Target intelligence / Profile preview

Glucagon-like peptide 1 receptor (GLP-1R) (GLP-1R)

Target
GLP-1R
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

The Glucagon-like peptide 1 receptor (GLP-1R) is a class B G protein-coupled receptor that plays a critical role in glucose homeostasis and energy regulation [2, 6]. It is primarily expressed in the pancreatic beta cells, where its activation by the incretin hormone GLP-1 or synthetic agonists like TQZ2451 (a liraglutide biosimilar) stimulates insulin secretion in a glucose-dependent manner [4, 6]. Additionally, GLP-1R activation suppresses glucagon release from alpha cells, slows gastric emptying, and acts on the central nervous system to increase satiety and reduce food intake [2, 3]. These multi-organ effects make the GLP-1 receptor a primary therapeutic target for the treatment of type 2 diabetes and obesity [6, 7]. Beyond metabolic control, ongoing research is exploring the receptor's potential roles in cardiovascular protection and neurodegenerative diseases [2, 8]. The development of long-acting agonists like TQZ2451 aims to provide sustained glycemic control and weight management for patients with metabolic disorders [4].

Other names
GLP1RGLP-1 receptorGlucagon-like peptide 1 receptor
02

Mechanism of action

Agonism of the GLP-1 receptor, leading to increased intracellular cAMP and glucose-dependent insulin secretion [4, 6].

03

Biological functions

Signal transductionInsulin secretionGlucagon suppressionGastric emptyingSatiety
04

Disease associations

Type 2 diabetesObesityCardiovascular disease
05

Safety considerations

Gastrointestinal side effects (nausea, vomiting, diarrhea)Risk of pancreatitisPotential risk of medullary thyroid carcinomaHypoglycemia (when used with insulin or sulfonylureas)
06

Interacting drugs

6 more in the full profile.

07

Biomarkers

HbA1cFasting plasma glucoseBody weightC-peptideInsulin levels

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