4.6 Review

Aminopeptidase N (APN/CD13) as a Target for Anti-Cancer Agent Design

Journal

CURRENT MEDICINAL CHEMISTRY
Volume 15, Issue 27, Pages 2850-2865

Publisher

BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/092986708786242840

Keywords

Aminopeptidase N; APN/CD13; structure; inhibitors; anti-cancer agent; rational drug design; structure activity relationship

Funding

  1. national high technology research and development program of china [2007AA02Z314]

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APN is an important zinc dependent metallo-exopeptidase; it has been considered as a suitable target for anticancer drug design. In this review we focus on the most effective and the most promising inhibitors of aminopeptidase N. Their binding modes to the enzyme, the attempt to explain the origin of the inhibitory activity, as well as the structure activity relationship for some of these compounds are discussed. Besides, the structural and electronic requirements of the enzyme active site and the binding pockets, together with the specificity towards the ligands are presented.

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