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TitleAnti-diabetic drug binding site in a mammalian K channel revealed by Cryo-EM.
Journal, issue, pagesElife, Vol. 6, Year 2017
Publish dateOct 24, 2017
AuthorsGregory M Martin / Balamurugan Kandasamy / Frank DiMaio / Craig Yoshioka / Show-Ling Shyng /
PubMed AbstractSulfonylureas are anti-diabetic medications that act by inhibiting pancreatic K channels composed of SUR1 and Kir6.2. The mechanism by which these drugs interact with and inhibit the channel has been ...Sulfonylureas are anti-diabetic medications that act by inhibiting pancreatic K channels composed of SUR1 and Kir6.2. The mechanism by which these drugs interact with and inhibit the channel has been extensively investigated, yet it remains unclear where the drug binding pocket resides. Here, we present a cryo-EM structure of a hamster SUR1/rat Kir6.2 channel bound to a high-affinity sulfonylurea drug glibenclamide and ATP at 3.63 Å resolution, which reveals unprecedented details of the ATP and glibenclamide binding sites. Importantly, the structure shows for the first time that glibenclamide is lodged in the transmembrane bundle of the SUR1-ABC core connected to the first nucleotide binding domain near the inner leaflet of the lipid bilayer. Mutation of residues predicted to interact with glibenclamide in our model led to reduced sensitivity to glibenclamide. Our structure provides novel mechanistic insights of how sulfonylureas and ATP interact with the K channel complex to inhibit channel activity.
External linksElife / PubMed:29035201 / PubMed Central
MethodsEM (single particle)
Resolution3.63 Å
Structure data

EMDB-7073, PDB-6baa:
Cryo-EM structure of the pancreatic beta-cell KATP channel bound to ATP and glibenclamide
Method: EM (single particle) / Resolution: 3.63 Å

Chemicals

ChemComp-ATP:
ADENOSINE-5'-TRIPHOSPHATE / ATP, energy-carrying molecule*YM / Adenosine triphosphate

ChemComp-GBM:
5-chloro-N-(2-{4-[(cyclohexylcarbamoyl)sulfamoyl]phenyl}ethyl)-2-methoxybenzamide / medication*YM / Glibenclamide

Source
  • rattus norvegicus (Norway rat)
  • cricetus cricetus (black-bellied hamster)
KeywordsAdenosine Triphosphate / Animals / Binding Sites / Cricetinae / Cryoelectron Microscopy / Glyburide / Hypoglycemic Agents / Kir6.2 channel / Models, Molecular / Potassium Channels, Inwardly Rectifying / Protein Binding / Sulfonylurea Receptors / METAL TRANSPORT / KATP / SUR1 / Kir6.2 / sulfonylurea receptor

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