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Nobel Prize Winners Experience GPCR-Mediated Adrenaline Rush

You can imagine that accepting a Nobel Prize in Chemistry would provide an amazing sense of pride and accomplishment, a true adrenaline rush. But would that experience feel any different if the very research you were being recognized for was in part responsible for our understanding of how such feelings and emotions arise from biochemical signals, such as those transmitted via G-Protein Coupled Receptors (GPCRs)? You’d have to ask Robert J. Lefkowitz and Brian K. Kobilka to know for sure. This past December, Lefkowitz (Duke University) and Kobilka (Stanford University) were awarded the 2012 Nobel Prize for Chemistry for their contributions to unfolding the structure and function of GPCRs.

GPCRs belong to a very large family of proteins involved in the transmission of intra-cellular signals following the binding of ligands (including hormones, neurotransmitters and cytokines) to their extra-cellular domains and the recruitment of intra-cellular GTP in order to activate or inhibit enzymes such as adenylate cyclase or phospholipase C. Several cell surface receptors were characterized by Lefkowitz’s laboratory using radioactively labeled hormones, notably the β2-adrenergic receptor and its ligand, adrenaline. This receptor was later isolated from cell membranes, sequenced, and its structure elucidated by Kobilka using techniques almost solely used by chemists at the time1,2,3. They realized that the β2-adrenergic receptor had a very similar structure to rhodopsin, an ocular light-detecting receptor. Using the premise that other receptors with identical organization may therefore exist, Lefkowitz, Kobilka and others managed to identify more than a thousand GPCRs implicated in almost every physiological process from metabolism to cardiac rhythm and pain tolerance4. Their efforts have enabled a much deeper understanding of cellular biology and signal transduction, and GPCRs continue to have a major impact in the world of drug discovery, serving as the targets for countless pharmacological therapeutics.

Today, a great number of orphan GPCRs remain to be fully characterized. Enzo Life Sciences offers a wide range of products for GPCR characterization and screening, including calcium and cAMP detection kits, Screen-Well® compound libraries consisting of GPCR agonists and antagonists, as well as worry-free antibody sets for GPCRs and GPCR signaling (see table below).


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