NDLI: Recent updates on GPCR biased agonism.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Pupo, André S. Duarte, Diego A. Lima, Vanessa Teixeira, Larissa B. Parreiras-E-Silva, Lucas T. Costa-Neto, Claudio M.
Description	Author Affiliation: Pupo AS ( Department of Pharmacology, Instituto de Biociências, UNESP, Botucatu, SP, Brazil. Electronic address: aspupo@ibb.unesp.br.); Duarte DA ( Department of Biochemistry and Immunology, Faculty of Medicine at Ribeirão Preto, University of São Paulo, 14049-900 Ribeirão Preto, SP, Brazil.); Lima V ( Department of Pharmacology, Instituto de Biociências, UNESP, Botucatu, SP, Brazil); Teixeira LB ( Department of Biochemistry and Immunology, Faculty of Medicine at Ribeirão Preto, University of São Paulo, 14049-900 Ribeirão Preto, SP, Brazil.); Parreiras-E-Silva LT ( Department of Biochemistry and Immunology, Faculty of Medicine at Ribeirão Preto, University of São Paulo, 14049-900 Ribeirão Preto, SP, Brazil.); Costa-Neto CM ( 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.)
Abstract	G protein-coupled receptors (GPCRs) are the most important targets for drug discovery and not surprisingly â¼40% 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.
File Format	HTM / HTML
ISSN	10436618
Journal	Pharmacological Research
Volume Number	112
e-ISSN	10961186
Language	English
Publisher	Elsevier
Publisher Date	2016-10-01
Publisher Place	Netherlands
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Discipline Pharmacology
Content Type	Text
Resource Type	Article
Subject	Pharmacology

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