The next generation of PDE4 inhibitors

被引：107

作者：

Huang, Z ^{[1
]}

Ducharme, Y ^{[1
]}

Macdonald, D ^{[1
]}

Robichaud, A ^{[1
]}

机构：

[1] Merck Frosst Ctr Therapeut Res, Pointe Claire, PQ H9R 4P8, Canada

来源：

CURRENT OPINION IN CHEMICAL BIOLOGY | 2001年 / 5卷 / 04期

关键词：

D O I：

10.1016/S1367-5931(00)00224-6

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A number of highly potent PDE4 inhibitors are being developed for the treatment of asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, multiple sclerosis and Crohn's disease. Cilomilast (Ariflo(TM), SB 207499, SmithKline Beecham), the most advanced member of the class in Phase III clinical trials, was reported to have a limited therapeutic window. Other inhibitors with improved profiles in preclinical models are entering into (or are in) clinical trials. The recent developments in understanding PDE4 catalysis, inhibitor binding and their emetic response should facilitate the design of the next generation of PDE4 inhibitors.

引用

页码：432 / 438

页数：7

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