'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
收藏
页码：2458 / 2461
页数：4
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