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