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Title: The old and new visions of biased agonism through the prism of adenosine receptor signaling and receptor/receptor and receptor/protein interactions
Author: Franco Fernández, Rafael
Rivas‐Santisteban, Rafael
Reyes Resina, Irene
Navarro Brugal, Gemma
Keywords: Desenvolupament de medicaments
Receptors de medicaments
Drug development
Drug receptors
Issue Date: 29-Jan-2021
Publisher: Frontiers Media
Abstract: Biased signaling is a concept that has arisen in the G protein-coupled receptor (GCPR) research field, and holds promise for the development of new drug development strategies. It consists of different signaling outputs depending on the agonist's chemical structure. Here we review the most accepted mechanisms for explaining biased agonism, namely the induced fit hypothesis and the key/lock hypothesis, but we also consider how bias can be produced by a given agonist. In fact, different signaling outputs may originate at a given receptor when activated by, for instance, the endogenous agonist. We take advantage of results obtained with adenosine receptors to explain how such mechanism of functional selectivity depends on the context, being receptor-receptor interactions (heteromerization) one of the most relevant and most studied mechanisms for mammalian homeostasis. Considering all the possible mechanisms underlying functional selectivity is essential to optimize the selection of biased agonists in the design of drugs targeting GPCRs.
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It is part of: Frontiers in Pharmacology, 2021, vol. 11
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ISSN: 1663-9812
Appears in Collections:Articles publicats en revistes (Bioquímica i Biomedicina Molecular)
Articles publicats en revistes (Bioquímica i Fisiologia)

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