Crystal structure of the beta2-adrenergic receptor protein, the first known structure of a human G protein-coupled receptor. (Source: The Stevens Laboratory, The Scripps Research Institute)
A detailed, three-dimensional look at beta blockers’ molecular target—the beta2-adrenergic receptor—was unveiled by researchers supported by the National Institutes of Health. The beta2-adrenergic receptor is part of a family of proteins called G protein-coupled receptors (GPCRs) that control critical bodily functions, several of our senses, and the action of many pharmaceuticals. To solve the new structure, the researchers overcame some scientific obstacles. Many of these difficulties arise because GPCRs are membrane proteins—some of the trickiest molecules to capture in three-dimensional detail because they resist forming crystals, which are needed for structure determination. The research is published online in Science Express.
This article was published in Drug Discovery & Development magazine: Vol. 10, No. 11, November, 2007, pp. 34.
Filed Under: Drug Discovery