KATP channels in focus: Progress toward a structural understanding of ligand regulation

Gregory M. Martin, Bruce L. Patton, Show Ling Shyng

Research output: Contribution to journalReview articlepeer-review

7 Scopus citations

Abstract

KATP channels are hetero-octameric complexes of four inward rectifying potassium channels, Kir6.1 or Kir6.2, and four sulfonylurea receptors, SUR1, SUR2A, or SUR2B from the ABC transporter family. This unique combination enables KATP channels to couple intracellular ATP/ADP ratios, through gating, with membrane excitability, thus regulating a broad range of cellular activities. The prominence of KATP channels in human physiology, disease, and pharmacology has long attracted research interest. Since 2017, a steady flow of high-resolution KATP cryoEM structures has revealed complex and dynamic interactions between channel subunits and their ligands. Here, we highlight insights from recent structures that begin to provide mechanistic explanations for decades of experimental data and discuss the remaining knowledge gaps in our understanding of KATP channel regulation.

Original languageEnglish (US)
Article number102541
JournalCurrent Opinion in Structural Biology
Volume79
DOIs
StatePublished - Apr 2023
Externally publishedYes

ASJC Scopus subject areas

  • Structural Biology
  • Molecular Biology

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