An allosteric modulator to control endogenous G protein-coupled receptors with light

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 knowledg...

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Detalles Bibliográficos
Autores: Pittolo, Silvia, Gómez-Santacana, Xavier, Eckelt, Kay, Rovira, Xavier, Dalton, James, Goudet, Cyril, Pin, Jean-Philippe, Llobet, Artur, Giraldo, Jesús, Llebaria, Amadeu, Gorostiza, Pau
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2014
País:España
Institución:Consejo Superior de Investigaciones Científicas (CSIC)
Repositorio:DIGITAL.CSIC. Repositorio Institucional del CSIC
OAI Identifier:oai:digital.csic.es:10261/415436
Acceso en línea:http://hdl.handle.net/10261/415436
https://api.elsevier.com/content/abstract/scopus_id/84922058988
Access Level:acceso abierto
Palabra clave:Pharmacological selectivity
Allosteric modulators
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Descripción
Sumario: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.