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Discovery of Selective Irreversible Inhibitors for Bruton’s Tyrosine Kinase
Author(s) -
Pan Zhengying,
Scheerens Heleen,
Li ShyrJiann,
Schultz Brian E.,
Sprengeler Paul A.,
Burrill L. Chuck,
Mendonca Rohan V.,
Sweeney Michael D.,
Scott Keana C. K.,
Grothaus Paul G.,
Jeffery Douglas A.,
Spoerke Jill M.,
Honigberg Lee A.,
Young Peter R.,
Dalrymple Stacie A.,
Palmer James T.
Publication year - 2007
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200600221
Subject(s) - bruton's tyrosine kinase , rheumatoid arthritis , tyrosine kinase , in vitro , tyrosine , in vivo , dosing , computational biology , chemistry , medicine , biochemistry , pharmacology , immunology , biology , signal transduction , microbiology and biotechnology
A series of highly selective irreversible inhibitors for Bruton's tyrosine kinase (Btk) was developed using a structural bioinformatics approach. Their capabilities to modulate Btk's activity were characterized both in vitro and in vivo. Oral treatment with once‐a‐day dosing of compound 4 greatly inhibited disease development in a rodent rheumatoid arthritis (RA) model.