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SUR, ABC proteins targeted by KATP channel openers.
Christophe Moreau1, Anne-Lise Prost, Renaud Dérand
1Biophysique Moléculaire and Cellulaire, CNRS UMR5090, CEA/DRDC, 17, Grenoble, France.
Journal of Molecular and Cellular Cardiology
|May 25, 2005
Summary
The sulfonylurea receptor (SUR) regulates ATP-sensitive potassium (KATP) channels by interacting with Kir6.x proteins. This review details how KATP channel openers like cromakalim bind to SUR, impacting channel activity.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- The sulfonylurea receptor (SUR) is an ATP binding cassette (ABC) protein from the ABCC/MRP family.
- SUR lacks intrinsic transport function but forms the ATP-sensitive potassium (KATP) channel with Kir6.1 or Kir6.2.
- SUR acts as a regulatory subunit, modulating Kir6.x gating in response to metabolic changes.
Purpose of the Study:
- To review current knowledge on the molecular mechanisms underlying the interaction between classical KATP channel openers and SUR.
- To elucidate the role of SUR as a pharmaceutical target for modulating KATP channel activity.
Main Methods:
- Literature review of existing research on SUR and KATP channel pharmacology.
- Analysis of molecular interactions between SUR and KATP channel openers.
Main Results:
- SUR's interaction with KATP channel openers fine-tunes channel gating.
- Classical openers like cromakalim, pinacidil, and diazoxide bind to SUR.
- This binding modulates KATP channel activity, affecting cellular metabolism.
Conclusions:
- SUR is a critical regulatory component of KATP channels, essential for their function.
- Understanding SUR-ligand interactions is key for developing drugs that target KATP channels.
- SUR represents a significant pharmaceutical target for various therapeutic applications.