Dithiocarbamates: a new class of carbonic anhydrase inhibitors. Crystallographic and kinetic investigations

被引：150

作者：

Carta, Fabrizio ^{[2
]}

Aggarwal, Mayank ^{[1
]}

Maresca, Alfonso ^{[2
]}

Scozzafava, Andrea ^{[2
]}

McKenna, Robert ^{[1
]}

Supuran, Claudiu T. ^{[2
]}

机构：

[1] Univ Florida, Coll Med, Dept Biochem & Mol Biol, Gainesville, FL 32610 USA

[2] Univ Florence, Lab Chim Bioinorgan, I-50019 Florence, Italy

来源：

CHEMICAL COMMUNICATIONS | 2012年 / 48卷 / 13期

关键词：

CRYSTAL-STRUCTURE; ISOFORMS IX; COUMARINS; TRANSMEMBRANE; DIOXIDE; HYPOXIA; XIII; SITE;

D O I：

10.1039/c2cc16395k

中图分类号：

O6 [化学];

学科分类号：

070301 [无机化学];

摘要：

The zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1) is inhibited by several classes of zinc-binders (sulfonamides, sulfamates, and sulfamides) as well as by compounds which do not interact with the metal ion (phenols, polyamines and coumarins). Here we report a new class of potent CA inhibitors which bind the zinc ion: the dithiocarbamates (DTCs). They coordinate to the zinc ion from the enzyme active site in monodentate manner and establish many favorable interactions with amino acid residues nearby. Several low nanomolar CA I, II and IX inhibitors were detected.

引用

页码：1868 / 1870

页数：3

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