title: An allosteric modulator to control endogenous G protein-coupled receptors with light.
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.
authors.affiliation: 1] Institute for Bioengineering of Catalonia (IBEC), Barcelona, Spain. [2].
authors.forename: Silvia
authors.initials: S
authors.lastname: Pittolo
authors.affiliation: 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].
authors.forename: Xavier
authors.initials: X
authors.lastname: Gómez-Santacana
authors.affiliation: 1] Institute for Bioengineering of Catalonia (IBEC), Barcelona, Spain. [2] Network Biomedical Research Center on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), Zaragoza, Spain.
authors.forename: Kay
authors.initials: K
authors.lastname: Eckelt
authors.affiliation: 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.
authors.forename: Xavier
authors.initials: X
authors.lastname: Rovira
authors.affiliation: Institut de Neurociències and Unitat de Bioestadística, Universitat Autònoma de Barcelona, Bellaterra, Spain.
authors.forename: James
authors.initials: J
authors.lastname: Dalton
authors.affiliation: 1] Institut de Génomique Fonctionnelle, CNRS, UMR-5203, Université de Montpellier, Montpellier, France. [2] INSERM, U661, F-34000 Montpellier, France.
authors.forename: Cyril
authors.initials: C
authors.lastname: Goudet
authors.affiliation: 1] Institut de Génomique Fonctionnelle, CNRS, UMR-5203, Université de Montpellier, Montpellier, France. [2] INSERM, U661, F-34000 Montpellier, France.
authors.forename: Jean-Philippe
authors.initials: JP
authors.lastname: Pin
authors.affiliation: Bellvitge Biomedical Research Institute (IDIBELL), Barcelona, Spain.
authors.forename: Artur
authors.initials: A
authors.lastname: Llobet
authors.affiliation: Institut de Neurociències and Unitat de Bioestadística, Universitat Autònoma de Barcelona, Bellaterra, Spain.
authors.forename: Jesús
authors.initials: J
authors.lastname: Giraldo
authors.affiliation: 1] Institute for Advanced Chemistry of Catalonia (IQAC-CSIC), Barcelona, Spain. [2].
authors.forename: Amadeu
authors.initials: A
authors.lastname: Llebaria
authors.affiliation: 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].
authors.forename: Pau
authors.identifier: 0000000272685577
authors.initials: P
authors.lastname: Gorostiza
mesh_terms: D000494:Allosteric Regulation / Q000528:radiation effects; D000495:Allosteric Site; D000818:Animals; D000831:Animals, Newborn; D001253:Astrocytes / Q000166:cytology / Q000187:drug effects / Q000378:metabolism / Q000528:radiation effects; D001391:Azo Compounds / Q000737:chemistry*; D015870:Gene Expression; D057809:HEK293 Cells; D006801:Humans; D007814:Larva / Q000187:drug effects / Q000502:physiology / Q000528:radiation effects; D008027:Light; D055668:Photochemical Processes; D061251:Primary Cell Culture; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats; D064529:Receptor, Metabotropic Glutamate 5 / Q000819:agonists / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism*; D011994:Recombinant Proteins / Q000737:chemistry / Q000235:genetics; D014162:Transfection; D014981:Xenopus / Q000502:physiology
chemical_list: D001391:Azo Compounds; C578937:Grm5 protein, rat; D011725:Pyridines; D064529:Receptor, Metabotropic Glutamate 5; D011994:Recombinant Proteins; C009850:azobenzene