Results 221 to 230 of about 1,253,570 (258)

Epac2: a sulfonylurea receptor?

Biochemical Society Transactions, 2012
Sulfonylureas 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 ...
openaire   +2 more sources

A New Mesangial Triumvirate: Sulfonylureas, Their Receptors and Endosulfines

Nephron Experimental Nephrology, 2002
Although 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
openaire   +2 more sources

Expression of sulfonylurea receptors in rat taste buds

Acta Histochemica, 2011
To test the possibility that a fast-onset promoting agent repaglinide may initiate prandial insulin secretion through the mechanism of cephalic-phase insulin release, we explored the expression and distribution character of sulfonylurea receptors in rat taste buds. Twenty male Wistar rats aged 10 weeks old were killed after general anesthesia.
Dian-Xin, Liu, Xiao-Min, Liu, Li-Hong, Zhou, Xiao-Hong, Feng, Xiao-Juan, Zhang   +4 more
openaire   +2 more sources

Sulfonylurea receptors, ion channels, and fruit flies

Diabetes, 1988
Recent 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.
openaire   +2 more sources

Insulin Secretagogues, Sulfonylurea Receptors and KATP Channels

Current Pharmaceutical Design, 2005
ATP-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, A, Crane, W H, Vila-Carriles, A P, Babenko, L, Aguilar-Bryan   +4 more
openaire   +2 more sources

The KATP Channel and the Sulfonylurea Receptor

2001
ATP-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
openaire   +1 more source

Four novel splice variants of sulfonylurea receptor 1

American Journal of Physiology-Cell Physiology, 2002
ATP-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, Regina, Preisig-Müller, Ulrich, Russ, Anke, Piehl, Peter J, Hanley, John, Ray, Jürgen, Daut, Ulrich, Quast, Christian, Derst   +8 more
openaire   +2 more sources

Molecular docking of sulfonylureas to the SUR1 receptor

2021
Molecular 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
openaire   +1 more source

Regional distribution of sulfonylurea receptors in the brain of rodent and primate

Neuroscience, 1993
Glibenclamide, 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, E, Tremblay, H, Pollard, J, Moreau, Y, Ben-Ari   +4 more
openaire   +2 more sources

Characterization of sulfonylurea receptors in isolated human pancreatic islets

Journal of Cellular Biochemistry, 1998
Current information on pancreatic islet sulfonylurea receptors has been obtained with laboratory animal pancreatic beta cells or stable beta-cell lines. In the present study, we evaluated the properties of sulfonylurea receptors of human islets of Langherans, prepared by collagenase digestion and density-gradient purification.
GIANNACCINI, GINO, LUPI R., TRINCAVELLI, MARIA LETIZIA, NAVALESI R., BETTI, LAURA, MARCHETTI, PIERO, LUCACCHINI, ANTONIO, DEL GUERRA S., MARTINI, CLAUDIA   +8 more
openaire   +3 more sources