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

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 16, 12 Issues, 2016


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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



Anti-Cancer Agents in Medicinal Chemistry, 5(3): 281-301.

Author(s): Wenfang Xu and Qianbin Li.

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

Abstract

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

Volume: 5
Issue Number: 3
First Page: 281
Last Page: 301
Page Count: 21
DOI: 10.2174/1568011053765949
Price: $58
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