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J Mol Cell Cardiol. 2005 Jun;38(6):951-63. Epub 2005 Feb 19.

SUR, ABC proteins targeted by KATP channel openers.

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Biophysique Moléculaire and Cellulaire, CNRS UMR5090, CEA/DRDC, 17, Grenoble, France.


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.

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