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An allosteric modulator to control endogenous G protein-coupled receptors with light.
Pittolo, Silvia; Gómez-Santacana, Xavier; Eckelt, Kay; Rovira, Xavier; Dalton, James; Goudet, Cyril; Pin, Jean-Philippe; Llobet, Artur; Giraldo, Jesús; Llebaria, Amadeu; Gorostiza, Pau.
Afiliação
  • Pittolo S; 1] Institute for Bioengineering of Catalonia (IBEC), Barcelona, Spain. [2].
  • Gómez-Santacana X; 1] Institute for Bioengineering of Catalonia (IBEC), Barcelona, Spain. [2] Institute for Advanced Chemistry of Catalonia (IQAC-CSIC), Barcelona, Spain. [3] Institut de Neurociències and Unitat de Bioestadística, Universitat Autònoma de Barcelona, Bellaterra, Spain. [4].
  • Eckelt K; 1] Institute for Bioengineering of Catalonia (IBEC), Barcelona, Spain. [2] Network Biomedical Research Center on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), Zaragoza, Spain.
  • Rovira X; 1] Institut de Neurociències and Unitat de Bioestadística, Universitat Autònoma de Barcelona, Bellaterra, Spain. [2] Institut de Génomique Fonctionnelle, CNRS, UMR-5203, Université de Montpellier, Montpellier, France. [3] INSERM, U661, F-34000 Montpellier, France.
  • Dalton J; Institut de Neurociències and Unitat de Bioestadística, Universitat Autònoma de Barcelona, Bellaterra, Spain.
  • Goudet C; 1] Institut de Génomique Fonctionnelle, CNRS, UMR-5203, Université de Montpellier, Montpellier, France. [2] INSERM, U661, F-34000 Montpellier, France.
  • Pin JP; 1] Institut de Génomique Fonctionnelle, CNRS, UMR-5203, Université de Montpellier, Montpellier, France. [2] INSERM, U661, F-34000 Montpellier, France.
  • Llobet A; Bellvitge Biomedical Research Institute (IDIBELL), Barcelona, Spain.
  • Giraldo J; Institut de Neurociències and Unitat de Bioestadística, Universitat Autònoma de Barcelona, Bellaterra, Spain.
  • Llebaria A; 1] Institute for Advanced Chemistry of Catalonia (IQAC-CSIC), Barcelona, Spain. [2].
  • Gorostiza P; 1] Institute for Bioengineering of Catalonia (IBEC), Barcelona, Spain. [2] Network Biomedical Research Center on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), Zaragoza, Spain. [3] Catalan Institution for Research and Advanced Studies (ICREA), Barcelona, Spain. [4].
Nat Chem Biol ; 10(10): 813-5, 2014 Oct.
Article em En | MEDLINE | ID: mdl-25173999
ABSTRACT
Controlling drug activity with light offers the possibility of enhancing pharmacological selectivity with spatial and temporal regulation, thus enabling highly localized therapeutic effects and precise dosing patterns. Here we report on the development and characterization of what is to our knowledge the first photoswitchable allosteric modulator of a G protein-coupled receptor. Alloswitch-1 is selective for the metabotropic glutamate receptor mGlu5 and enables the optical control of endogenous mGlu5 receptors.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Piridinas / Compostos Azo / Receptor de Glutamato Metabotrópico 5 Idioma: En Ano de publicação: 2014 Tipo de documento: Article
Texto completo
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Piridinas / Compostos Azo / Receptor de Glutamato Metabotrópico 5 Idioma: En Ano de publicação: 2014 Tipo de documento: Article