Deciphering the specific role of G(?i/o) isoforms: functional selective oxytocin ligands and somatostatin SST5 receptor mutants. (Articolo in rivista)

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  • Deciphering the specific role of G(?i/o) isoforms: functional selective oxytocin ligands and somatostatin SST5 receptor mutants. (Articolo in rivista) (literal)
Anno
  • 2013-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1042/BST20120306 (literal)
Alternative label
  • Busnelli M1, Peverelli E2, Mantovani G2, Spada A2, Chini B1. (2013)
    Deciphering the specific role of G(?i/o) isoforms: functional selective oxytocin ligands and somatostatin SST5 receptor mutants.
    in Biochemical Society transactions
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Busnelli M1, Peverelli E2, Mantovani G2, Spada A2, Chini B1. (literal)
Pagina inizio
  • 166 (literal)
Pagina fine
  • 171 (literal)
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  • 41 (literal)
Rivista
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  • 6 (literal)
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  • 1 (literal)
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  • 1CNR, Institute of Neuroscience, Via Vanvitelli 32, 20129, Milan, Italy, and 2Endocrinology and Diabetology Unit, Department of Clinical Sciences and Community Health, University of Milan, Fondazione IRCCS Ca'Granda Policlinico, Via Francesco Sforza 35, 20122 Milan, Italy (literal)
Titolo
  • Deciphering the specific role of G(?i/o) isoforms: functional selective oxytocin ligands and somatostatin SST5 receptor mutants. (literal)
Abstract
  • Receptor coupling to different G-proteins and ?-arrestins has been described for a number of GPCRs (G-protein-coupled receptors), suggesting a multi-state model of receptor activation in which each receptor can assume a number of different active conformations, each capable of promoting the coupling to a specific effector. Consistently, functional-selective ligands and biased agonists have been described to be able to induce and/or stabilize only a subset of specific active conformations. Furthermore, GPCR mutants deficient in selective coupling have been reported. Functional selective ligands and receptor mutants thus constitute unique tools to dissect the specific roles of different effectors, in particular among the Gi/o family. In the present mini-review, we focus on (i) the identification of functional selective OXT (oxytocin)-derived peptides capable of activating single Gi/o isoforms, namely Gi1 or Gi3; and (ii) the characterization of an SS (somatostatin) receptor SST5 mutant selectively impaired in its GoA coupling. These analogues and receptor mutants represent unique tools for examining the contribution of Gi/o isoforms in complex biological responses and open the way for the development of drugs with peculiar selectivity profiles. (literal)
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