G protein-coupled receptors: structure-and function-based drug discovery
D Yang, Q Zhou, V Labroska, S Qin… - Signal transduction and …, 2021 - nature.com
As one of the most successful therapeutic target families, G protein-coupled receptors
(GPCRs) have experienced a transformation from random ligand screening to knowledge …
(GPCRs) have experienced a transformation from random ligand screening to knowledge …
Molecular dynamics simulations in drug discovery and pharmaceutical development
Molecular dynamics (MD) simulations have become increasingly useful in the modern drug
development process. In this review, we give a broad overview of the current application …
development process. In this review, we give a broad overview of the current application …
Common activation mechanism of class A GPCRs
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …
physiology. Understanding receptor activation mechanism is critical for discovering novel …
The tethered peptide activation mechanism of adhesion GPCRs
X Barros-Álvarez, RM Nwokonko, A Vizurraga… - Nature, 2022 - nature.com
Adhesion G-protein-coupled receptors (aGPCRs) are characterized by the presence of auto-
proteolysing extracellular regions that are involved in cell–cell and cell–extracellular matrix …
proteolysing extracellular regions that are involved in cell–cell and cell–extracellular matrix …
GPCR signaling regulation: the role of GRKs and arrestins
VV Gurevich, EV Gurevich - Frontiers in pharmacology, 2019 - frontiersin.org
Every animal species expresses hundreds of different G protein-coupled receptors (GPCRs)
that respond to a wide variety of external stimuli. GPCRs-driven signaling pathways are …
that respond to a wide variety of external stimuli. GPCRs-driven signaling pathways are …
Mechanisms of signalling and biased agonism in G protein-coupled receptors
D Wootten, A Christopoulos, M Marti-Solano… - … reviews Molecular cell …, 2018 - nature.com
G protein-coupled receptors (GPCRs) are the largest group of cell surface receptors in
humans that signal in response to diverse inputs and regulate a plethora of cellular …
humans that signal in response to diverse inputs and regulate a plethora of cellular …
Structure and dynamics of GPCR signaling complexes
D Hilger, M Masureel, BK Kobilka - Nature structural & molecular …, 2018 - nature.com
G-protein-coupled receptors (GPCRs) relay numerous extracellular signals by triggering
intracellular signaling through coupling with G proteins and arrestins. Recent breakthroughs …
intracellular signaling through coupling with G proteins and arrestins. Recent breakthroughs …
Structure of the µ-opioid receptor–Gi protein complex
The μ-opioid receptor (μOR) is a G-protein-coupled receptor (GPCR) and the target of most
clinically and recreationally used opioids. The induced positive effects of analgesia and …
clinically and recreationally used opioids. The induced positive effects of analgesia and …
Biased signalling: from simple switches to allosteric microprocessors
G protein-coupled receptors (GPCRs) are the largest class of receptors in the human
genome and some of the most common drug targets. It is now well established that GPCRs …
genome and some of the most common drug targets. It is now well established that GPCRs …
[HTML][HTML] Pharmacogenomics of GPCR drug targets
Natural genetic variation in the human genome is a cause of individual differences in
responses to medications and is an underappreciated burden on public health. Although …
responses to medications and is an underappreciated burden on public health. Although …