Trends in GPCR drug discovery: new agents, targets and indications

AS Hauser, MM Attwood, M Rask-Andersen… - Nature reviews Drug …, 2017 - nature.com
G protein-coupled receptors (GPCRs) are the most intensively studied drug targets, mostly
due to their substantial involvement in human pathophysiology and their pharmacological …

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 …

International Union of Basic and Clinical Pharmacology. CX. Classification of receptors for 5-hydroxytryptamine; pharmacology and function

NM Barnes, GP Ahern, C Becamel, J Bockaert… - Pharmacological …, 2021 - Elsevier
HT receptors expressed throughout the human body are targets for established therapeutics
and various drugs in development. Their diversity of structure and function reflects the …

How ligands illuminate GPCR molecular pharmacology

D Wacker, RC Stevens, BL Roth - Cell, 2017 - cell.com
G protein-coupled receptors (GPCRs), which are modulated by a variety of endogenous and
synthetic ligands, represent the largest family of druggable targets in the human genome …

Structure-based virtual screening for ligands of G protein–coupled receptors: what can molecular docking do for you?

F Ballante, AJ Kooistra, S Kampen, C de Graaf… - Pharmacological …, 2021 - Elsevier
G protein–coupled receptors (GPCRs) constitute the largest family of membrane proteins in
the human genome and are important therapeutic targets. During the last decade, the …

Glycine: the smallest anti-inflammatory micronutrient

KA Aguayo-Cerón, F Sánchez-Muñoz… - International journal of …, 2023 - mdpi.com
Glycine is a non-essential amino acid with many functions and effects. Glycine can bind to
specific receptors and transporters that are expressed in many types of cells throughout an …

Structural insights into G-protein-coupled receptor allostery

DM Thal, A Glukhova, PM Sexton, A Christopoulos - Nature, 2018 - nature.com
G-protein-coupled receptors (GPCRs) are key cell-surface proteins that transduce external
environmental cues into biochemical signals across the membrane. GPCRs are intrinsically …

GABAA receptor: Positive and negative allosteric modulators

RW Olsen - Neuropharmacology, 2018 - Elsevier
Abstract gamma-Aminobutyric acid (GABA)-mediated inhibitory neurotransmission and the
gene products involved were discovered during the mid-twentieth century. Historically …

[HTML][HTML] LEAP2 is an endogenous antagonist of the ghrelin receptor

X Ge, H Yang, MA Bednarek, H Galon-Tilleman… - Cell metabolism, 2018 - cell.com
Ghrelin, an appetite-stimulatory hormone secreted by the stomach, was discovered as a
ligand for the growth hormone secretagogue receptor (GHSR). Through GHSR, ghrelin …

Cardiotoxic effects of common and emerging drugs: role of cannabinoid receptors

Y Bo, X Zhao, L Li - Clinical Science, 2024 - portlandpress.com
Drug-induced cardiotoxicity has become one of the most common and detrimental health
concerns, which causes significant loss to public health and drug resources. Cannabinoid …