Patient-Level Multidimensional Response Phenotypes in Obesity-Associated Type 2 Diabetes: A 12-Month Real-World Cohort Study. [PDF]
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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.
Adam Szewczyk, Maciej Nałecz
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Differential interaction of glimepiride and glibenclamide with the β-cell sulfonylurea receptor I. Binding characteristics [PDF]
Biochimica Et Biophysica Acta - Biomembranes, 1994 Glimepiride is a novel sulfonylurea drug for treatment of non-insulin-dependent diabetes mellitus with higher blood sugar lowering efficacy in diabetic patients than glibenclamide raising the question whether this characteristics is in line with ...
Günter Müller, Werner Kramer
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Direct photoaffinity labeling of the putative sulfonylurea receptor in rat β-cell tumor membranes by [3H]glibenclamide [PDF]
FEBS Letters, 1988 The oral antidiabetic sulfonylurea [3H]glibenclamide specifically binds to plasma membranes from a rat β-cell tumor indicating a receptor for sulfonylureas in these membranes.
Werner Kramer
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Mechanism of KATP hyperactivity and sulfonylurea tolerance due to a diabetogenic mutation in L0 helix of sulfonylurea receptor 1 (ABCC8) [PDF]
FEBS Letters, 2011 Activating mutations in different domains of the ABCC8 gene-coded sulfonylurea receptor 1 (SUR1) cause neonatal diabetes. Here we show that a diabetogenic mutation in an unexplored helix preceding the ABC core of SUR1 dramatically increases open ...
Martine Vaxillaire, Andrey P Babenko
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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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Pancreatic and Extrapancreatic Sulfonylurea Receptors
Hormone and Metabolic Research, 1992The hypoglycemic effect of sulfonylureas and their analogues results from their binding to a high affinity site in the B-cell plasma membrane. This site seems to be a structural component of the ATP-sensitive K(+)-channel and represents the pancreatic sulfonylurea receptor.
U, Panten +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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