Jenine K Anday

Publications (2)10.96 Total impact

• Article: Ligand-binding architecture of human CB2 cannabinoid receptor: evidence for receptor subtype-specific binding motif and modeling GPCR activation.

  Ying Pei, Richard W Mercier, Jenine K Anday, Ganesh A Thakur, Alexander M Zvonok, Dow Hurst, Patricia H Reggio, David R Janero, Alexandros Makriyannis
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  ABSTRACT: The extensive physiological influence of transmission through the CB2 cannabinoid receptor makes this G protein-coupled receptor (GPCR) a promising therapeutic target for treating neuropathic pain, inflammation, and immune disorders. However, there is little direct structural information pertaining to either GPCR or CB2-receptor ligand recognition and activation. The present work helps characterize experimentally the ligand-binding interactions of the human CB2 (hCB2) receptor. This study illustrates how our overall experimental approach, "ligand-assisted protein structure" (LAPS), affords direct determination of the requirements for ligand binding to the hCB2 receptor and discrimination among the binding motifs for ligands that activate therapeutically relevant GPCRs.
  Chemistry & biology 12/2008; 15(11):1207-19. · 6.52 Impact Factor
• Article: Gene ancestry of the cannabinoid receptor family.

  Jenine K Anday, Richard W Mercier
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  ABSTRACT: Genome sequencing projects, and their available resources, have revealed two distinct genes encoding cannabinoid receptors, CB(1) and CB(2). Biochemical evidence in support of a third cannabinoid receptor includes signal transduction events and vasodilation in the vasculature of cannabinoid receptor knockout mice after exposure to the endogenous cannabinoid, anandamide. In addition, a nonpsychoactive ingredient in marijuana, abnormal cannabidiol, which does not activate the two characterized cannabinoid receptor homologues, has been shown to induce vasodilation in the endothelium. Our work distinguishes the biochemical differences by way of a phylogenetic analysis of cannabinoid receptors. Recently a putative orthologue to CB(1) and CB(2) has been identified in the urochordate, Ciona intestinalis, indicating the presence of cannabinoid receptors previous to the evolution of vertebrates. Moreover, the Ciona sequence shares equal identity to both cannabinoid paralogous sequences and no other GPCR sequence identified in an exhaustive database search is as similar. We propose that, although an alternate cannabinergic-activating pathway may be present, it does not include a GPCR (or other receptor type) phylogenetically related to the CB(1)/CB(2)Ciona lineage.
  Pharmacological Research 01/2006; 52(6):463-6. · 4.44 Impact Factor