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Start Over Descriptor "peptide GPCR" Publisher mdpi ag
2 results on '"peptide GPCR"'

1. The Structural Basis of Peptide Binding at Class A G Protein-Coupled Receptors

Author

Oanh Vu, Brian Joseph Bender, Lisa Pankewitz, Daniel Huster, Annette G. Beck-Sickinger, and Jens Meiler

Subjects
peptide GPCR, class A GPCR, peptide docking, non-canonical amino acids, Organic chemistry, QD241-441
Abstract

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.

Published
2021
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2. The Structural Basis of Peptide Binding at Class A G Protein-Coupled Receptors

Author

Oanh Vu, Brian Joseph Bender, Lisa Pankewitz, Daniel Huster, Annette G. Beck-Sickinger, and Jens Meiler

Subjects
Models, Molecular, Molecular Conformation, Pharmaceutical Science, Organic chemistry, non-canonical amino acids, Review, peptide GPCR, class A GPCR, peptide docking, Ligands, Analytical Chemistry, Receptors, G-Protein-Coupled, Structure-Activity Relationship, QD241-441, Drug Discovery, Humans, Protein Interaction Domains and Motifs, Amino Acid Sequence, Physical and Theoretical Chemistry, Conserved Sequence, Binding Sites, Chemistry (miscellaneous), ddc:540, Molecular Medicine, Peptides, Protein Binding
Abstract

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.

Published
2022

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