β− Arrestins: structure, function, physiology, and pharmacological perspectives
The two β-arrestins, β-arrestin-1 and-2 (systematic names: arrestin-2 and-3, respectively),
are multifunctional intracellular proteins that regulate the activity of a very large number of …
are multifunctional intracellular proteins that regulate the activity of a very large number of …
Glucagon-like peptide-1 and its class BG protein–coupled receptors: a long march to therapeutic successes
The glucagon-like peptide (GLP)-1 receptor (GLP-1R) is a class BG protein–coupled
receptor (GPCR) that mediates the action of GLP-1, a peptide hormone secreted from three …
receptor (GPCR) that mediates the action of GLP-1, a peptide hormone secreted from three …
[HTML][HTML] Psychedelic-inspired drug discovery using an engineered biosensor
C Dong, C Ly, LE Dunlap, MV Vargas, J Sun… - Cell, 2021 - cell.com
Ligands can induce G protein-coupled receptors (GPCRs) to adopt a myriad of
conformations, many of which play critical roles in determining the activation of specific …
conformations, many of which play critical roles in determining the activation of specific …
The role of kinetic context in apparent biased agonism at GPCRs
Biased agonism describes the ability of ligands to stabilize different conformations of a
GPCR linked to distinct functional outcomes and offers the prospect of designing pathway …
GPCR linked to distinct functional outcomes and offers the prospect of designing pathway …
Mechanisms of regulation of the chemokine-receptor network
The interactions of chemokines with their G protein-coupled receptors promote the migration
of leukocytes during normal immune function and as a key aspect of the inflammatory …
of leukocytes during normal immune function and as a key aspect of the inflammatory …
Biased agonism: An emerging paradigm in GPCR drug discovery
G protein coupled receptors have historically been one of the most druggable classes of
cellular proteins. The members of this large receptor gene family couple to primary effectors …
cellular proteins. The members of this large receptor gene family couple to primary effectors …
Making sense of pharmacology: inverse agonism and functional selectivity
KA Berg, WP Clarke - International Journal of …, 2018 - academic.oup.com
Constitutive receptor activity/inverse agonism and functional selectivity/biased agonism are
2 concepts in contemporary pharmacology that have major implications for the use of drugs …
2 concepts in contemporary pharmacology that have major implications for the use of drugs …
[BUCH][B] Introduction to proteins: structure, function, and motion
Introduction to Proteins provides a comprehensive and state-of-the-art introduction to the
structure, function, and motion of proteins for students, faculty, and researchers at all levels …
structure, function, and motion of proteins for students, faculty, and researchers at all levels …
A kinetic view of GPCR allostery and biased agonism
G-protein-coupled receptors (GPCRs) are one of the most tractable classes of drug targets.
These dynamic proteins can adopt multiple active states that are linked to distinct functional …
These dynamic proteins can adopt multiple active states that are linked to distinct functional …
Biased ligands of G protein-coupled receptors (GPCRs): Structure–functional selectivity relationships (SFSRs) and therapeutic potential
L Tan, W Yan, JD McCorvy, J Cheng - Journal of medicinal …, 2018 - ACS Publications
G protein-coupled receptors (GPCRs) signal through both G-protein-dependent and G-
protein-independent pathways, and β-arrestin recruitment is the most recognized one of the …
protein-independent pathways, and β-arrestin recruitment is the most recognized one of the …