GLP1R Antibodies

Structure of GLP1R

The glucagon-like peptide 1 receptor encoded by the GLP1R gene is a G protein-coupled receptor with a molecular weight of approximately 59 kDa. There are certain differences in this molecular weight among different species, mainly due to the degree of receptor glycosylation modification and the minor changes in the amino acid sequence of the extracellular region.

This receptor protein is composed of approximately 463 amino acid residues and presents a classic seven-transmembrane topological structure. The core of its function lies in that the N-terminal extracellular domain can specifically recognize and bind to GLP-1 peptide hormones, and then activate the downstream Gαs protein signaling pathway through conformational changes in the transmembrane region. Several conserved amino acid residues (such as arginine and glutamic acid) on the extracellular second ring of the receptor play a decisive role in ligand binding affinity, while the intracellular third ring directly participates in the coupling and signal transduction of G proteins. This ingenious structural arrangement enables it to efficiently regulate insulin secretion and blood glucose homeostasis.

Fig. 1 Cryo-EM maps of retatrutide-bound GLP-1R.¹

Key structural properties of GLP1R:

• Classical seven-fold transmembrane (7TM) helical bundle structure
• The larger N-terminal extracellular domain, responsible for specific recognition of GLP-1
• Ligand binding pocket by transmembrane helical and extracellular ring together

Functions of GLP1R

The main function of the glucagon-like peptide-1 receptor (GLP-1R) encoded by the GLP1R gene is to mediate the physiological effects of glucagon-like peptide-1 (GLP-1). It plays a core role in a variety of physiological and pharmacological processes, including the regulation of blood glucose homeostasis, appetite control, and protection of the cardiovascular system.

The signal transduction of GLP-1R presents the characteristics of high efficiency and strict regulation. Unlike the extensive physiological effects of certain receptors, the signal transduction of GLP-1R is highly dependent on the concentration and tissue distribution of its specific ligand GLP-1, which enables it to respond precisely and promptly to postprandial blood glucose changes and play the role of an "intelligent sensor" in maintaining metabolic homeostasis.

Applications of GLP1R and GLP1R Antibody in Literature

1. Li, Wenzhuo, et al. "Structural insights into the triple agonism at GLP-1R, GIPR and GCGR manifested by retatrutide." Cell Discovery 10.1 (2024): 77. https://doi.org/10.1038/s41421-024-00700-0

The study employed cryo-electron microscopy to analyze the structure of the binding of the novel hypoglycemic and bariatric drug retalutide to GLP-1R, GIPR and GCGR, and to clarify its triple activation mechanism, providing a structural basis for optimizing the treatment of diabetes and obesity.

2. Ungvari, Zoltan, et al. "Prognostic impact of glucagon-like peptide-1 receptor (GLP1R) expression on cancer survival and its implications for GLP-1R agonist therapy: an integrative analysis across multiple tumor types." Geroscience (2025): 1-15. https://doi.org/10.1007/s11357-024-01494-5

This study reveals the dual prognostic role of GLP1R expression levels in different cancers. High expression can improve the survival of patients with bladder cancer, breast cancer, etc., but is associated with adverse prognoses such as cervical cancer and lung cancer, while having no significant effect in some cancers, suggesting its potential as an individualized cancer risk diagnosis and treatment marker.

3. Normand, Émilie, et al. "Association between the GLP1R A316T Mutation and Adolescent Idiopathic Scoliosis in French Canadian and Italian Cohorts." Genes 15.4 (2024): 481. https://doi.org/10.3390/genes15040481

Studies have shown that the GLP1R A316T gene polymorphism increases the risk of adolescent idiopathic scoliosis (AIS), but is not related to the severity, progression or body mass index of the disease. This discovery points to the potential role of GLP1R in the pathogenesis of AIS.

4. Hall, Elin, et al. "DNA methylation of the glucagon-like peptide 1 receptor (GLP1R) in human pancreatic islets." BMC medical genetics 14.1 (2013): 76. https://doi.org/10.1186/1471-2350-14-76

Research has found that the DNA methylation level at a specific CpG site of the GLP1R gene is negatively correlated with the expression of this gene in the islets of patients with type 2 diabetes, and positively correlated with BMI and HbA1c, suggesting that DNA methylation may be involved in the down-regulation of GLP1R in diabetes.

5. Farokhnia, Mehdi, et al. "Differential association between the GLP1R gene variants and brain functional connectivity according to the severity of alcohol use." Scientific reports 12.1 (2022): 13027. https://doi.org/10.1038/s41598-022-17190-3

Research shows that GLP1R gene variations (rs6923761 and rs1042044) are associated with brain functional connectivity. Among heavy drinkers, carrying the variant alleles is linked to enhanced internal connectivity in key brain networks such as the saliency network and the default network, suggesting that GLP1R may be involved in the neural mechanisms of alcohol dependence.

Creative Biolabs: GLP1R Antibodies for Research

Creative Biolabs specializes in the production of high-quality GLP1R antibodies for research and industrial applications. Our portfolio includes monoclonal antibodies tailored for ELISA, Flow Cytometry, Western blot, immunohistochemistry, and other diagnostic methodologies.

• Custom GLP1R Antibody Development: Tailor-made solutions to meet specific research requirements.
• Bulk Production: Large-scale antibody manufacturing for industry partners.
• Technical Support: Expert consultation for protocol optimization and troubleshooting.
• Aliquoting Services: Conveniently sized aliquots for long-term storage and consistent experimental outcomes.

For more details on our GLP1R antibodies, custom preparations, or technical support, contact us at email.