Glucagon-like peptide 1 receptor (GLP1R) (GLP1R)

The Glucagon-like peptide 1 receptor (GLP1R) is a Class B G protein-coupled receptor (GPCR) that serves as a primary regulator of glucose metabolism and energy balance [1, 3]. It is predominantly expressed in the pancreatic beta cells, where its activation by the incretin hormone GLP-1 stimulates insulin secretion in a glucose-dependent manner [1, 5]. This mechanism allows for effective blood sugar control with a low risk of hypoglycemia [1, 9]. Beyond the pancreas, GLP1R is found in the gastrointestinal tract, where it slows gastric emptying, and in the central nervous system, where it modulates satiety and suppresses appetite [2, 6]. These multi-organ effects have made GLP1R a cornerstone therapeutic target for the treatment of type 2 diabetes and obesity [8, 9]. Therapeutic agents targeting this receptor, such as semaglutide and tirzepatide, have demonstrated significant efficacy in weight loss and cardiovascular risk reduction [10, 11]. Furthermore, GLP1R activation is being investigated for its potential neuroprotective effects in Alzheimer's and Parkinson's diseases [3, 15]. The receptor also plays a role in reducing systemic inflammation and improving outcomes in metabolic dysfunction-associated steatohepatitis (MASH) [3, 10]. While the physiological secretion of GLP-1 from intestinal L-cells is a key upstream process, the receptor itself remains the primary focus of pharmacological intervention [1, 2]. Overall, GLP1R represents one of the most clinically impactful targets in modern metabolic medicine [17].

Other names

GLP-1RGLP1RGlucagon-like peptide 1 receptorIncretin receptorGLP-1 receptor

GLP-1 receptor agonist