Abstract
The sulfonylurea receptor SUR is an ATP binding cassette (ABC) protein of the ABCC/MRP family. Unlike other ABC proteins, it has no intrinsic transport function, neither active nor passive, but associates with the potassium channel proteins Kir6.1 or Kir6.2 to form the ATP-sensitive potassium (K(ATP)) channel. Within the channel complex SUR serves as a regulatory subunit which fine-tunes the gating of Kir6.x in response to alterations in cellular metabolism. It constitutes a major pharmaceutical target as it binds numerous drugs, K(ATP) channel openers and blockers, capable of up- or down-regulating channel activity. We here review current knowledge on the molecular basis of the interaction of classical K(ATP) channel openers (cromakalim, pinacidil, diazoxide) with SUR.
MeSH terms
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ATP-Binding Cassette Transporters / chemistry*
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ATP-Binding Cassette Transporters / metabolism
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ATP-Binding Cassette Transporters / physiology*
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Adenosine Triphosphate / chemistry
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Animals
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Cromakalim / pharmacology
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Cytoplasm / metabolism
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Diazoxide / pharmacology
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Down-Regulation
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Humans
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KATP Channels
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Models, Biological
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Pinacidil / pharmacology
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Potassium Channels / chemistry*
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Potassium Channels / physiology
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Potassium Channels, Inwardly Rectifying / chemistry*
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Potassium Channels, Inwardly Rectifying / metabolism
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Potassium Channels, Inwardly Rectifying / physiology*
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Protein Binding
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Protein Isoforms
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Protein Structure, Secondary
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Protein Structure, Tertiary
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Receptors, Drug / chemistry*
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Receptors, Drug / physiology*
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Sulfonylurea Receptors
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Up-Regulation
Substances
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ATP-Binding Cassette Transporters
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KATP Channels
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Kir6.2 channel
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Potassium Channels
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Potassium Channels, Inwardly Rectifying
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Protein Isoforms
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Receptors, Drug
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Sulfonylurea Receptors
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uK-ATP-1 potassium channel
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Cromakalim
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Pinacidil
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Adenosine Triphosphate
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Diazoxide