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Sulfonylurea receptor 2-containing ATP-sensitive potassium channel complex (SUR2-KATP) (SUR2-KATP channel)

Target
SUR2-KATP channel
Molecular classification
Ion channel, ATP-binding cassette (ABC) transporter family, Inward-rectifier potassium channel
01

Overview

SUR2-containing KATP channel complexes are hetero-octameric ion channels that serve as critical metabolic sensors, linking the cellular energetic state to membrane excitability [PubMed: 15131018]. These complexes consist of four pore-forming inward-rectifier potassium channel subunits (typically Kir6.1 or Kir6.2) and four regulatory sulfonylurea receptor 2 (SUR2) subunits, the latter encoded by the ABCC9 gene [UniProt: P59768]. SUR2 exists in two major isoforms: SUR2A, which is predominantly expressed in cardiac and skeletal muscle, and SUR2B, which is found in vascular and non-vascular smooth muscle [PubMed: 9159554]. These channels play a vital role in cardiovascular physiology, where they regulate vascular tone and provide cytoprotection during periods of metabolic stress or ischemia [PubMed: 11880371]. Pharmacologically, these complexes are the primary targets for potassium channel openers such as minoxidil and nicorandil, which induce vasodilation by promoting channel opening and subsequent membrane hyperpolarization [StatPearls: NBK539895]. Mutations in the subunits of these complexes are associated with clinical conditions including Cantu syndrome, characterized by hypertrichosis and cardiovascular abnormalities, and dilated cardiomyopathy [PubMed: 22703874].

Other names
ABCC9-containing KATP channelSUR2/Kir6.x complexATP-sensitive potassium channel (SUR2 type)
02

Mechanism of action

Potassium channel opening (activator) or Potassium channel blocking (inhibitor)

03

Biological functions

Vascular tone regulationCardiac cytoprotectionMetabolic sensingMembrane potential regulation
04

Disease associations

Cantu syndromeDilated cardiomyopathyHypertrichosisIschemic heart diseaseArterial hypertension
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Safety considerations

HypotensionReflex tachycardiaPeripheral edemaHypertrichosis
06

Interacting drugs

Minoxidil

5 more in the full profile.

07

Biomarkers

ABCC9 gene mutationKCNJ8 gene mutationKCNJ11 gene mutation

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