Trends in antidiabetic drug discovery: FDA approved drugs, new drugs in clinical trials and global sales

AD Dahlén, G Dashi, I Maslov, MM Attwood… - Frontiers in …, 2022 - frontiersin.org
Type 2 diabetes mellitus (T2DM) continues to be a substantial medical problem due to its
increasing global prevalence and because chronic hyperglycemic states are closely linked …

GPCR-mediated signaling of metabolites

AS Husted, M Trauelsen, O Rudenko, SA Hjorth… - Cell metabolism, 2017 - cell.com
In addition to their bioenergetic intracellular function, several classical metabolites act as
extracellular signaling molecules activating cell-surface G-protein-coupled receptors …

International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid receptors and their ligands: beyond CB1 and CB2

RG Pertwee, AC Howlett, ME Abood… - Pharmacological …, 2010 - Elsevier
There are at least two types of cannabinoid receptors (CB 1 and CB 2). Ligands activating
these G protein-coupled receptors (GPCRs) include the phytocannabinoid Δ 9 …

Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120

A Hirasawa, K Tsumaya, T Awaji, S Katsuma… - Nature medicine, 2005 - nature.com
Diabetes, a disease in which the body does not produce or use insulin properly, is a serious
global health problem,,. Gut polypeptides secreted in response to food intake, such as …

Structural diversity of G protein-coupled receptors and significance for drug discovery

MC Lagerström, HB Schiöth - Nature reviews Drug discovery, 2008 - nature.com
G protein-coupled receptors (GPCRs) are the largest family of membrane-bound receptors
and also the targets of many drugs. Understanding of the functional significance of the wide …

TLR4 at the crossroads of nutrients, gut microbiota, and metabolic inflammation

LA Velloso, F Folli, MJ Saad - Endocrine reviews, 2015 - academic.oup.com
Obesity is accompanied by the activation of low-grade inflammatory activity in metabolically
relevant tissues. Studies have shown that obesity-associated insulin resistance results from …

Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents

HA Overton, AJ Babbs, SM Doel, MCT Fyfe… - Cell metabolism, 2006 - cell.com
The endogenous lipid signaling agent oleoylethanolamide (OEA) has recently been
described as a peripherally acting agent that reduces food intake and body weight gain in …

[HTML][HTML] Comprehensive repertoire and phylogenetic analysis of the G protein-coupled receptors in human and mouse

TK Bjarnadóttir, DE Gloriam, SH Hellstrand… - Genomics, 2006 - Elsevier
Understanding differences in the repertoire of orthologous gene pairs is vital for
interpretation of pharmacological and physiological experiments if conclusions are …

The repertoire of G-protein–coupled receptors in fully sequenced genomes

R Fredriksson, HB Schiöth - Molecular pharmacology, 2005 - Elsevier
The superfamily of G-protein–coupled receptors (GPCRs) is one of the largest and most
studied families of proteins. We created Hidden Markov Models derived from sorted groups …

Fatty acid signaling mechanisms in neural cells: fatty acid receptors

LJ Falomir-Lockhart, GF Cavazzutti… - Frontiers in cellular …, 2019 - frontiersin.org
Fatty acids (FAs) are typically associated with structural and metabolic roles, as they can be
stored as triglycerides, degraded by β-oxidation or used in phospholipids' synthesis, the …