PT - JOURNAL ARTICLE AU - Roger K. Sunahara AU - Paul A. Insel TI - The Molecular Pharmacology of G Protein Signaling Then and Now: A Tribute to Alfred G. Gilman AID - 10.1124/mol.116.104216 DP - 2016 May 01 TA - Molecular Pharmacology PG - 585--592 VI - 89 IP - 5 4099 - http://molpharm.aspetjournals.org/content/89/5/585.short 4100 - http://molpharm.aspetjournals.org/content/89/5/585.full SO - Mol Pharmacol2016 May 01; 89 AB - The recent, unfortunate death of Alfred G. (“Al”) Gilman, M.D., Ph.D., represents a sad signpost for an era spanning over 40 years 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 underlies affinity and efficacy, two of the most important features of drug action, which represent the latest chapter in the saga that Al Gilman’s work helped launch.