PUBLICATION
OptoGluNAM4.1, a Photoswitchable Allosteric Antagonist for Real-Time Control of mGlu4 Receptor Activity
- Authors
- Rovira, X., Trapero, A., Pittolo, S., Zussy, C., Faucherre, A., Jopling, C., Giraldo, J., Pin, J.P., Gorostiza, P., Goudet, C., Llebaria, A.
- ID
- ZDB-PUB-160802-2
- Date
- 2016
- Source
- Cell chemical biology 23(8): 929-34 (Journal)
- Registered Authors
- Faucherre, Adele, Jopling, Chris
- Keywords
- none
- MeSH Terms
-
- Animals
- Structure-Activity Relationship
- Pyrrolidonecarboxylic Acid/analogs & derivatives*
- Pyrrolidonecarboxylic Acid/chemistry
- Pyrrolidonecarboxylic Acid/pharmacology
- Light*
- Allosteric Regulation/drug effects
- Allosteric Regulation/radiation effects
- Receptors, Metabotropic Glutamate/antagonists & inhibitors*
- Receptors, Metabotropic Glutamate/metabolism
- Humans
- Pain Threshold/drug effects
- Mice
- Azo Compounds/chemistry
- Azo Compounds/pharmacology*
- Mice, Inbred C57BL
- HEK293 Cells
- Disease Models, Animal
- Dose-Response Relationship, Drug
- Zebrafish/metabolism
- Time Factors
- PubMed
- 27478159 Full text @ Cell Chem Biol
Citation
Rovira, X., Trapero, A., Pittolo, S., Zussy, C., Faucherre, A., Jopling, C., Giraldo, J., Pin, J.P., Gorostiza, P., Goudet, C., Llebaria, A. (2016) OptoGluNAM4.1, a Photoswitchable Allosteric Antagonist for Real-Time Control of mGlu4 Receptor Activity. Cell chemical biology. 23(8):929-34.
Abstract
OptoGluNAM4.1, a negative allosteric modulator (NAM) of metabotropic glutamate receptor 4 (mGlu4) contains a reactive group that covalently binds to the receptor and a blue-light-activated, fast-relaxing azobenzene group that allows reversible receptor activity photocontrol in vitro and in vivo. OptoGluNAM4.1 induces light-dependent behavior in zebrafish and reverses the activity of the mGlu4 agonist LSP4-2022 in a mice model of chronic pain, defining a photopharmacological tool to better elucidate the physiological roles of the mGlu4 receptor in the nervous system.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping