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Principles of agonist recognition in Cys-loop receptors
Cys-loop receptors are ligand-gated ion channels that are activated by a structurally diverse array of neurotransmitters, including acetylcholine, serotonin, glycine, and GABA. After the term “chemoreceptor” emerged over 100 years ago, there was some wait until affinity labeling, molecular cloning,...
Autores principales: | , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Frontiers Media S.A.
2014
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4006026/ https://www.ncbi.nlm.nih.gov/pubmed/24795655 http://dx.doi.org/10.3389/fphys.2014.00160 |
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author | Lynagh, Timothy Pless, Stephan A. |
author_facet | Lynagh, Timothy Pless, Stephan A. |
author_sort | Lynagh, Timothy |
collection | PubMed |
description | Cys-loop receptors are ligand-gated ion channels that are activated by a structurally diverse array of neurotransmitters, including acetylcholine, serotonin, glycine, and GABA. After the term “chemoreceptor” emerged over 100 years ago, there was some wait until affinity labeling, molecular cloning, functional studies, and X-ray crystallography experiments identified the extracellular interface of adjacent subunits as the principal site of agonist binding. The question of how subtle differences at and around agonist-binding sites of different Cys-loop receptors can accommodate transmitters as chemically diverse as glycine and serotonin has been subject to intense research over the last three decades. This review outlines the functional diversity and current structural understanding of agonist-binding sites, including those of invertebrate Cys-loop receptors. Together, this provides a framework to understand the atomic determinants involved in how these valuable therapeutic targets recognize and bind their ligands. |
format | Online Article Text |
id | pubmed-4006026 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2014 |
publisher | Frontiers Media S.A. |
record_format | MEDLINE/PubMed |
spelling | pubmed-40060262014-05-02 Principles of agonist recognition in Cys-loop receptors Lynagh, Timothy Pless, Stephan A. Front Physiol Physiology Cys-loop receptors are ligand-gated ion channels that are activated by a structurally diverse array of neurotransmitters, including acetylcholine, serotonin, glycine, and GABA. After the term “chemoreceptor” emerged over 100 years ago, there was some wait until affinity labeling, molecular cloning, functional studies, and X-ray crystallography experiments identified the extracellular interface of adjacent subunits as the principal site of agonist binding. The question of how subtle differences at and around agonist-binding sites of different Cys-loop receptors can accommodate transmitters as chemically diverse as glycine and serotonin has been subject to intense research over the last three decades. This review outlines the functional diversity and current structural understanding of agonist-binding sites, including those of invertebrate Cys-loop receptors. Together, this provides a framework to understand the atomic determinants involved in how these valuable therapeutic targets recognize and bind their ligands. Frontiers Media S.A. 2014-04-24 /pmc/articles/PMC4006026/ /pubmed/24795655 http://dx.doi.org/10.3389/fphys.2014.00160 Text en Copyright © 2014 Lynagh and Pless. http://creativecommons.org/licenses/by/3.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms. |
spellingShingle | Physiology Lynagh, Timothy Pless, Stephan A. Principles of agonist recognition in Cys-loop receptors |
title | Principles of agonist recognition in Cys-loop receptors |
title_full | Principles of agonist recognition in Cys-loop receptors |
title_fullStr | Principles of agonist recognition in Cys-loop receptors |
title_full_unstemmed | Principles of agonist recognition in Cys-loop receptors |
title_short | Principles of agonist recognition in Cys-loop receptors |
title_sort | principles of agonist recognition in cys-loop receptors |
topic | Physiology |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4006026/ https://www.ncbi.nlm.nih.gov/pubmed/24795655 http://dx.doi.org/10.3389/fphys.2014.00160 |
work_keys_str_mv | AT lynaghtimothy principlesofagonistrecognitionincysloopreceptors AT plessstephana principlesofagonistrecognitionincysloopreceptors |