Progress in the Development of Aminopeptidase N (APN/CD13) Inhibitors

Author(s): Wenfang Xu, Qianbin Li

Journal Name: Current Medicinal Chemistry - Anti-Cancer Agents
Continued as Anti-Cancer Agents in Medicinal Chemistry

Volume 5 , Issue 3 , 2005


Aminopeptidase N (APN; CD13) is a member of zinc-containing ectoenzymes family involved in the degradation of neutral or basic amino acids (Ala > Phe > Leu > Gly) from N-terminal of bioactive peptides and amide or arylamide derivatives of amino acids. The expression of APN being up regulated has been implicated in the pathogenesis of a variety of diseases such as cancer, leukemia, diabetic nephropathy, and rheumatoid arthritis. Thus, APN inhibitors (APNIs) are expected to be useful for the treatment of these disorders. This article reviews briefly the structure characteristic and possible function of APN. The proposed biomolecular structures and mechanism of action used in the design of APNIs are thoroughly covered. Major emphasis is on recently published potent, small molecular weight APNIs and their essential structure activity relationship (SAR). Finally, available clinical results of compounds in development are summarized in this review.

Keywords: aminopeptidase n, inhibitors, mechanisms

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Article Details

Year: 2005
Page: [281 - 301]
Pages: 21
DOI: 10.2174/1568011053765949
Price: $58

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