Discovery of Selective Irreversible Inhibitors for Bruton's Tyrosine Kinase

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...

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Veröffentlicht in:	ChemMedChem 2007-01, Vol.2 (1), p.58-61
Hauptverfasser:	Pan, Zhengying, Scheerens, Heleen, Li, Shyr-Jiann, 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.
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine Triphosphate - metabolism Amino Acid Sequence Animals Antirheumatic Agents - chemistry Antirheumatic Agents - pharmacology Antirheumatic Agents - therapeutic use Arthritis, Rheumatoid - drug therapy Arthritis, Rheumatoid - enzymology Binding Sites biological activity Disease Models, Animal Drug Design enzymes medicinal chemistry Molecular Sequence Data Oligopeptides - chemistry Oligopeptides - metabolism Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Protein Kinase Inhibitors - therapeutic use Protein-Tyrosine Kinases - antagonists & inhibitors Protein-Tyrosine Kinases - metabolism Rodentia structural bioinformatics Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	1860-7179 1860-7187
DOI:	10.1002/cmdc.200600221