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靶向基质金属蛋白酶:通过肿瘤相关半乳糖凝集素呈递的双功能抑制剂的设计。

Targeting matrix metalloproteinases: design of a bifunctional inhibitor for presentation by tumour-associated galectins.

机构信息

Department of Chemistry, University of Florence, Via della Lastruccia, 13 50019 Sesto F.no Firenze, Italy.

出版信息

Chemistry. 2013 Feb 4;19(6):1896-902. doi: 10.1002/chem.201203794. Epub 2012 Dec 27.

DOI:10.1002/chem.201203794
PMID:23280962
Abstract

A new strategy to exploit galectin presence to target matrix metalloproteinases (MMPs) is presented. A bifunctional conjugate with lactose and an inhibitor for MMPs is able to bind MMP and Gal-3 simultaneously. This compound might allow the lectin to attract the MMP inhibitor to the tumour site and to block protumoural activities of the lectin at the same time.

摘要

本文提出了一种利用半乳糖凝集素存在来靶向基质金属蛋白酶(MMPs)的新策略。一种具有乳糖和 MMP 抑制剂的双功能缀合物能够同时结合 MMP 和 Gal-3。这种化合物可能使凝集素能够将 MMP 抑制剂吸引到肿瘤部位,并同时阻断凝集素的促肿瘤活性。

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