Glucagon receptor mRNA (GCGR mRNA)

Glucagon receptor (GCGR) mRNA is the messenger RNA transcript that encodes the glucagon receptor, a Class B G protein-coupled receptor primarily located on hepatocytes (Source: UniProt P47871). This mRNA serves as a therapeutic target for antisense oligonucleotides (ASOs) designed to treat metabolic disorders like type 2 diabetes by reducing the synthesis of the GCGR protein (Source: PubMed PMID: 25643358). By lowering the abundance of the glucagon receptor, these therapies decrease hepatic glucose production, which is often pathologically elevated in diabetic patients (Source: PubMed PMID: 29127220). Clinical evaluation of drugs targeting GCGR mRNA, such as IONIS-GCGRRx, has demonstrated significant reductions in glycated hemoglobin (HbA1c) and fasting blood glucose (Source: PubMed PMID: 29127220). However, the reduction in glucagon signaling leads to a compensatory increase in circulating glucagon levels and has been associated with potential safety concerns such as pancreatic alpha-cell hyperplasia and increases in liver fat or enzymes (Source: PubMed PMID: 30104248). The use of ligand-conjugated antisense technology (LICA) has been explored to improve the potency and liver-targeting specificity of these mRNA-targeted agents (Source: PubMed PMID: 29127220). Overall, GCGR mRNA represents a validated target for RNA-based therapeutics aiming to restore glucose balance in metabolic disease.

Other names

Glucagon receptor messenger RNAGCGR transcriptGCGR mRNA

Antisense oligonucleotide-mediated degradation of mRNA via RNase H, leading to reduced translation of the glucagon receptor protein.