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The Structural Basis of Peptide Binding at Class A G Protein-Coupled Receptors
G protein-coupled receptors (GPCRs) represent the largest membrane protein family and a significant target class for therapeutics. Receptors from GPCRs’ largest class, class A, influence virtually every aspect of human physiology. About 45% of the members of this family endogenously bind flexible pe...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8746363/ https://www.ncbi.nlm.nih.gov/pubmed/35011444 http://dx.doi.org/10.3390/molecules27010210 |
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author | Vu, Oanh Bender, Brian Joseph Pankewitz, Lisa Huster, Daniel Beck-Sickinger, Annette G. Meiler, Jens |
author_facet | Vu, Oanh Bender, Brian Joseph Pankewitz, Lisa Huster, Daniel Beck-Sickinger, Annette G. Meiler, Jens |
author_sort | Vu, Oanh |
collection | PubMed |
description | G protein-coupled receptors (GPCRs) represent the largest membrane protein family and a significant target class for therapeutics. Receptors from GPCRs’ largest class, class A, influence virtually every aspect of human physiology. About 45% of the members of this family endogenously bind flexible peptides or peptides segments within larger protein ligands. While many of these peptides have been structurally characterized in their solution state, the few studies of peptides in their receptor-bound state suggest that these peptides interact with a shared set of residues and undergo significant conformational changes. For the purpose of understanding binding dynamics and the development of peptidomimetic drug compounds, further studies should investigate the peptide ligands that are complexed to their cognate receptor. |
format | Online Article Text |
id | pubmed-8746363 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-87463632022-01-11 The Structural Basis of Peptide Binding at Class A G Protein-Coupled Receptors Vu, Oanh Bender, Brian Joseph Pankewitz, Lisa Huster, Daniel Beck-Sickinger, Annette G. Meiler, Jens Molecules Review G protein-coupled receptors (GPCRs) represent the largest membrane protein family and a significant target class for therapeutics. Receptors from GPCRs’ largest class, class A, influence virtually every aspect of human physiology. About 45% of the members of this family endogenously bind flexible peptides or peptides segments within larger protein ligands. While many of these peptides have been structurally characterized in their solution state, the few studies of peptides in their receptor-bound state suggest that these peptides interact with a shared set of residues and undergo significant conformational changes. For the purpose of understanding binding dynamics and the development of peptidomimetic drug compounds, further studies should investigate the peptide ligands that are complexed to their cognate receptor. MDPI 2021-12-30 /pmc/articles/PMC8746363/ /pubmed/35011444 http://dx.doi.org/10.3390/molecules27010210 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Review Vu, Oanh Bender, Brian Joseph Pankewitz, Lisa Huster, Daniel Beck-Sickinger, Annette G. Meiler, Jens The Structural Basis of Peptide Binding at Class A G Protein-Coupled Receptors |
title | The Structural Basis of Peptide Binding at Class A G Protein-Coupled Receptors |
title_full | The Structural Basis of Peptide Binding at Class A G Protein-Coupled Receptors |
title_fullStr | The Structural Basis of Peptide Binding at Class A G Protein-Coupled Receptors |
title_full_unstemmed | The Structural Basis of Peptide Binding at Class A G Protein-Coupled Receptors |
title_short | The Structural Basis of Peptide Binding at Class A G Protein-Coupled Receptors |
title_sort | structural basis of peptide binding at class a g protein-coupled receptors |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8746363/ https://www.ncbi.nlm.nih.gov/pubmed/35011444 http://dx.doi.org/10.3390/molecules27010210 |
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