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'Click cyclic ADP-ribose': a neutral second messenger mimic.

ABSTRACT: 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.

SUBMITTER: Swarbrick JM 

PROVIDER: S-EPMC4047616 | biostudies-literature | 2014 Mar

REPOSITORIES: biostudies-literature

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'Click cyclic ADP-ribose': a neutral second messenger mimic.

Swarbrick Joanna M JM   Graeff Richard R   Garnham Clive C   Thomas Mark P MP   Galione Antony A   Potter Barry V L BV  

Chemical communications (Cambridge, England) 20140123 19

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. ...[more]

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