‘Click cyclic ADP-ribose’: a neutral second messenger mimic

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 inh...

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Detalles Bibliográficos
Autores principales: Swarbrick, Joanna M., Graeff, Richard, Garnham, Clive, Thomas, Mark P., Galione, Antony, Potter, Barry V. L.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Royal Society of Chemistry 2014
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4047616/
https://www.ncbi.nlm.nih.gov/pubmed/24452494
http://dx.doi.org/10.1039/c3cc49249d
Descripción
Sumario: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.

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