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G-Protein Coupled Receptors Targeted by Analgesic Venom Peptides

School of Biomedical Sciences, University of Queensland, Brisbane, QLD 4072, Australia
Author to whom correspondence should be addressed.
Academic Editors: Stuart M. Brierley and Irina Vetter
Toxins 2017, 9(11), 372;
Received: 24 October 2017 / Revised: 13 November 2017 / Accepted: 13 November 2017 / Published: 16 November 2017
(This article belongs to the Special Issue Animal Venoms and Pain)
Chronic pain is a complex and debilitating condition associated with a large personal and socioeconomic burden. Current pharmacological approaches to treating chronic pain such as opioids, antidepressants and anticonvulsants exhibit limited efficacy in many patients and are associated with dose-limiting side effects that hinder their clinical use. Therefore, improved strategies for the pharmacological treatment of pathological pain are urgently needed. G-protein coupled receptors (GPCRs) are ubiquitously expressed on the surface of cells and act to transduce extracellular signals and regulate physiological processes. In the context of pain, numerous and diverse families of GPCRs expressed in pain pathways regulate most aspects of physiological and pathological pain and are thus implicated as potential targets for therapy of chronic pain. In the search for novel compounds that produce analgesia via GPCR modulation, animal venoms offer an enormous and virtually untapped source of potent and selective peptide molecules. While many venom peptides target voltage-gated and ligand-gated ion channels to inhibit neuronal excitability and blunt synaptic transmission of pain signals, only a small proportion are known to interact with GPCRs. Of these, only a few have shown analgesic potential in vivo. Here we review the current state of knowledge regarding venom peptides that target GPCRs to produce analgesia, and their development as therapeutic compounds. View Full-Text
Keywords: pain; GPCR; venom peptide; analgesia; Conus pain; GPCR; venom peptide; analgesia; Conus
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Daniel, J.T.; Clark, R.J. G-Protein Coupled Receptors Targeted by Analgesic Venom Peptides. Toxins 2017, 9, 372.

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