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芳基双膦酸盐：肿瘤相关碳酸酐酶 XII 的有效且选择性抑制剂。

Arylamino bisphosphonates: potent and selective inhibitors of the tumor-associated carbonic anhydrase XII.

机构信息

Dipartimento di Farmacia-Scienze del Farmaco, Università degli Studi 'Aldo Moro' di Bari, Via Orabona 4, 70126 Bari, Italy.

Università degli Studi di Firenze, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy.

出版信息

Bioorg Med Chem Lett. 2014 Apr 15;24(8):1941-3. doi: 10.1016/j.bmcl.2014.03.001. Epub 2014 Mar 12.

DOI:10.1016/j.bmcl.2014.03.001
PMID:24650641
Abstract

A set of matrix metalloproteinases (MMPs) inhibitors, containing a bisphosphonate moiety (BP), has been evaluated for the inhibitory activity of carbonic anhydrases (CAs, EC 4.2.1.1). Human (h) isoforms hCA I, II, IX, XII and XIV were included in the study due to their involvement in crucial physiologic and pathologic processes. Some of these molecules selectively inhibited CA XII in the nanomolar range, showing an attractive dual mechanism (anti-MMP and anti-CA) of action as potential antitumor agents. The BP inhibitors investigated in this study are also excellent leads for obtaining even more effective compounds able to selectively target membrane-bound CA XII and having the potential to be used as tools for understanding physiologic processes regulated by this isoform.

摘要

一组基质金属蛋白酶 (MMPs) 抑制剂，含有双膦酸盐部分 (BP)，已针对碳酸酐酶 (CA，EC 4.2.1.1) 的抑制活性进行了评估。由于其参与了重要的生理和病理过程，因此包括人 (h) 同工型 hCA I、II、IX、XII 和 XIV。由于其在纳摩尔范围内选择性抑制 CA XII，这些分子中的一些表现出有吸引力的双重机制（抗 MMP 和抗 CA）作用，作为潜在的抗肿瘤药物。本研究中研究的 BP 抑制剂也是获得更有效化合物的良好先导，这些化合物能够选择性靶向膜结合 CA XII，并有可能用作研究该同工型调节的生理过程的工具。

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