title: Recent updates on GPCR biased agonism.
abstract: G protein-coupled receptors (GPCRs) are the most important targets for drug discovery and not surprisingly ∼40% of all drugs currently in the market act on these receptors. Currently, one of the most active areas in GPCRs signaling is biased agonism, a phenomenon that occurs when a given ligand is able to preferentially activate one (or some) of the possible signaling pathways. In this review, we highlight the most recent findings about biased agonism, including an extension of this concept to intracellular signaling, allosterism, strategies for assessment and interpretation, and perspectives of therapeutic applications for biased agonists.
authors.affiliation: Department of Pharmacology, Instituto de Biociências, UNESP, Botucatu, SP, Brazil. Electronic address: aspupo@ibb.unesp.br.
authors.forename: André S
authors.initials: AS
authors.lastname: Pupo
authors.affiliation: Department of Biochemistry and Immunology, Faculty of Medicine at Ribeirão Preto, University of São Paulo, 14049-900 Ribeirão Preto, SP, Brazil.
authors.forename: Diego A
authors.initials: DA
authors.lastname: Duarte
authors.affiliation: Department of Pharmacology, Instituto de Biociências, UNESP, Botucatu, SP, Brazil; Department of Biochemistry and Immunology, Faculty of Medicine at Ribeirão Preto, University of São Paulo, 14049-900 Ribeirão Preto, SP, Brazil.
authors.forename: Vanessa
authors.initials: V
authors.lastname: Lima
authors.affiliation: Department of Biochemistry and Immunology, Faculty of Medicine at Ribeirão Preto, University of São Paulo, 14049-900 Ribeirão Preto, SP, Brazil.
authors.forename: Larissa B
authors.initials: LB
authors.lastname: Teixeira
authors.affiliation: Department of Biochemistry and Immunology, Faculty of Medicine at Ribeirão Preto, University of São Paulo, 14049-900 Ribeirão Preto, SP, Brazil.
authors.forename: Lucas T
authors.initials: LT
authors.lastname: Parreiras-E-Silva
authors.affiliation: Department of Biochemistry and Immunology, Faculty of Medicine at Ribeirão Preto, University of São Paulo, 14049-900 Ribeirão Preto, SP, Brazil. Electronic address: claudio@fmrp.usp.br.
authors.forename: Claudio M
authors.initials: CM
authors.lastname: Costa-Neto
mesh_terms: D000495:Allosteric Site; D000818:Animals; D001665:Binding Sites; D055808:Drug Discovery; D006801:Humans; D008024:Ligands; D058990:Molecular Targeted Therapy; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000378:metabolism; D015398:Signal Transduction
chemical_list: D008024:Ligands; D043562:Receptors, G-Protein-Coupled
keywords: 7TMR; Functional selectivity; GPCR