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Photocontrol of Endogenous Glycine Receptors In Vivo.
Cell Chemical Biology ( IF 8.6 ) Pub Date : 2020-08-25 , DOI: 10.1016/j.chembiol.2020.08.005
Alexandre M J Gomila 1 , Karin Rustler 2 , Galyna Maleeva 3 , Alba Nin-Hill 4 , Daniel Wutz 2 , Antoni Bautista-Barrufet 1 , Xavier Rovira 1 , Miquel Bosch 1 , Elvira Mukhametova 5 , Elena Petukhova 6 , Daria Ponomareva 6 , Marat Mukhamedyarov 6 , Franck Peiretti 7 , Mercedes Alfonso-Prieto 8 , Carme Rovira 9 , Burkhard König 2 , Piotr Bregestovski 10 , Pau Gorostiza 11
Affiliation  

Glycine receptors (GlyRs) are indispensable for maintaining excitatory/inhibitory balance in neuronal circuits that control reflexes and rhythmic motor behaviors. Here we have developed Glyght, a GlyR ligand controlled with light. It is selective over other Cys-loop receptors, is active in vivo, and displays an allosteric mechanism of action. The photomanipulation of glycinergic neurotransmission opens new avenues to understanding inhibitory circuits in intact animals and to developing drug-based phototherapies.



中文翻译:

体内内源性甘氨酸受体的光控。

甘氨酸受体(GlyRs)对于维持神经元回路中控制反射和节律性运动行为的兴奋性/抑制性平衡是必不可少的。在这里,我们开发了Glyght,一种受光控制的GlyR配体。它对其他半胱氨酸环受体具有选择性,在体内具有活性,并表现出变构作用机制。甘氨酸能神经传递的光操纵为了解完整动物的抑制回路和开发基于药物的光疗开辟了新途径。

更新日期:2020-08-25
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