[HTML][HTML] Free fatty acid receptors (FFARs) in adipose: physiological role and therapeutic outlook

S Al Mahri, SS Malik, M Al Ibrahim, E Haji, G Dairi… - Cells, 2022 - mdpi.com
Fatty acids (FFAs) are important biological molecules that serve as a major energy source
and are key components of biological membranes. In addition, FFAs play important roles in …

Targeting lipid GPCRs to treat type 2 diabetes mellitus—Progress and challenges

J Ghislain, V Poitout - Nature Reviews Endocrinology, 2021 - nature.com
Therapeutic approaches to the treatment of type 2 diabetes mellitus that are designed to
increase insulin secretion either directly target β-cells or indirectly target gastrointestinal …

[HTML][HTML] Dissecting the physiology and pathophysiology of glucagon-like peptide-1

S Paternoster, M Falasca - Frontiers in endocrinology, 2018 - frontiersin.org
An aging world population exposed to a sedentary life style is currently plagued by chronic
metabolic diseases, such as type-2 diabetes, that are spreading worldwide at an …

[HTML][HTML] GPCR in adipose tissue function—focus on lipolysis

D Malfacini, A Pfeifer - Biomedicines, 2023 - mdpi.com
Adipose tissue can be divided anatomically, histologically, and functionally into two major
entities white and brown adipose tissues (WAT and BAT, respectively). WAT is the primary …

Naturally occurring mutations in G protein-coupled receptors associated with obesity and type 2 diabetes mellitus

T Liu, RL Ji, YX Tao - Pharmacology & Therapeutics, 2022 - Elsevier
G protein-coupled receptors (GPCRs) are the largest family of membrane receptors involved
in the regulation of almost all known physiological processes. Dysfunctions of GPCR …

A novel model of diabetic complications: adipocyte mitochondrial dysfunction triggers massive β-cell hyperplasia

CM Kusminski, AL Ghaben, TS Morley, RJ Samms… - Diabetes, 2020 - Am Diabetes Assoc
Obesity-associated type 2 diabetes mellitus (T2DM) entails insulin resistance and loss of β-
cell mass. Adipose tissue mitochondrial dysfunction is emerging as a key component in the …

The current state of GPCR‐based drug discovery to treat metabolic disease

KW Sloop, PJ Emmerson, MA Statnick… - British journal of …, 2018 - Wiley Online Library
One approach of modern drug discovery is to identify agents that enhance or diminish signal
transduction cascades in various cell types and tissues by modulating the activity of GPCRs …

[HTML][HTML] Autocrine negative feedback regulation of lipolysis through sensing of NEFAs by FFAR4/GPR120 in WAT

AS Husted, JH Ekberg, E Tripp, TAD Nissen… - Molecular …, 2020 - Elsevier
Objectives Long-chain fatty acids (LCFAs) released from adipocytes inhibit lipolysis through
an unclear mechanism. We hypothesized that the LCFA receptor, FFAR4 (GPR120), which …

[HTML][HTML] A new synthetic dual agonist of GPR120/GPR40 induces GLP-1 secretion and improves glucose homeostasis in mice

G Bianchini, C Nigro, A Sirico, R Novelli… - Biomedicine & …, 2021 - Elsevier
G-protein coupled receptors 40 and 120 (GPR40 and GPR120) are increasingly emerging
as potential therapeutic targets for the treatment of altered glucose homeostasis, and their …

[HTML][HTML] Fatty acid mimetic PBI-4547 restores metabolic homeostasis via GPR84 in mice with non-alcoholic fatty liver disease

JC Simard, JF Thibodeau, M Leduc, M Tremblay… - Scientific Reports, 2020 - nature.com
Abstract Non-alcoholic Fatty Liver Disease (NAFLD) is the most common form of liver
disease and is associated with metabolic dysregulation. Although G protein-coupled …