Referenced in: none

Automatically associated channels: Kir6.2

Title: [Mechanisms of action of peroral antidiabetics. Sulfonylurea preparations block the ATP-dependent potassium channels]

Authors: O Larsson, H Kindmark, R Bränström, P O Berggren

Journal, date & volume: Lakartidningen, 1997 Nov 26 , 94, 4473-7

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/9424548

Abstract
Although hypoglycaemic sulphonylureas have been used to treat non-insulin-dependent diabetes mellitus (NIDDM) for the past forty years, their mechanisms of action at the molecular level have only recently been elucidated. A combination of electrophysiological and molecular biological techniques showed the target of sulphonylureas to be a sulphonylurea receptor (SUR1) and potassium channel (Kir6.2) complex. Together, these two proteins form the ATP-dependent potassium (KATP) channel occurring in insulin-secreting cells. An increase in the blood glucose level triggers a chain of events in insulin-secreting cells and K(ATP) channel closure which is a prerequisite for insulin secretion. In NIDDM, however, an increase in blood glucose fails to close the K(ATP) channel satisfactorily, but this can be remedied by the administration of sulphonylureas.