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

Nicola Micale, Rajendran Vairagoundar, Alexander G. Yakovlev, Alan P. Kozikowski

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish (US)
Pages (from-to)6455-6458
Number of pages4
JournalJournal of medicinal chemistry
Volume47
Issue number26
DOIs
StatePublished - Dec 16 2004

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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