Abstract Title:

Novel aminopeptidase N inhibitors derived from antineoplaston AS2-5 (Part I).

Abstract Source:

Bioorg Med Chem. 2009 Apr 15 ;17(8):3053-60. Epub 2009 Mar 6. PMID: 19329328

Abstract Author(s):

Xun Li, Junli Wang, Jinpei Li, Jifeng Wu, Yonggang Li, Huawei Zhu, Ruifang Fan, Wenfang Xu

Article Affiliation:

School of Pharmaceutical Sciences, Shandong University, No. 44 WenhuaXi Road, Ji'nan, 250012, Shandong Province, PR China.

Abstract:

Overexpression of zinc-dependent metalloproteinase, aminopeptidase N (APN/CD13), is considered to be involved in the process of tumor invasion and metastasis. Herein we describe the synthesis and in vitro enzymatic inhibition assay of antineoplaston AS2-5 scaffold peptidomimetic compounds. The results demonstrated that most of these L-iso-glutamine derivatives displayed selective inhibitory activity against APN as compared with MMP-2, with IC(50) values in the micromole range. The structure-activity relationships were also briefly discussed.

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