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1000 Titel
  • The Old and New Visions of Biased Agonism Through the Prism of Adenosine Receptor Signaling and Receptor/Receptor and Receptor/Protein Interactions
1000 Autor/in
  1. Franco, Rafael |
  2. Rivas‐Santisteban, Rafael |
  3. Reyes, Irene |
  4. Navarro, Gemma |
1000 Erscheinungsjahr 2021
1000 LeibnizOpen
1000 Publikationstyp
  1. Artikel |
1000 Online veröffentlicht
  • 2021-01-29
1000 Erschienen in
1000 Quellenangabe
  • 11:628601
1000 FRL-Sammlung
1000 Copyrightjahr
  • 2021
1000 Lizenz
1000 Verlagsversion
  • https://doi.org/10.3389/fphar.2020.628601 |
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7878529/ |
1000 Publikationsstatus
1000 Begutachtungsstatus
1000 Sprache der Publikation
1000 Abstract/Summary
  • 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.
1000 Sacherschließung
lokal adenylyl cyclase
lokal functional selectivity
lokal heteromer
lokal GPCR
lokal MAPK pathway
lokal tetramer
lokal cAMP
lokal receptor-receptor interactions
1000 Fächerklassifikation (DDC)
1000 Liste der Beteiligten
  1. https://frl.publisso.de/adhoc/uri/RnJhbmNvLCBSYWZhZWw=|https://frl.publisso.de/adhoc/uri/Uml2YXPigJBTYW50aXN0ZWJhbiwgUmFmYWVs|https://orcid.org/0000-0003-2077-2537|https://frl.publisso.de/adhoc/uri/TmF2YXJybywgR2VtbWE=
1000 Label
1000 Förderer
  1. Ministerio de Economía y Competitividad |
  2. European Regional Development Fund |
  3. Alzheimer's Association |
  4. Generalitat de Catalunya |
1000 Fördernummer
  1. SAF2017-84117-R; RTI2018-094204-B-I00
  2. -
  3. AARFD-17-503612
  4. #2017 SGR 1497
1000 Förderprogramm
  1. -
  2. -
  3. -
  4. -
1000 Dateien
1000 Förderung
  1. 1000 joinedFunding-child
    1000 Förderer Ministerio de Economía y Competitividad |
    1000 Förderprogramm -
    1000 Fördernummer SAF2017-84117-R; RTI2018-094204-B-I00
  2. 1000 joinedFunding-child
    1000 Förderer European Regional Development Fund |
    1000 Förderprogramm -
    1000 Fördernummer -
  3. 1000 joinedFunding-child
    1000 Förderer Alzheimer's Association |
    1000 Förderprogramm -
    1000 Fördernummer AARFD-17-503612
  4. 1000 joinedFunding-child
    1000 Förderer Generalitat de Catalunya |
    1000 Förderprogramm -
    1000 Fördernummer #2017 SGR 1497
1000 Objektart article
1000 Beschrieben durch
1000 @id frl:6425755.rdf
1000 Erstellt am 2021-02-19T14:38:12.561+0100
1000 Erstellt von 242
1000 beschreibt frl:6425755
1000 Bearbeitet von 122
1000 Zuletzt bearbeitet Mon Mar 01 09:14:09 CET 2021
1000 Objekt bearb. Mon Mar 01 09:13:26 CET 2021
1000 Vgl. frl:6425755
1000 Oai Id
  1. oai:frl.publisso.de:frl:6425755 |
1000 Sichtbarkeit Metadaten public
1000 Sichtbarkeit Daten public
1000 Gegenstand von

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