A high-affinity carbohydrate-containing inhibitor of matrix metalloproteinases

被引:28
作者
Calderone, Vito
Fragai, Marco
Luchinat, Claudio
Nativi, Cristina
Richichi, Barbara
Roelens, Stefano
机构
[1] Magnetic Resonance Center, University of Florence, Sesto Fiorentino 50019
[2] Department of Organic Chemistry, University of Florence, Sesto Fiorentino 50019
[3] Department of Chemistry, University of Siena, Siena
[4] Department of Agricultural Biotechnology, University of Florence, Florence
[5] ProtEra S.r.l.
[6] CNR, Istituto di Chimica del Composti Organometallici, Florence
关键词
Albumin interaction; Glycosyl derivatives; Inhibitors; Lipophilicity; Metalloproteinases;
D O I
10.1002/cmdc.200600020
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Matrix metalloproteinases (MMPs) are a class of Zn-containing hydrolases that participate in a variety of biological processes, and aberrant activity of MMPs has been implicated in a number of diseases including cancer. A new glycoside-containing inhibitor of MMPs, unprecedented among the inhibitors of this family of enzymes, is reported. This inhibitor is water soluble, and displays nanomolar affinity toward several MMPs.
引用
收藏
页码:598 / +
页数:5
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