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

Silvia Pittolo, Xavier Gómez-Santacana, Kay Eckelt, Xavier Rovira, James Dalton, Cyril Goudet, Jean Philippe Pin, Artur Llobet, Jesús Giraldo, Amadeu Llebaria, Pau Gorostiza

Research output: Contribution to journalArticleResearchpeer-review

78 Citations (Scopus)

Abstract

© 2015 Nature America, Inc. 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 mGlu 5 and enables the optical control of endogenous mGlu 5 receptors.
Original languageEnglish
Pages (from-to)813-815
JournalNature Chemical Biology
Volume10
Issue number10
DOIs
Publication statusPublished - 1 Oct 2014

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