SYNTHESIS AND EVALUATION OF DUAL DOMAIN MACROCYCLIC FKBP12 LIGANDS

被引：7

作者：

CAFFREY, MV

CLADINGBOEL, DE

COOPER, ME

DONALD, DK

FURBER, M

HARDERN, DN

HARRISON, RP

STOCKS, MJ

TEAGUE, SJ

机构：

[1] Fisons plc, Pharmaceuticals Division, Loughborough, LE11 ORH, Bakewell Road

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 21期

关键词：

D O I：

10.1016/S0960-894X(01)80273-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A number of dual domain, macrocyclic FKBP12 ligands were synthesised in which the FK506 effector domain was fused to simplified FKBP12 binding domains. The resulting macrocyclic compounds possessed moderate binding affinities for FKBP12 but showed no activity in an assay for FKBPl2 dependent calcineurin inhibition.

引用

收藏

页码：2507 / 2510

页数：4

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