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TitleMechanism of pharmacochaperoning in a mammalian K channel revealed by cryo-EM.
Journal, issue, pagesElife, Vol. 8, Year 2019
Publish dateJul 25, 2019
AuthorsGregory M Martin / Min Woo Sung / Zhongying Yang / Laura M Innes / Balamurugan Kandasamy / Larry L David / Craig Yoshioka / Show-Ling Shyng /
PubMed AbstractATP-sensitive potassium (K) channels composed of a pore-forming Kir6.2 potassium channel and a regulatory ABC transporter sulfonylurea receptor 1 (SUR1) regulate insulin secretion in pancreatic β- ...ATP-sensitive potassium (K) channels composed of a pore-forming Kir6.2 potassium channel and a regulatory ABC transporter sulfonylurea receptor 1 (SUR1) regulate insulin secretion in pancreatic β-cells to maintain glucose homeostasis. Mutations that impair channel folding or assembly prevent cell surface expression and cause congenital hyperinsulinism. Structurally diverse K inhibitors are known to act as pharmacochaperones to correct mutant channel expression, but the mechanism is unknown. Here, we compare cryoEM structures of a mammalian K channel bound to pharmacochaperones glibenclamide, repaglinide, and carbamazepine. We found all three drugs bind within a common pocket in SUR1. Further, we found the N-terminus of Kir6.2 inserted within the central cavity of the SUR1 ABC core, adjacent the drug binding pocket. The findings reveal a common mechanism by which diverse compounds stabilize the Kir6.2 N-terminus within SUR1's ABC core, allowing it to act as a firm 'handle' for the assembly of metastable mutant SUR1-Kir6.2 complexes.
External linksElife / PubMed:31343405 / PubMed Central
MethodsEM (single particle)
Resolution3.65 - 4.55 Å
Structure data

20528

6pz9

EMDB-20528, PDB-6pz9:
Cryo-EM structure of the pancreatic beta-cell SUR1 bound to ATP and repaglinide
Method: EM (single particle) / Resolution: 3.65 Å

20530

6pza

EMDB-20530, PDB-6pza:
Cryo-EM structure of the pancreatic beta-cell SUR1 bound to ATP and glibenclamide
Method: EM (single particle) / Resolution: 3.74 Å

20533

6pzb

EMDB-20533, PDB-6pzb:
Cryo-EM structure of the pancreatic beta-cell SUR1 Apo state
Method: EM (single particle) / Resolution: 4.55 Å

20534

6pzc

EMDB-20534, PDB-6pzc:
Cryo-EM structure of the pancreatic beta-cell SUR1 bound to carbamazepine
Method: EM (single particle) / Resolution: 4.34 Å

20535

6pzi

EMDB-20535, PDB-6pzi:
Cryo-EM structure of the pancreatic beta-cell SUR1 bound to ATP only
Method: EM (single particle) / Resolution: 4.5 Å

Chemicals

ChemComp-BJX:
Repaglinide / medication*YM

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

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

Source
  • cricetus cricetus (black-bellied hamster)
  • rattus norvegicus (Norway rat)
KeywordsMEMBRANE PROTEIN / KATP / SUR1 / RPG / GBC / apo / carbamazepine / ATP

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