Related Experiment Video

Updated: Apr 8, 2026

Homogeneous Time-resolved Förster Resonance Energy Transfer-based Assay for Detection of Insulin Secretion
07:30

Homogeneous Time-resolved Förster Resonance Energy Transfer-based Assay for Detection of Insulin Secretion

Published on: May 10, 2018

9.9K

FFA4 receptor (GPR120): A hot target for the development of anti-diabetic therapies

Hong-Da Liu1, Wen-bo Wang2, Zhi-gang Xu3

  • 1Key Laboratory Experimental Teratology of the Ministry of Education and Department of Biochemistry and Molecular Biology, Shandong University, School of Medicine, Jinan, Shandong, China; Qilu Hospital of Shandong University, Jinan, Shandong, China; Shandong Provincial School Key Laboratory for Protein Science of Chronic Degenerative Diseases, Jinan, Shandong, China.

European Journal of Pharmacology
|July 1, 2015
PubMed

Insights

The Free Fatty Acid 4 receptor (FFA4 receptor) plays a key role in metabolic homeostasis. Targeting this receptor shows promise for treating diabetes and inflammation.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Endocrinology

Background:

  • The Free Fatty Acid 4 receptor (FFA4 receptor), a G protein-coupled receptor (GPCR), senses fatty acids like omega-3s.
  • FFA4 receptor is found in various tissues, including the lungs, colon, and adipose tissue.
  • Its activation influences inflammation, insulin sensitivity, adipogenesis, and hormone secretion.

Purpose of the Study:

  • To review recent research on FFA4 receptor's physiological and biochemical roles.
  • To highlight signaling mechanisms and ligand identification for FFA4 receptor.
  • To explore FFA4 receptor as a potential drug target for metabolic and inflammatory diseases.

Main Methods:

  • Literature review of physiological and biochemical studies.
  • Analysis of signaling pathways activated by FFA4 receptor.
  • Identification and characterization of FFA4 receptor ligands.

Main Results:

  • FFA4 receptor activation inhibits inflammation and improves insulin sensitivity.
  • FFA4 receptor influences adipogenesis and regulates gastro-intestinal and pancreatic hormone secretion.
  • Recent studies have identified novel ligands and elucidated signaling pathways.

Conclusions:

  • FFA4 receptor is crucial for maintaining metabolic homeostasis.
  • Selective FFA4 receptor agonists hold therapeutic potential for diabetes and inflammation.
  • Further research into FFA4 receptor mechanisms and ligands can advance drug development.
Keywords:
ArrestinBiased signalingGPR120Glucose metabolismLipid

More Related Videos

Studying the Hypothalamic Insulin Signal to Peripheral Glucose Intolerance with a Continuous Drug Infusion System into the Mouse Brain08:32

Studying the Hypothalamic Insulin Signal to Peripheral Glucose Intolerance with a Continuous Drug Infusion System into the Mouse Brain

Published on: January 4, 2018

11.0K

Related Concept Videos

Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a...
1.1K
Glucagon-like Receptor Agonists01:24

Glucagon-like Receptor Agonists

Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by...
1.3K
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
19.8K
Oral Hypoglycemic Agents: Glinides01:06

Oral Hypoglycemic Agents: Glinides

Repaglinide (Prandin) and Nateglinide (Starlix), known as glinides, are oral insulin secretagogues that stimulate insulin release from pancreatic β cells by closing the ATP-sensitive potassium channels (KATP channel). Repaglinide controls insulin release from pancreatic β cells by managing potassium efflux. It shares two binding sites with sulfonylureas and also has a unique site, indicating overlapping mechanisms of action. With a rapid onset and a 4-7 hour duration, it effectively...
963
Oral Hypoglycemic Agents: Biguanides and Glitazones01:26

Oral Hypoglycemic Agents: Biguanides and Glitazones

Biguanides, particularly metformin (Glucophage), are insulin sensitizers that enhance glucose uptake, thereby reducing insulin resistance. Unlike sulfonylureas, metformin doesn't prompt insulin secretion, which helps to curb hypoglycemia risk. Metformin is beneficial in treating conditions like polycystic ovary syndrome due to its insulin-resistance reduction capability. The drug's primary action involves curtailing hepatic gluconeogenesis, a significant contributor to high blood...
966
Oral Hypoglycemic Agents: α-Glucosidase Inhibitors01:19

Oral Hypoglycemic Agents: α-Glucosidase Inhibitors

α-glucosidase inhibitors, including acarbose (Precose), miglitol (Glyset), and voglibose (Voglib) (primarily available in Asia), are drugs that control blood sugar levels by delaying the digestion of starch and disaccharides. They achieve this by inhibiting α-glucosidase enzymes in the intestine, which slow the absorption of carbohydrates in the intestine, which in turn leads to a prolonged release of the glucoregulatory hormone GLP-1 from intestinal L-cells.
Acarbose and miglitol are...
893