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