ATP-binding cassette sub-family C member 8 (SUR1) (ABCC8)

The ATP-binding cassette sub-family C member 8 (ABCC8), commonly known as the Sulfonylurea receptor 1 (SUR1), is a critical regulatory subunit of the ATP-sensitive potassium (K_ATP) channel found in pancreatic beta cells (UniProt, 2024). This channel functions as a metabolic sensor, coupling the intracellular ATP/ADP ratio to the cell's membrane potential to regulate insulin secretion (PubMed, PMC2642993). When blood glucose levels rise, the resulting increase in ATP leads to the closure of the K_ATP channel via SUR1, triggering membrane depolarization, calcium influx, and subsequent insulin release (StatPearls, 2023). Mutations in the ABCC8 gene are a primary cause of glycemic disorders, including neonatal diabetes and congenital hyperinsulinism, highlighting its central role in glucose homeostasis (NIH, GeneReviews). Pharmacologically, SUR1 is the primary target for sulfonylureas and meglitinides, which promote insulin secretion by closing the channel to treat type 2 diabetes (PubChem, CID 3488). Conversely, potassium channel openers like diazoxide bind to SUR1 to maintain the channel in an open state, which is used to treat conditions of excessive insulin secretion (NCBI, NBK537154).

Other names

Sulfonylurea receptor 1SUR1ABC36HRINSMRP8PHHI

Sulfonylureas and meglitinides bind to the SUR1 subunit of the K_ATP channel to induce channel closure, which triggers membrane depolarization and subsequent insulin release; conversely, diazoxide binds to SUR1 to stabilize the channel in the open state, inhibiting insulin secretion.