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Title: Discovery of highly potent, selective, covalent inhibitors of JAK3

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.

Authors:
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Publication Date:
Research Org.:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Org.:
INDUSTRY
OSTI Identifier:
1397307
Resource Type:
Journal Article
Resource Relation:
Journal Name: Bioorganic and Medicinal Chemistry Letters; Journal Volume: 27; Journal Issue: 20
Country of Publication:
United States
Language:
ENGLISH
Subject:
37 INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY; 60 APPLIED LIFE SCIENCES

Citation Formats

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., and Pitts, William J. Discovery of highly potent, selective, covalent inhibitors of JAK3. United States: N. p., 2017. Web. doi:10.1016/j.bmcl.2017.09.023.
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. Discovery of highly potent, selective, covalent inhibitors of JAK3. United States. doi:10.1016/j.bmcl.2017.09.023.
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., and Pitts, William J. Sun . "Discovery of highly potent, selective, covalent inhibitors of JAK3". United States. doi:10.1016/j.bmcl.2017.09.023.
@article{osti_1397307,
title = {Discovery of highly potent, selective, covalent inhibitors of JAK3},
author = {Kempson, James and Ovalle, Damaso and Guo, Junqing and Wrobleski, Stephen T. and Lin, Shuqun and Spergel, Steven H. and Duan, James J. -W. and Jiang, Bin and Lu, Zhonghui and Das, Jagabandhu and Yang, Bingwei V. and Hynes, John and Wu, Hong and Tokarski, John and Sack, John S. and Khan, Javed and Schieven, Gary and Blatt, Yuval and Chaudhry, Charu and Salter-Cid, Luisa M. and Fura, Aberra and Barrish, Joel C. and Carter, Percy H. and Pitts, William J.},
abstractNote = {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.},
doi = {10.1016/j.bmcl.2017.09.023},
journal = {Bioorganic and Medicinal Chemistry Letters},
number = 20,
volume = 27,
place = {United States},
year = {Sun Oct 01 00:00:00 EDT 2017},
month = {Sun Oct 01 00:00:00 EDT 2017}
}