Promiscuous coupling between the sulphonylurea receptor and inwardly rectifying potassium channels.

Journal article

Sulphonylureas are a class of drugs widely used to treat non-insulin-dependent diabetes mellitus. These drugs act by binding to a sulphonylurea receptor (SUR) in the pancreatic beta-cell membrane which inhibits an ATP-sensitive potassium (K-ATP) channel and thereby stimulates insulin secretion. There has been much debate as to whether SUR and the K-ATP channel are the same or separate proteins, whether SUR confers ATP-sensitivity on an ATP-insensitive pore-forming subunit, and whether sulphonylureas can also modulate other types of K-channel. We show here that SUR itself does not possess intrinsic channel activity but that it endows sulphonylurea sensitivity on several types of inwardly-rectifying K-channels. It does not necessarily confer ATP-sensitivity on these channels.

Authors: Ammälä, C; Moorhouse, A; Gribble, F; Ashfield, R; Proks, P

• Publication status: Published
• Journal: Nature
• Volume: 379
• Issue: 6565
• Pages: 545-548
• Publication date: 1996-02-01
• DOI: 10.1038/379545a0
• EISSN: 1476-4687
• ISSN: 0028-0836
• Language: English
• Keywords: Patch-Clamp Techniques; Sulfonylurea Compounds; Recombinant Proteins; Membrane Potentials; Glyburide; ATP-Binding Cassette Transporters; Receptors, Drug; Cell Line; Xenopus; Adenosine Triphosphate; Potassium Channels; Potassium Channels, Inwardly Rectifying; Cloning, Molecular; Animals; Cricetinae