TY - JOUR
T1 - An allosteric modulator to control endogenous G protein-coupled receptors with light
AU - Pittolo, Silvia
AU - Gómez-Santacana, Xavier
AU - Eckelt, Kay
AU - Rovira, Xavier
AU - Dalton, James
AU - Goudet, Cyril
AU - Pin, Jean Philippe
AU - Llobet, Artur
AU - Giraldo, Jesús
AU - Llebaria, Amadeu
AU - Gorostiza, Pau
PY - 2014/10/1
Y1 - 2014/10/1
N2 - © 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.
AB - © 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.
U2 - 10.1038/nchembio.1612
DO - 10.1038/nchembio.1612
M3 - Article
SN - 1552-4450
VL - 10
SP - 813
EP - 815
JO - Nature Chemical Biology
JF - Nature Chemical Biology
IS - 10
ER -