'Click cyclic ADP-ribose': a neutral second messenger mimic

被引：26

作者：

Swarbrick, Joanna M. ^{[1
]}

Graeff, Richard ^{[2
]}

Garnham, Clive ^{[3
]}

Thomas, Mark P. ^{[1
]}

Galione, Antony ^{[3
]}

Potter, Barry V. L. ^{[2
]}

机构：

[1] Univ Bath, Dept Pharm & Pharmacol, Wolfson Lab Med Chem, Bath BA2 7AY, Avon, England

[2] Univ Hong Kong, Dept Physiol, Hong Kong, Hong Kong, Peoples R China

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

来源：

CHEMICAL COMMUNICATIONS | 2014年 / 50卷 / 19期

基金：

英国惠康基金;

关键词：

ADENOSINE 5'-DIPHOSPHATE RIBOSE; CA2+ RELEASE; INOSITOL TRISPHOSPHATE; MEDICINAL CHEMISTRY; CALCIUM-RELEASE; ANALOGS; PYROPHOSPHATE; CADPR; CD38; DERIVATIVES;

D O I：

10.1039/c3cc49249d

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Analogues of the potent Ca2+ releasing second messenger cyclic ADP-ribose (cADPR) with a 1,2,3-triazole pyrophosphate bioisostere were synthesised by click-mediated macrocyclisation. The ability to activate Ca2+ release was surprisingly retained, and hydrolysis of cADPR by CD38 could also be inhibited, illustrating the potential of this approach to design drug-like signalling pathway modulators.

引用

页码：2458 / 2461

页数：4

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