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Neuron, 1996 We have cloned an isoform of the sulfonylurea receptor (SUR), designated SUR2. Coexpression of SUR2 and the inward rectifier K+ channel subunit Kir6.2 in COS1 cells reconstitutes the properties of KATP channels described in cardiac and skeletal muscle ...
Nobuya Inagaki +2 more
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Sulfonylurea receptors: ABC transporters that regulate ATP-sensitive K+ channels
Biochimica Et Biophysica Acta - Biomembranes, 1999 The association of sulfonylurea receptors (SURs) with KIR6.x subunits to form ATP-sensitive K+ channels presents perhaps the most unusual function known for members of the transport ATPase family.
Joseph Bryan +2 more
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Characterization and Significance of Sulfonylurea Receptors
Diabetes Care, 1990This study describes and characterizes a putative sulfonylurea receptor. The radioligand used was [3H]glipizide (9 Ci/mmol). The β-cell plasma membranes were derived from a transplantable rat insulinoma generated by subcutaneous injection of RINm5F cells and purified by ultracentrifugation on a 15–55% sucrose gradient. Specific binding of [3H]glipizide
L, Siconolfi-Baez +2 more
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The Mitochondrial Sulfonylurea Receptor: Identification and Characterization
Biochemical and Biophysical Research Communications, 1997Biochemical identification of mitochondrial sulfonylurea receptors has been carried out through binding studies performed with [3H]glibenclamide. The presence of a single class of low affinity binding sites for glibenclamide in the inner mitochondrial membrane has been found, with a KD of 360 +/- 48 nM and BMAX of 48 +/- 7 pmoles/mg in beef heart ...
A, Szewczyk +3 more
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Modification of the Mitochondrial Sulfonylurea Receptor by Thiol Reagents
Biochemical and Biophysical Research Communications, 1999The purpose of this study was to investigate the effects exerted by thiol-modifying reagents on themitochondrial sulfonylurea receptor. The thiol-oxidizing agents (timerosal and 5, 5'-dithio-bis(2-nitrobenzoic acid)) were found to produce a large inhibition (70% to 80%) of specific binding of [(3)H]glibenclamide to the beef heart mitochondrial membrane.
A, Szewczyk +3 more
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Epac2: a sulfonylurea receptor?
Biochemical Society Transactions, 2012Sulfonylureas are widely used oral drugs in the treatment of diabetes mellitus. They function by the inhibition of ATP-sensitive K+ channels in pancreatic β-cells, which are thus considered the ‘classical’ sulfonylurea receptor. Next to the ATP-sensitive K+ channels, additional sulfonylurea-interacting proteins were identified, which might contribute ...
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Insulin Secretagogues, Sulfonylurea Receptors and KATP Channels
Current Pharmaceutical Design, 2005ATP-sensitive K+ channels, termed K(ATP) channels, provide a link between cellular metabolism and membrane electrical activity in a variety of tissues. Channel isoforms have been identified and are targets for compounds that both stimulate and inhibit their activity resulting in membrane hyperpolarization and depolarization, respectively.
J, Bryan +4 more
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Four novel splice variants of sulfonylurea receptor 1
American Journal of Physiology-Cell Physiology, 2002ATP-sensitive K+ (KATP) channels are composed of pore-forming Kir6.x subunits and regulatory sulfonylurea receptor (SUR) subunits. SURs are ATP-binding cassette proteins with two nucleotide-binding folds (NBFs) and binding sites for sulfonylureas, like glibenclamide, and for channel openers.
Annette, Hambrock +8 more
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Regional distribution of sulfonylurea receptors in the brain of rodent and primate
Neuroscience, 1993Glibenclamide, one of the most potent antidiabetic sulfonylureas, inhibits the activity of ATP-sensitive K+ channels in the pancreas as well as in the brain through its binding to specific receptors. Quantitative autoradiography was used to localize such receptors in the brain of rat, mouse, guinea-pig and marmoset, using [3H]glibenclamide as ...
S, Zini +4 more
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Molecular docking of sulfonylureas to the SUR1 receptor
2021Molecular docking is a powerful tool in drug discovery. It intuitively presents invisible bonds and atoms in a visible way so that it makes drug discovery more efficient and affordable. In recent years, it has become one of the most commonly used methods in drug discovery. Drug design has shifted from a tool purely focusing on molecular interactions to
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