Scientists Uncover the Crystal Structures of Class B GPCRs and Expand Their Pharmaceutical Importance
GPCRs, a kind of membrane receptors, serve as extracellular signal sensors, including photons, ions, small organic molecules, even the whole proteins. About one third of known drugs use GPCRs to be active targets.
Currently, all the published GPCR structures come from class A. But recently the crystal structures of two Class B GPCRs—corticotropin releasing factor receptor 1 and Glucagon receptor–are revealed. According to the basic sequence and pharmacology, Class B GPCR belongs to the second category of four categories.
Corticotropin-releasing hormone is an effective media of endocrine, human’s behaviors and immune stress response. corticotropin releasing factor receptor 1 binds to the hormone. For Class A GPCRs, ligand is close to receptor’s extracellular boundary; while in the corticotropin releasing factor receptor 1, antagonists bind at a hydrophobic cavity in a V-shaped portion of the cytoplasmic receptor.
Under x-ray crystallography, researchers find that Glucagon receptor binds to Glucagon, which trigger the release of glucose from the liver. And there is a bigger ligand binding cavity than observed in Class A GPCRs. For this, Glucagon receptor is a promising drug target for Type 2 diabetes.
Nowadays, the targets of about 40% of all modern medicinal drugs are GPCRs. Creative BioMart is a world leading GPCR supplier. For additional information, please visit http://www.creativebiomart.net/researcharea_GPCR.htm.