منابع مشابه
Discovery of Novel Glucagon Receptor Antagonists Using Combined Pharmacophore Modeling and Docking
Glucagon and the glucagon receptor are most important molecules control over blood glucose concentrations. These two molecules are very important to studies of type 2 diabetic patients. In literature, several classes of small molecule antagonists of the human glucagon receptor have been reported. Glucagon receptor antagonist could decrease hepatic glucose output and improve glucose control in d...
متن کاملDiscovery of Novel Glucagon Receptor Antagonists Using Combined Pharmacophore Modeling and Docking
Glucagon and the glucagon receptor are most important molecules control over blood glucose concentrations. These two molecules are very important to studies of type 2 diabetic patients. In literature, several classes of small molecule antagonists of the human glucagon receptor have been reported. Glucagon receptor antagonist could decrease hepatic glucose output and improve glucose control in d...
متن کاملDiscovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor.
A novel class of antagonists of the human glucagon receptor (hGCGR) has been discovered. Systematic modification of the lead compound identified substituents that were essential for activity and those that were amenable to further optimization. This SAR exploration resulted in the synthesis of 13, which exhibited good potency as an hGCGR functional antagonist (IC50 = 34 nM) and moderate bioavai...
متن کاملChemogenomic discovery of allosteric antagonists at the GPRC6A receptor.
GPRC6A is a Family C G protein-coupled receptor recently discovered and deorphanized by our group. This study integrates chemogenomic ligand inference, homology modeling, compound synthesis, and pharmacological mechanism-of-action studies to disclose two noticeable results of methodological and pharmacological character: (1) chemogenomic lead identification through the first, to our knowledge, ...
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ژورنال
عنوان ژورنال: Chemical Biology <html_ent glyph="@amp;" ascii="&"/> Drug Design
سال: 2006
ISSN: 1747-0277,1747-0285
DOI: 10.1111/j.1747-0285.2006.00376.x