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The Retinoid and Non-Retinoid Ligands of the Rod Visual G Protein-Coupled Receptor
G protein-coupled receptors (GPCRs) play a predominant role in the drug discovery effort. These cell surface receptors are activated by a variety of specific ligands that bind to the orthosteric binding pocket located in the extracellular part of the receptor. In addition, the potential binding site...
Autores principales: | , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2019
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6941084/ https://www.ncbi.nlm.nih.gov/pubmed/31835521 http://dx.doi.org/10.3390/ijms20246218 |
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author | Ortega, Joseph T. Jastrzebska, Beata |
author_facet | Ortega, Joseph T. Jastrzebska, Beata |
author_sort | Ortega, Joseph T. |
collection | PubMed |
description | G protein-coupled receptors (GPCRs) play a predominant role in the drug discovery effort. These cell surface receptors are activated by a variety of specific ligands that bind to the orthosteric binding pocket located in the extracellular part of the receptor. In addition, the potential binding sites located on the surface of the receptor enable their allosteric modulation with critical consequences for their function and pharmacology. For decades, drug discovery focused on targeting the GPCR orthosteric binding sites. However, finding that GPCRs can be modulated allosterically opened a new venue for developing novel pharmacological modulators with higher specificity. Alternatively, focus on discovering of non-retinoid small molecules beneficial in retinopathies associated with mutations in rhodopsin is currently a fast-growing pharmacological field. In this review, we summarize the accumulated knowledge on retinoid ligands and non-retinoid modulators of the light-sensing GPCR, rhodopsin and their potential in combating the specific vision-related pathologies. Also, recent findings reporting the potential of biologically active compounds derived from natural products as potent rod opsin modulators with beneficial effects against degenerative diseases related to this receptor are highlighted here. |
format | Online Article Text |
id | pubmed-6941084 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-69410842020-01-09 The Retinoid and Non-Retinoid Ligands of the Rod Visual G Protein-Coupled Receptor Ortega, Joseph T. Jastrzebska, Beata Int J Mol Sci Review G protein-coupled receptors (GPCRs) play a predominant role in the drug discovery effort. These cell surface receptors are activated by a variety of specific ligands that bind to the orthosteric binding pocket located in the extracellular part of the receptor. In addition, the potential binding sites located on the surface of the receptor enable their allosteric modulation with critical consequences for their function and pharmacology. For decades, drug discovery focused on targeting the GPCR orthosteric binding sites. However, finding that GPCRs can be modulated allosterically opened a new venue for developing novel pharmacological modulators with higher specificity. Alternatively, focus on discovering of non-retinoid small molecules beneficial in retinopathies associated with mutations in rhodopsin is currently a fast-growing pharmacological field. In this review, we summarize the accumulated knowledge on retinoid ligands and non-retinoid modulators of the light-sensing GPCR, rhodopsin and their potential in combating the specific vision-related pathologies. Also, recent findings reporting the potential of biologically active compounds derived from natural products as potent rod opsin modulators with beneficial effects against degenerative diseases related to this receptor are highlighted here. MDPI 2019-12-10 /pmc/articles/PMC6941084/ /pubmed/31835521 http://dx.doi.org/10.3390/ijms20246218 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Review Ortega, Joseph T. Jastrzebska, Beata The Retinoid and Non-Retinoid Ligands of the Rod Visual G Protein-Coupled Receptor |
title | The Retinoid and Non-Retinoid Ligands of the Rod Visual G Protein-Coupled Receptor |
title_full | The Retinoid and Non-Retinoid Ligands of the Rod Visual G Protein-Coupled Receptor |
title_fullStr | The Retinoid and Non-Retinoid Ligands of the Rod Visual G Protein-Coupled Receptor |
title_full_unstemmed | The Retinoid and Non-Retinoid Ligands of the Rod Visual G Protein-Coupled Receptor |
title_short | The Retinoid and Non-Retinoid Ligands of the Rod Visual G Protein-Coupled Receptor |
title_sort | retinoid and non-retinoid ligands of the rod visual g protein-coupled receptor |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6941084/ https://www.ncbi.nlm.nih.gov/pubmed/31835521 http://dx.doi.org/10.3390/ijms20246218 |
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