X-ray crystallographic studies reveal that the incorporation of spacer groups in carbonic anhydrase inhibitors causes alternate binding modes

被引：18

作者：

Fisher, S. Zoe

Govindasamy, Lakshmanan

Boyle, Nicholas

Agbandje-McKenna, Mavis

Silverman, David N.

Blackburn, G. Michael

McKenna, Robert ^{[1
]}

机构：

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

[2] Univ Sheffield, Dept Chem, Sheffield S3 7HF, S Yorkshire, England

[3] Univ Florida, Coll Med, Dept Pharmacol & Therapeut, Gainesville, FL 32610 USA

来源：

ACTA CRYSTALLOGRAPHICA SECTION F-STRUCTURAL BIOLOGY COMMUNICATIONS | 2006年 / 62卷

关键词：

D O I：

10.1107/S1744309106020446

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Human carbonic anhydrases (CAs) are well studied targets for the development of inhibitors for pharmaceutical applications. The crystal structure of human CA II has been determined in complex with two CA inhibitors (CAIs) containing conventional sulfonamide and thiadiazole moieties separated by a -CF2- or --CHNH2- spacer group. The structures presented here reveal that these spacer groups allow novel binding modes for the thiadiazole moiety compared with conventional CAIs.

引用

页码：618 / 622

页数：5

共 25 条

[1] A new synthesis of difluoromethanesulfonamides - a novel pharmacophore for carbonic anhydrase inhibition [J].