Discovery of highly potent, selective, covalent inhibitors of JAK3

Journal Article · Sun Oct 01 04:00:00 EDT 2017 · Bioorganic and Medicinal Chemistry Letters

DOI:https://doi.org/10.1016/j.bmcl.2017.09.023· OSTI ID:1397307

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.

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.

• Research Organization: Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)
• Sponsoring Organization: INDUSTRY
• OSTI ID: 1397307
• Journal Information: Bioorganic and Medicinal Chemistry Letters, Journal Name: Bioorganic and Medicinal Chemistry Letters Journal Issue: 20 Vol. 27; ISSN 0960-894X
• Publisher: Elsevier
• Country of Publication: United States
• Language: ENGLISH

Related Subjects

37 INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY
60 APPLIED LIFE SCIENCES