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'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
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.
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页码:2458 / 2461
页数:4
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