821800-04-8Relevant articles and documents
Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3
Micale, Nicola,Vairagoundar, Rajendran,Yakovlev, Alexander G.,Kozikowski, Alan P.
, p. 6455 - 6458 (2004)
In this paper we report the synthesis and characterization of a novel potent and selective inhibitor of caspase-3, a member of the caspase family of cysteine proteases which plays an important role in many human disorders. This molecule represents 3(S)-acetylamino-N-{1-[(((3S)-2-hydroxy-5-oxo- tetrahydrofuran-3-yl)carbamoyl)methyl]-2-oxo-5-phenyl-2,3-dihydro-1H/-benzo[e] [1,4]diazepin-3-yl}succinamic acid, a monocyclic conformationally constrained form of the tetrapeptide Ac-DEVD-H, in which a 1,4-benzodiazepine nucleus is introduced internally to the peptidic sequence.