Document Report Card

ID: ALA1149270

Journal: J Med Chem

Title: Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3.

Authors: Micale N, Vairagoundar R, Yakovlev AG, Kozikowski AP.

Abstract: 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.

CiteXplore: 15588079

DOI: 10.1021/jm049248f