CALCINEURIN HAS A VERY TIGHT-BINDING POCKET FOR THE SIDE-CHAIN OF RESIDUE-4 OF CYCLOSPORINE

被引：39

作者：

PAPAGEORGIOU, C

BORER, X

FRENCH, RR

机构：

[1] Sandoz Pharma Ltd., Preclinical Research

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(01)80127-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Derivatives of cyclosporin A (CsA) at position 4 were synthesised to probe the interaction of the CsA/CypA complex with calcineurin (CaN). Both lipophilic and hydrophilic substituents are detrimental for the immunosuppressive activity, indicating that CaN has a very ''tight-binding pocket'' for this region.

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页码：267 / 272

页数：6

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