Abstract
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.
Original language | English (US) |
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Pages (from-to) | 2458-2461 |
Number of pages | 4 |
Journal | Chemical Communications |
Volume | 50 |
Issue number | 19 |
DOIs | |
State | Published - Feb 7 2014 |