A5022310266- Photochromic and Fluorescence Chemistry
- Photoreceptor and optogenetics research
- Receptor Mechanisms and Signaling
- Molecular Sensors and Ion Detection
- bioluminescence and chemiluminescence research
- Neuroscience and Neuropharmacology Research
- Click Chemistry and Applications
- Enzyme Catalysis and Immobilization
- Retinal Development and Disorders
Institute for Bioengineering of Catalonia
2014-2020
Universitat de Barcelona
2020
Institute of Science and Technology
2019
Institut Català d'Investigació Química
2014
Abstract Light-regulated drugs allow remotely photoswitching biological activity and enable plausible therapies based on small molecules. However, only freely diffusible photochromic ligands have been shown to work directly in endogenous receptors methods for covalent attachment depend genetic manipulation. Here we introduce a chemical strategy covalently conjugate photoswitch the of proteins demonstrate its application kainate receptor channel GluK1. The approach is photoswitchable...
Background and Purpose Anion‐selective Cys‐loop receptors (GABA glycine receptors) provide the main inhibitory drive in CNS. Both types of receptor operate via chloride‐selective ion channels, though with different kinetics, pharmacological profiles, localization. Disequilibrium their function leads to a variety disorders, which are often treated allosteric modulators. The few available GABA channel blockers effectively suppress currents neurons, but systemic administration is highly toxic....
A lipase was immobilized on transparent agarose microspheres and genetically engineered to specifically anchor photochromic molecules into its catalytic site. Several combinations of azobenzene spiropyran groups were conjugated cysteines introduced at different positions near the active center. Light modulated properties resulting solid bioconjugates, such modulation depended both nature compound anchoring position. Covalent derivatives residue 295 2 from Bacillus thermocathenolatus...
ABSTRACT Glycine receptors (GlyRs) are indispensable to maintain excitatory/inhibitory balance in neuronal circuits controlling reflex and rhythmic motor behaviors. Here we have developed Glyght, the first GlyR ligand controlled with light. It is selective over other cys-loop receptors, active vivo , displays an allosteric mechanism of action. The photomanipulation glycinergic neurotransmission opens new avenues understand inhibitory intact animals, develop drug-based phototherapies.