β− Arrestins: structure, function, physiology, and pharmacological perspectives

J Wess, AB Oteng, O Rivera-Gonzalez… - Pharmacological …, 2023 - Elsevier
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 …

Glucagon-like peptide-1 and its class BG protein–coupled receptors: a long march to therapeutic successes

C De Graaf, D Donnelly, D Wootten, J Lau… - Pharmacological …, 2016 - Elsevier
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 …

[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 …

The role of kinetic context in apparent biased agonism at GPCRs

C Klein Herenbrink, DA Sykes, P Donthamsetti… - Nature …, 2016 - nature.com
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 …

Mechanisms of regulation of the chemokine-receptor network

MJ Stone, JA Hayward, C Huang, Z E. Huma… - International journal of …, 2017 - mdpi.com
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 …

Biased agonism: An emerging paradigm in GPCR drug discovery

Z Rankovic, TF Brust, LM Bohn - Bioorganic & medicinal chemistry letters, 2016 - Elsevier
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 …

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 …

[BUCH][B] Introduction to proteins: structure, function, and motion

A Kessel, N Ben-Tal - 2018 - taylorfrancis.com
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 …

A kinetic view of GPCR allostery and biased agonism

JR Lane, LT May, RG Parton, PM Sexton… - Nature chemical …, 2017 - nature.com
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 …

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 …