Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:3.4.21.4 (
trypsin
)
42,187
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
The serine protease
tryptase
has been associated with a broad range of allergic and inflammatory diseases and, in particular, has been implicated as a critical mediator of asthma. The inhibition of
tryptase
therefore has the potential to be a valuable therapy for asthma. The synthesis, employing solution phase parallel methods, and SAR of a series of novel
2-azepanone
tryptase
inhibitors are presented. A member of this series, 8t, was identified as a potent inhibitor of human
tryptase
(IC(50)=38 nM) with selectivity >/=330-fold versus related serine proteases (
trypsin
, plasmin, uPA, tPA, APC, alpha-thrombin, and FXa) [corrected].
...
PMID:Synthesis of potent and selective 2-azepanone inhibitors of human tryptase. 1469 47
