Scientists Unveil Structure of Molecular Target of Many Drugs

More than 40 years after beta blockers were first used clinically, scientists can finally get a close-up look at the drugs' molecular target-the ß2-adrenergic receptor. The work is particularly exciting because it offers the first glimpse into an important, but scientifically elusive family of human proteins called G protein-coupled receptors (GPCRs). Because GPCRs control critical bodily functions, several of our senses, and the action of about half of today's pharmaceuticals, the research promises not only to speed the discovery of new and improved drugs, but also to broaden our understanding of human health and disease. Published online in the October 25 issue of Science Express, the research was supported by two major initiatives of the National Institutes of Health-the Roadmap and the Protein Structure Initiative (PSI), which is led by the National Institute of General Medical Sciences. Additional funding came from the National Institute of Neurological Disorders and Stroke.