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作为基质金属蛋白酶MMP - 2和MMP - 8抑制剂的拟肽次膦酸酯的设计、建模、合成及生物学评价

Design, modelling, synthesis and biological evaluation of peptidomimetic phosphinates as inhibitors of matrix metalloproteinases MMP-2 and MMP-8.

作者信息

Bianchini Gianluca, Aschi Massimiliano, Cavicchio Giancarlo, Crucianelli Marcello, Preziuso Serena, Gallina Carlo, Nastari Adele, Gavuzzo Enrico, Mazza Fernando

机构信息

Dipartimento di Chimica, Ingegneria Chimica e Materiali, Università dell'Aquila, via Vetoio, I-67010-Coppito, AQ, Italy.

出版信息

Bioorg Med Chem. 2005 Aug 1;13(15):4740-9. doi: 10.1016/j.bmc.2005.04.079.

DOI:10.1016/j.bmc.2005.04.079
PMID:15935680
Abstract

Three novel peptidomimetic phosphinate inhibitors have been synthesized and evaluated as inhibitors of matrix metalloproteinases MMP-2 and MMP-8. Their IC50 values are in the micromolar range, and one of them showed to be the most effective inhibitor of MMP-2. The differences in binding affinities for MMP-2 and MMP-8 of the three phosphinates have been rationalized by means of modelling studies and molecular dynamics simulations.

摘要

已经合成了三种新型拟肽次膦酸酯抑制剂，并对其作为基质金属蛋白酶MMP - 2和MMP - 8的抑制剂进行了评估。它们的IC50值在微摩尔范围内，其中一种显示是MMP - 2最有效的抑制剂。通过建模研究和分子动力学模拟，对这三种次膦酸酯与MMP - 2和MMP - 8结合亲和力的差异进行了合理解释。

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