Novel aminopeptidase N inhibitors derived from antineoplaston AS2-5 (Part I).
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.
Li
Xun
X
School of Pharmaceutical Sciences, Shandong University, No. 44 WenhuaXi Road, Ji'nan, 250012, Shandong Province, PR China.
Wang
Junli
J
Li
Jinpei
J
Wu
Jifeng
J
Li
Yonggang
Y
Zhu
Huawei
H
Fan
Ruifang
R
Xu
Wenfang
W