Discovery of potent, selective human granzyme B inhibitors that inhibit CTL mediated apoptosis

Christopher A. Willoughby,Herbert G. Bull,Margarita Garcia-Calvo,Joanne Jiang,Kevin T. Chapman,Nancy A. Thornberry

Discovery of potent, selective human granzyme B inhibitors that inhibit CTL mediated apoptosis

2002

Christopher A. Willoughby
Herbert G. Bull
Margarita Garcia-Calvo
Joanne Jiang
Kevin T. Chapman
Nancy A. Thornberry

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.

Keywords:

Enzyme
Granzyme B
Small molecule
CTL*
Organic chemistry
Cytotoxicity
Apoptosis
Programmed cell death
Chemistry
Enzyme inhibitor
Biochemistry
Biological activity
In vitro

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