Issue 19, 2014
From the journal:

Chemical Communications

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

Joanna M. Swarbrick,a   Richard Graeff,b   Clive Garnham,c   Mark P. Thomas,a   Antony Galionec  and  Barry V. L. Potter*b  

* Corresponding authors

a Wolfson Laboratory of Medicinal Chemistry, Dept. of Pharmacy and Pharmacology, University of Bath, Bath, UK
E-mail: B.V.L.Potter@bath.ac.uk
Fax: +44-(0)1225-386114
Tel: +44-(0)1225-386639

b Department of Physiology, University of Hong Kong, Hong Kong, China

c Department of Pharmacology, University of Oxford, Mansfield Road, Oxford OX1 3QT, UK

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.

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

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Article information

DOI
https://doi.org/10.1039/C3CC49249D
Article type
Communication
Submitted
05 Dec 2013
Accepted
08 Jan 2014
First published
15 Jan 2014
This article is Open Access
Creative Commons BY license

Chem. Commun., 2014,50, 2458-2461

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

J. M. Swarbrick, R. Graeff, C. Garnham, M. P. Thomas, A. Galione and B. V. L. Potter, Chem. Commun., 2014, 50, 2458 DOI: 10.1039/C3CC49249D

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