4.6 Review

Progress in the Development of Bestatin Analogues as Aminopeptidases Inhibitors

Journal

CURRENT MEDICINAL CHEMISTRY
Volume 18, Issue 7, Pages 964-976

Publisher

BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/092986711794940879

Keywords

Aminopeptidases; analogues; bestatin; optimization

Funding

  1. National High Technology Research and Development Program of China [2007AA02Z314]
  2. National Nature Science Foundation of China [90713041, 30772654]

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Aminopeptidases play essential roles in protein maturation, activation, and stability as well as in the degradation and regulation of hormonal and nonhormonal peptides that can serve as important enzyme targets for drug design. This review will focus on an effective inhibitor of aminopeptidases, bestatin, including work to find better inhibitors in the past three decades that has sought to optimize bestatin and prospective developments in bestatin optimization in the future.

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