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.
Journal article
2014-03-07T00:00:00+00:00
50
2458 - 2461
3
Animals, Calcium, Click Chemistry, Cyclic ADP-Ribose, Diphosphates, Female, Ovum, Sea Urchins, Second Messenger Systems