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

August 31st, 2014 by Silvia Pittolo

Nature Chemical Biology 10, 813 (2014). doi:10.1038/nchembio.1612

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

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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