Journal
CHEMICAL COMMUNICATIONS
Volume 50, Issue 19, Pages 2458-2461Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c3cc49249d
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Funding
- Wellcome Trust [084068, 082837, 084102, 101010]
- RCGAS [201105159001]
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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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