Topic: Bioluminescence Resonance Energy Transfer

Photopharmacology is an emerging approach that allows the spatiotemporal control of receptor function using photodrugs and offers superior tissue specificity and reduced off-target effects. Previously, we successfully demonstrated the blockade the adenosine A2A receptor (A2AR) in mouse brain using MRS7145, a photocaged derivative of the selective A2AR antagonist SCH442416.1 Here, we explore the use of bioluminescence resonance energy transfer (BRET) to photouncage MRS7145 in vitro and in vivo. First, we demonstrated the effective release of SCH442416 by BRET uncaging or bioluminolysis of MRS71

Epilepsy is a frequent neurological disorder affecting about 1% of the general population, with 30% of patients that are resistant to antiepileptic drugs. In the last decade, optogenetics has emerged as an efficient antiepileptic strategy, although the difficulty of illuminating multiple and deep areas of the brain still poses translational challenges. In this scenario, the search of alternative light sources is strongly needed. Here, we developed a closed-loop chemo-optogenetic nanomachine, named pH-sensitive inhibitory luminopsin (pHIL), composed of a luciferase-based light generator, a fluo