TY - JOUR T1 - The molecular pharmacology of G protein signaling then and now: A tribute to Alfred G. Gilman JF - Molecular Pharmacology JO - Mol Pharmacol DO - 10.1124/mol.116.104216 SP - mol.116.104216 AU - Roger K. Sunahara AU - Paul A. Insel Y1 - 2016/01/01 UR - http://molpharm.aspetjournals.org/content/early/2016/03/15/mol.116.104216.abstract N2 - The recent, unfortunate death of Alfred G. ("Al") Gilman, M.D./Ph.D., represents a sad signpost for a 40+ year era in molecular pharmacology. Gilman’s discoveries, influence and persona were dominant forces in research and training in pharmacology. Here, we review the progression of ideas and knowledge that spawned early work by Gilman and collaborators (among them, one of the authors) and later efforts (including those of the other author) that have recently yielded a comprehensive and precise structural understanding of fundamental topics in pharmacology: the binding of ligands to G-protein-coupled receptors (GPCRs) and the interaction of GPCRs with heterotrimeric G proteins and effector molecules. Those data provide new and important insights into the molecular basis that underlie affinity and efficacy, two of the most important features of drug action, and as such, represent the latest chapter in the saga that Al Gilman's work helped launch. ER -