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- Title
An allosteric modulator to control endogenous G protein-coupled receptors with light.
- Authors
Pittolo, Silvia; Gómez-Santacana, Xavier; Eckelt, Kay; Rovira, Xavier; Dalton, James; Goudet, Cyril; Pin, Jean-Philippe; Llobet, Artur; Giraldo, Jesús; Llebaria, Amadeu; Gorostiza, Pau
- 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.
- Subjects
G protein coupled receptors; ALLOSTERIC regulation; DRUG activation; PHARMACOLOGY; GLUTAMATE receptors
- Publication
Nature Chemical Biology, 2014, Vol 10, Issue 10, p813
- ISSN
1552-4450
- Publication type
Article
- DOI
10.1038/nchembio.1612