Discovery of GPCRs Sample Clauses

Discovery of GPCRs. The ability for cells to communicate with one another is essential for all aspects of life. Effective communication requires a means for converting information into a transmissible signal, a method for receiving the signal, and the ability to transfer information into the cell where it can be acted upon. Signaling molecules come in a diverse variety of forms and include neurotransmitters, hormones, lipids, peptides, proteins, and sensory molecules. Receptors for extracellular signals classically reside at the cell surface and upon ligand binding, change conformation, inducing intracellular signaling cascades. Of the vast array of surface receptors, G protein-coupled receptors (GPCRs) are the largest and most abundant family of receptors, contributing to nearly all physiological processes (Bjarnadottir et al. 2006). Since the purification and cloning of rhodopsin in 1983 (Nathans & Hogness, Cell, 1983) and the β2 adrenergic receptor in 1986 (Xxxxx et al. 1986), followed by the subsequent homology cloning of additional adrenergic (Kobilka et al. 1987; Xxxxxxxxx and Xxxxx 1990) and serotonin receptors (Fargin et al. 1988), more than 800 GPCRs have been identified (Fredriksson and Schioth 2005; Fredriksson et al. 2003; Munk et al. 2016). All GPCRs share a core structural homology, consisting of seven transmembrane (7TM) helices, an extracellular N-terminus (NT), and intracellular C-terminal domain (CT).