GPR119 receptor

The GPR119 receptor protein is a G protein-coupled receptor that is expressed in the pancreas, gastrointestinal tract and sebaceous glands, among others. Ligands of this receptor protein are the endogenous fatty acid ethanolamides oleoylethanolamide (OEA) and lysophosphatidylcholine (LPC). The recptor functions as a glucose-dependent insulinotropic receptor . Its activity is mediated by G proteins that activate adenylate cyclase.

GPR119 has also been shown to regulate the secretion of the hormones incretin and insulin (Ning Y et al. 2008). Furthermore, GPR119 was shown to be downregulated in the sebaceous glands of patients with acne. This may indicate that GPR119 signaling is impaired in acne. Apparently, the OEA/GPR119 signaling pathway is considered a positive regulator of sebocyte differentiation. Dysregulation of this pathway could contribute to the development of seborrhea and acne (Markovics A et al. 2020).

The GPR119 protein is a potential drug target for the treatment of type 2 diabetes.

Associated diseases associated with mutations in the GPR119 gene include type 2 diabetes mellitus.

1. Markovics A et al (2020) GPR119 Is a Potent Regulator of Human Sebocyte Biology. J Invest Dermatol 140:1909-1918.e8.
2. Ning Y et al. (2008) Endogenous and synthetic agonists of GPR119 differ in signalling pathways and their effects on insulin secretion in MIN6c4 insulinoma cells. British Journal of Pharmacology 155: 1056-1065.
3. Swaminath G (2008). Fatty acid binding receptors and their physiological role in type 2 diabetes. Archives of Pharmacy 341: 753-761.
4. Lan H et al. (2009) GPR119 is required for physiological regulation of glucagon-like peptide-1 secretion but not for metabolic homeostasis. The Journal of Endocrinology 201: 219-230.