Development of inositol-based antagonists for the D-myo-inositol 1,4,5-trisphosphate receptor

被引：15

作者：

Keddie, Neil S. ^{[2
,3
]}

Ye, Yulin ^{[1
]}

Aslam, Tashfeen ^{[2
,3
]}

Luyten, Tomas ^{[4
]}

Bello, Davide ^{[2
,3
]}

Garnham, Clive ^{[5
]}

Bultynck, Geert ^{[4
]}

Galione, Antony ^{[5
]}

Conway, Stuart J. ^{[1
]}

机构：

[1] Univ Oxford, Dept Chem, Chem Res Lab, Oxford OX1 3TA, England

[2] Univ St Andrews, Sch Chem, St Andrews KY16 9ST, Fife, Scotland

[3] Univ St Andrews, Ctr Biomol Sci, St Andrews KY16 9ST, Fife, Scotland

[4] Katholieke Univ Leuven, Mol Signalling Lab, B-3000 Louvain, Belgium

[5] Univ Oxford, Dept Pharmacol, Oxford OX1 3QT, England

来源：

CHEMICAL COMMUNICATIONS | 2011年 / 47卷 / 01期

基金：

英国生物技术与生命科学研究理事会;

关键词：

2-AMINOETHOXYDIPHENYL BORATE 2-APB; CALCIUM-RELEASE; MYOINOSITOL 1,4,5-TRISPHOSPHATE; 5-PHOSPHONATE ANALOGS; PARTIAL AGONISTS; CA2+ RELEASE; DERIVATIVES; PATHWAY; BINDING; NAADP;

D O I：

10.1039/c0cc03003a

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The syntheses of four D-myo-inositol 1,4,5-trisphosphate (InsP(3)) derivatives, incorporating phosphate bioisosteres at the 5-position, are reported. The methyl phosphate ester and sulfate derivatives retain InsP(3) receptor (InsP(3)R) agonist activity; the compounds that possess a methylphosphonate or a carboxymethyl moiety are InsP(3)R antagonists.

引用

页码：242 / 244

页数：3

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