Cargando…

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...

Descripción completa

Detalles Bibliográficos
Autores principales: Vu, Oanh, Bender, Brian Joseph, Pankewitz, Lisa, Huster, Daniel, Beck-Sickinger, Annette G., Meiler, Jens
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
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
_version_ 1784630567449395200
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
work_keys_str_mv AT vuoanh thestructuralbasisofpeptidebindingatclassagproteincoupledreceptors
AT benderbrianjoseph thestructuralbasisofpeptidebindingatclassagproteincoupledreceptors
AT pankewitzlisa thestructuralbasisofpeptidebindingatclassagproteincoupledreceptors
AT husterdaniel thestructuralbasisofpeptidebindingatclassagproteincoupledreceptors
AT becksickingerannetteg thestructuralbasisofpeptidebindingatclassagproteincoupledreceptors
AT meilerjens thestructuralbasisofpeptidebindingatclassagproteincoupledreceptors
AT vuoanh structuralbasisofpeptidebindingatclassagproteincoupledreceptors
AT benderbrianjoseph structuralbasisofpeptidebindingatclassagproteincoupledreceptors
AT pankewitzlisa structuralbasisofpeptidebindingatclassagproteincoupledreceptors
AT husterdaniel structuralbasisofpeptidebindingatclassagproteincoupledreceptors
AT becksickingerannetteg structuralbasisofpeptidebindingatclassagproteincoupledreceptors
AT meilerjens structuralbasisofpeptidebindingatclassagproteincoupledreceptors