Novel aminopeptidase N inhibitors derived from antineoplaston AS2-5 - GreenMedInfo Summary
Novel aminopeptidase N inhibitors derived from antineoplaston AS2-5 (Part I).
Bioorg Med Chem. 2009 Apr 15 ;17(8):3053-60. Epub 2009 Mar 6. PMID: 19329328
School of Pharmaceutical Sciences, Shandong University, No. 44 WenhuaXi Road, Ji'nan, 250012, Shandong Province, PR China.
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.