Mapping Cannabinoid 1 Receptor Allosteric Site(s): Critical Molecular Determinant and Signaling Profile of GAT100, a Novel, Potent, and Irreversibly Binding Probe

Robert B. Laprairie, Abhijit R. Kulkarni, Pushkar M. Kulkarni, Dow P. Hurst, Diane Lynch, Patricia H. Reggio, David R. Janero, Roger G. Pertwee, Lesley A. Stevenson, Melanie E.M. Kelly, Eileen M. Denovan-Wright, Ganesh A. Thakur

Research output: Contribution to journalArticlepeer-review

32 Citations (Scopus)
Original languageEnglish
Pages (from-to)776-798
Number of pages23
JournalACS Chemical Neuroscience
Volume7
Issue number6
DOIs
Publication statusPublished - Jun 15 2016

ASJC Scopus Subject Areas

  • Cognitive Neuroscience
  • Biochemistry
  • Physiology
  • Cell Biology

Keywords

  • 7-transmembrane receptor
  • Allosteric covalent probe
  • G protein-coupled receptors
  • allosteric site
  • biased signaling
  • binding domain
  • cannabinoid 1 receptor
  • cysteine
  • functional selectivity
  • homology modeling
  • isothiocyanate
  • ligand bias
  • ligand-binding motif
  • negative allosteric modulator
  • signal transduction
  • therapeutics discovery

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