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Sulfonylurea receptors and mechanism of sulfonylurea action
Experimental and Clinical Endocrinology & Diabetes, 2009Binding of hypoglycemic sulfonylureas and their analogues to the sulfonylurea receptor in the beta-cell plasma membrane mediates closure of the ATP-sensitive K+-channel (KATP-channel) and thereby stimulation of insulin release. The sulfonylurea receptor is a member of the traffic ATPase family with two intracellular nucleotide binding folds.
U, Panten +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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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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A New Mesangial Triumvirate: Sulfonylureas, Their Receptors and Endosulfines
Nephron Experimental Nephrology, 2002Although sulfonylureas have long been therapeutically utilized for their hypoglycemic properties in type 2 diabetic patients, there is a paucity of clinical or experimental data that suggests that this pharmacotherapeutic class confers a benefit on the course of diabetic renal disease.
Jerry, Yee, Balàzs, Szamosfalvi
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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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Sulfonylurea receptors, ion channels, and fruit flies
Diabetes, 1988Recent studies have identified a high-affinity receptor on the plasma membrane of the β-cell that is specific for all of the sulfonylureas. The most potent secondgeneration drugs, glyburide and glipizide, bind to the receptor and trigger insulin release at nanomolar concentrations.
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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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The KATP Channel and the Sulfonylurea Receptor
2001ATP-sensitive K+ channels (KAgp channels) were first described in cardiac myocytes (1) and were subsequently found in many other tissues including pancreatic 13-cells (25), skeletal muscle (6), smooth muscle (7), brain (8), pituitary (9), and kidney (10) and in mitochondria (11).
Susumu Seino, Takashi Miki, Hideki Yano
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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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