THE CONTRIBUTION TO BINDING OF THE PYRANOSIDE SUBSTITUENTS IN THE EXCISED BINDING DOMAIN OF FK-506

被引：7
|
作者：
STOCKS, MJ
BIRKINSHAW, TN
TEAGUE, SJ
机构：
[1] Fisons Pharmaceuticals PLC, Loughborough, LE11 ORH, Bakewell Road
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 12期
关键词：
D O I：
10.1016/S0960-894X(01)80513-8
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The contributions of the C-ll methyl and C-13 / C-15 methoxy substituents to the affinity of FK-506 for the immunophilin FKBP-12 were investigated. Subtraction of the C-11 methyl group led to a 400-fold drop in affinity. Removal of the C-13 and C-15 methoxy substituents led to a much smaller drop in affinity.
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页码：1457 / 1460
页数：4
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