Li Xun, Wang Junli, Li Jinpei, Wu Jifeng, Li Yonggang, Zhu Huawei, Fan Ruifang, Xu Wenfang
School of Pharmaceutical Sciences, Shandong University, No. 44 WenhuaXi Road, Ji'nan, 250012, Shandong Province, PR China.
Bioorg Med Chem. 2009 Apr 15;17(8):3053-60. doi: 10.1016/j.bmc.2009.02.063. Epub 2009 Mar 6.
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.
锌依赖性金属蛋白酶氨肽酶N（APN/CD13）的过表达被认为参与肿瘤侵袭和转移过程。在此，我们描述了抗肿瘤素AS2-5支架拟肽化合物的合成及体外酶抑制试验。结果表明，与基质金属蛋白酶-2（MMP-2）相比，这些L-异谷氨酰胺衍生物中的大多数对APN表现出选择性抑制活性，半数抑制浓度（IC50）值在微摩尔范围内。还简要讨论了构效关系。
