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Receptor and Channel Heteromers as Pain Targets

Recent discoveries indicate that many G-protein coupled receptors (GPCRs) and channels involved in pain modulation are able to form receptor heteromers. Receptor and channel heteromers often display distinct signaling characteristics, pharmacological properties and physiological function in comparis...

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Detalles Bibliográficos
Autores principales: Berg, Kelly A., Patwardhan, Amol M., Akopian, Armen N.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2012
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3763638/
https://www.ncbi.nlm.nih.gov/pubmed/24281378
http://dx.doi.org/10.3390/ph5030249
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author Berg, Kelly A.
Patwardhan, Amol M.
Akopian, Armen N.
author_facet Berg, Kelly A.
Patwardhan, Amol M.
Akopian, Armen N.
author_sort Berg, Kelly A.
collection PubMed
description Recent discoveries indicate that many G-protein coupled receptors (GPCRs) and channels involved in pain modulation are able to form receptor heteromers. Receptor and channel heteromers often display distinct signaling characteristics, pharmacological properties and physiological function in comparison to monomer/homomer receptor or ion channel counterparts. It may be possible to capitalize on such unique properties to augment therapeutic efficacy while minimizing side effects. For example, drugs specifically targeting heteromers may have greater tissue specificity and analgesic efficacy. This review will focus on current progress in our understanding of roles of heteromeric GPCRs and channels in pain pathways as well as strategies for controlling pain pathways via targeting heteromeric receptors and channels. This approach may be instrumental in the discovery of novel classes of drugs and expand our repertoire of targets for pain pharmacotherapy.
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spelling pubmed-37636382013-11-14 Receptor and Channel Heteromers as Pain Targets Berg, Kelly A. Patwardhan, Amol M. Akopian, Armen N. Pharmaceuticals (Basel) Review Recent discoveries indicate that many G-protein coupled receptors (GPCRs) and channels involved in pain modulation are able to form receptor heteromers. Receptor and channel heteromers often display distinct signaling characteristics, pharmacological properties and physiological function in comparison to monomer/homomer receptor or ion channel counterparts. It may be possible to capitalize on such unique properties to augment therapeutic efficacy while minimizing side effects. For example, drugs specifically targeting heteromers may have greater tissue specificity and analgesic efficacy. This review will focus on current progress in our understanding of roles of heteromeric GPCRs and channels in pain pathways as well as strategies for controlling pain pathways via targeting heteromeric receptors and channels. This approach may be instrumental in the discovery of novel classes of drugs and expand our repertoire of targets for pain pharmacotherapy. MDPI 2012-02-23 /pmc/articles/PMC3763638/ /pubmed/24281378 http://dx.doi.org/10.3390/ph5030249 Text en © 2012 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Review
Berg, Kelly A.
Patwardhan, Amol M.
Akopian, Armen N.
Receptor and Channel Heteromers as Pain Targets
title Receptor and Channel Heteromers as Pain Targets
title_full Receptor and Channel Heteromers as Pain Targets
title_fullStr Receptor and Channel Heteromers as Pain Targets
title_full_unstemmed Receptor and Channel Heteromers as Pain Targets
title_short Receptor and Channel Heteromers as Pain Targets
title_sort receptor and channel heteromers as pain targets
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3763638/
https://www.ncbi.nlm.nih.gov/pubmed/24281378
http://dx.doi.org/10.3390/ph5030249
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