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

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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.

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

Document Type: Research Article


Affiliations: Department of Medicinal Chemistry, School of Pharmaceutical Sciences, ShanDong University, 44, West Wenhua Road, 250012, Ji' nan, ShanDong, P.R. China.

Publication date: 2008-11-01

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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