Target intelligence / Profile preview

ATP-sensitive potassium channel subunit SUR2 (SUR2)

Target
SUR2
Molecular classification
Ion channel subunit, ATP-binding cassette (ABC) transporter superfamily (ABC transporter, family C), Membrane-associated receptor, Regulatory subunit
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Overview

ATP-sensitive potassium channel subunit SUR2 is a regulatory subunit of KATP channels, part of the ATP-binding cassette (ABC) transporter C family. It exists mainly as two splice variants, SUR2A (predominantly cardiac) and SUR2B (predominantly smooth muscle), and co-assembles with Kir6.x (Kir6.1 or Kir6.2) pore-forming subunits to form functional KATP channels. SUR2 senses intracellular nucleotides (Mg-ADP, Mg-ATP) and pharmacologic ligands, linking cellular metabolic state to membrane excitability. SUR2-based KATP channels play fundamental roles in cardiovascular homeostasis, stress response (e.g., ischemic preconditioning), and muscle function. Targeting SUR2 is therapeutically relevant for cardiovascular disorders, certain metabolic and muscular conditions, and as a secondary target for some antidiabetic drugs.

Other names
Sulfonylurea receptor 2SUR2A (isoform)SUR2B (isoform)ABCC9 (gene symbol)
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Mechanism of action

Channel inhibition: Sulfonylureas bind SUR2 and inhibit KATP channel activity, leading to cell membrane depolarization and downstream effects Channel activation: KATP openers bind SUR2, increasing channel opening, hyperpolarizing membranes, and reducing cellular excitability

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Biological functions

Regulation of potassium ion (K⁺) flow across cell membranesCoupling of cellular metabolic state to membrane excitabilityControl of insulin secretion (indirectly, as part of KATP channel complexes)Modulation of vascular tone, cardiac protection, and muscle response
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Disease associations

Cardiovascular disease (e.g., cardiac ischemia, arrhythmias)Diabetes and metabolic syndromeIschemic preconditioning and tissue protectionMuscular diseases
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Safety considerations

Risk of hypotension and edema with KATP channel openersOff-target cardiovascular effects (especially for non-selective agents)Hypoglycemia risk less pronounced for SUR2 than SUR1, but possible with non-specific drugs
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Interacting drugs

Sulfonylureas (e.g., glibenclamide, tolbutamide; primarily act on related SUR1, but some activity at SUR2)

2 more in the full profile.

07

Biomarkers

ABCC9 (SUR2) expression levels (potential utility in research for cardiovascular and metabolic disorders; not standard clinical practice)

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