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
  • Time Factors
  • Pain Threshold/drug effects
  • Allosteric Regulation/drug effects
  • Allosteric Regulation/radiation effects
  • Disease Models, Animal
  • Receptors, Metabotropic Glutamate/antagonists & inhibitors*
  • Receptors, Metabotropic Glutamate/metabolism
  • Dose-Response Relationship, Drug
  • Azo Compounds/chemistry
  • Azo Compounds/pharmacology*
  • Pyrrolidonecarboxylic Acid/analogs & derivatives*
  • Pyrrolidonecarboxylic Acid/chemistry
  • Pyrrolidonecarboxylic Acid/pharmacology
  • Animals
  • Mice, Inbred C57BL
  • Light*
  • Humans
  • Structure-Activity Relationship
  • Mice
  • Zebrafish/metabolism
  • HEK293 Cells
PubMed
27478159 Full text @ Cell Chem Biol
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
Figures
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Antibodies
Orthology
Engineered Foreign Genes
Mapping