Defining a binding pocket for sulfonylureas in ATP-sensitive potassium channels.

@article{VilaCarriles2007DefiningAB,
  title={Defining a binding pocket for sulfonylureas in ATP-sensitive potassium channels.},
  author={Wanda H. Vila-Carriles and Guiling Zhao and Joseph J. Bryan},
  journal={FASEB journal : official publication of the Federation of American Societies for Experimental Biology},
  year={2007},
  volume={21 1},
  pages={
          18-25
        }
}
Sulfonylurea receptors SUR1 and SUR2 are the regulatory subunits of K(ATP) channels. Their differential affinity for hypoglycemic sulfonylureas provides a basis for the selectivity of these compounds for different K(ATP) channel isoforms. Sulfonylureas have a 100- to 1000-fold greater affinity for SUR1 vs. SUR2. Structure-activity studies suggested a bipartite binding pocket. Chimeric SUR1 approximately SUR2 receptors have shown TMD2, the third bundle of transmembrane helices, to be part of an… CONTINUE READING
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