Discovery of a Highly Potent, Nonabsorbable Apical Sodium-Dependent Bile Acid Transporter Inhibitor (GSK2330672) for Treatment of Type 2 Diabetes

The apical sodium-dependent bile acid transporter (ASBT) transports bile salts from the lumen of the gastrointestinal (GI) tract to the liver via the portal vein. Multiple pharmaceutical companies have exploited the physiological link between ASBT and hepatic cholesterol metabolism, which led to the...

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Veröffentlicht in:	Journal of medicinal chemistry 2013-06, Vol.56 (12), p.5094-5114
Hauptverfasser:	Wu, Yulin, Aquino, Christopher J, Cowan, David J, Anderson, Don L, Ambroso, Jeff L, Bishop, Michael J, Boros, Eric E, Chen, Lihong, Cunningham, Alan, Dobbins, Robert L, Feldman, Paul L, Harston, Lindsey T, Kaldor, Istvan W, Klein, Ryan, Liang, Xi, McIntyre, Maggie S, Merrill, Christine L, Patterson, Kristin M, Prescott, Judith S, Ray, John S, Roller, Shane G, Yao, Xiaozhou, Young, Andrew, Yuen, Josephine, Collins, Jon L
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Bile Acids and Salts - metabolism Diabetes Mellitus, Type 2 - drug therapy Dogs Drug Discovery Drug Stability HEK293 Cells Humans Hypoglycemic Agents - chemistry Hypoglycemic Agents - metabolism Hypoglycemic Agents - pharmacology Hypoglycemic Agents - therapeutic use Male Methylamines - chemistry Methylamines - metabolism Methylamines - pharmacology Methylamines - therapeutic use Mice Organic Anion Transporters, Sodium-Dependent - antagonists & inhibitors Rats Solubility Symporters - antagonists & inhibitors Thiazepines - chemistry Thiazepines - metabolism Thiazepines - pharmacology Thiazepines - therapeutic use
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