Molecular Cloning, Characterization, and Inhibition Studies of a β-Carbonic Anhydrase from Malassezia globosa, a Potential Antidandruff Target

被引：47

作者：

Hewitson, Kirsty S. ^{[2
]}

Vullo, Daniela ^{[1
]}

Scozzafava, Andrea ^{[1
]}

Mastrolorenzo, Antonio ^{[3
]}

Supuran, Claudiu T. ^{[1
]}

机构：

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

[2] Union Life Sci Ltd, London EC3V 3ND, England

[3] Univ Florence, Ctr MST, I-50129 Florence, Italy

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 55卷 / 07期

关键词：

YEAST SACCHAROMYCES-CEREVISIAE; HELICOBACTER-PYLORI; CRYSTAL-STRUCTURE; CLASS ENZYME; X-RAY; MYCOBACTERIUM-TUBERCULOSIS; ANTITUMOR SULFONAMIDE; ISOZYME-II; DANDRUFF; PLANT;

D O I：

10.1021/jm300203r

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A beta-carbonic anhydrase (CA, EC 4.2.1.1) from the fungal pathogen Malassezia globosa has been cloned, characterized, and studied for its inhibition with sulfonamides. This enzyme, designated MG-CA, has significant catalytic activity in the CO2 hydration reaction and was inhibited by sulfonamides, sulfamates, and sulfamides with K-1 in the nanomolar to micromolar range. Several sulfonamides have also been investigated for the inhibition of growth of M. globosa, M. dermatis, M. pachydermatic, and M. furfur in cultures, whereas a mouse model of dandruff showed that treatment with sulfonamides led to fragmented fungal hyphae, as for the treatment with ketoconazole, a clinically used antifungal agent. These data prompt us to propose MG-CA as a new antidandruff drug target.

引用

页码：3513 / 3520

页数：8

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