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National Academy of Sciences, Proceedings of the National Academy of Sciences, 47(111), p. 16937-16942, 2014

DOI: 10.1073/pnas.1417365111

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Targeting the minor pocket of C5aR for the rational design of an oral allosteric inhibitor for inflammatory and neuropathic pain relief

Journal article published in 2014 by Alessio Moriconi, Mauro M. Teixeirah, Thiago M. Cunha ORCID, Guilherme R. Souza, Alexandre H. Lopes, Fernando Q. Cunha ORCID, Victor L. Carneiro, Larissa G. Pinto, Laura Brandolini, Andrea Aramini ORCID, Cinzia Bizzarri, Gianluca Bianchini, Andrea R. Beccari, Marco Fanton, Agostino Bruno and other authors.
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

Significance Persistent pain in inflammatory and neuropathic conditions is often refractory to conventional analgesic therapy, with most patients suffering with unrelieved pain and serious treatment-related side effects. There is still a tremendous need to identify novel therapeutics for pain control with innovative biological mechanisms and minimal side effects. In this paper we challenge the hypothesis that a conserved structural motif across the G protein-coupled receptor family plays a regulatory role in the negative modulation of receptor activation and use a multidisciplinary approach to the rational drug design and characterization of a novel potent allosteric inhibitor of the C5a anaphylatoxin receptor (C5aR), thus providing a new promising avenue for the improvement of pharmacotherapy of chronic pain.