'Click cyclic ADP-ribose'

Joanna M. Swarbrick, Richard Graeff, Clive Garnham, Mark P. Thomas, Antony Galione, Barry V. L. Potter

OAI: oai:purehost.bath.ac.uk:publications/afe572a6-c47a-4dd2-9213-85b85271ba63 • DOI: https://doi.org/10.1039/c3cc49249d

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 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