed Khan; Percy H Carter; Joel C Barrish; Steven G Nadler; Luisa M Salter-Cid; Gary L Schieven; Stephen T Wrobleski; William J Pitts
Journal:  ACS Med Chem Lett       Date:  2019-02-13       Impact factor: 4.345

2.  In Ovo Injection of CHIR-99021 Promotes Feather Follicle Development via Modulating the Wnt Signaling Pathway and Transcriptome in Goose Embryos (Anser cygnoides).

Authors:  Ziqiang Feng; Haizhou Gong; Jinhong Fu; Xiaohui Xu; Yupu Song; Xiaomin Yan; Ichraf Mabrouk; Yuxuan Zhou; Yudong Wang; Xianou Fu; Yujian Sui; Tuoya Liu; Chuanghang Li; Zebei Liu; Xu Tian; Le Sun; Keying Guo; Yongfeng Sun; Jingtao Hu
Journal:  Front Physiol       Date:  2022-05-20       Impact factor: 4.755

3.  Design of Rational JAK3 Inhibitors Based on the Parent Core Structure of 1,7-Dihydro-Dipyrrolo [2,3-b:3',2'-e] Pyridine.

Authors:  Yihao Li; Dan Meng; Jiali Xie; Ruoyu Li; Zifan Wang; Jinlong Li; Lin Mou; Xinhao Deng; Ping Deng
Journal:  Int J Mol Sci       Date:  2022-05-13       Impact factor: 6.208

Review 4.  Essential Kinases and Transcriptional Regulators and Their Roles in Autoimmunity.

Authors:  Ya Nan Deng; Joseph A Bellanti; Song Guo Zheng
Journal:  Biomolecules       Date:  2019-04-10

Review 5.  Covalent inhibitors: a rational approach to drug discovery.

Authors:  Fandi Sutanto; Markella Konstantinidou; Alexander Dömling
Journal:  RSC Med Chem       Date:  2020-07-02

Review 6.  Advances in covalent drug discovery.

Authors:  Lydia Boike; Nathaniel J Henning; Daniel K Nomura
Journal:  Nat Rev Drug Discov       Date:  2022-08-25       Impact factor: 112.288
  6 in total

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