'Click cyclic ADP-ribose': a neutral second messenger mimicElectronic supplementary information (ESI) available: Fig. S1-S3, experimental details, 1H- and 13C-NMR. See DOI: 10.1039/c3cc49249d

Analogues of the potent Ca 2+ 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 Ca 2+ release was surprisingly retained, and hydrolysis of cADPR by CD38 could also be inhib...

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Main Authors: Swarbrick, Joanna M, Graeff, Richard, Garnham, Clive, Thomas, Mark P, Galione, Antony, Potter, Barry V. L
Format: Article
Language:English
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Summary:Analogues of the potent Ca 2+ 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 Ca 2+ 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. Neutral synthetic analogues of the second messenger cADPR with a 1,2,3-triazole pyrophosphate bioisostere retain the ability to activate Ca 2+ release and to inhibit hydrolysis of cADPR by CD38.
ISSN:1359-7345
1364-548X
DOI:10.1039/c3cc49249d