Abstract
A novel class of small molecule human granzyme B inhibitors is reported. Compound 20 has a K(i) of 7 nM against human granzyme B and blocks CTL mediated apoptosis with an IC(50) of 3 micromolar.
MeSH terms
-
Apoptosis / drug effects*
-
Cytotoxicity, Immunologic / drug effects
-
Drug Design
-
Granzymes
-
Humans
-
Inhibitory Concentration 50
-
Molecular Structure
-
Serine Endopeptidases / metabolism*
-
Serine Proteinase Inhibitors / chemistry*
-
Serine Proteinase Inhibitors / pharmacology*
-
Structure-Activity Relationship
-
Substrate Specificity
-
T-Lymphocytes, Cytotoxic / drug effects*
-
T-Lymphocytes, Cytotoxic / immunology*
Substances
-
Serine Proteinase Inhibitors
-
GZMB protein, human
-
Granzymes
-
Serine Endopeptidases