Activity of L-alpha-amino acids at the promiscuous goldfish odorant receptor 5.24.
The goldfish odorant receptor 5.24 is a member of family C of G protein-coupled receptors and is closely related to the human receptor GPRC6A. Receptor 5.24 has previously been shown to have binding affinity for L-alpha-amino acids, especially the basic amino acids arginine and lysine. Here we report the agonist activities of the 20 proteinogenic L-alpha-amino acids, and L-ornithine and L-citrulline, measured in an intracellular calcium release assay in mammalian tsA cells. The results show that receptor 5.24 is broadly activated by 19 of the tested L-alpha-amino acids and displays a preference for basic amino acids.
Christiansen
Bolette
B
Department of Medicinal Chemistry, Danish University of Pharmaceutical Sciences, 2 Universitetsparken, DK-2100 Copenhagen, Denmark.
Wellendorph
Petrine
P
Bräuner-Osborne
Hans
H
D000596:Amino Acids / Q000494:pharmacology*; D000814:Aniline Compounds / Q000737:chemistry / Q000493:pharmacokinetics; D000818:Animals; D001667:Binding, Competitive; D002118:Calcium / Q000737:chemistry / Q000378:metabolism; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D005456:Fluorescent Dyes / Q000737:chemistry / Q000493:pharmacokinetics; D015870:Gene Expression; D006054:Goldfish / Q000378:metabolism*; D006801:Humans; D007424:Intracellular Fluid / Q000187:drug effects / Q000378:metabolism; D018035:Receptors, Odorant / Q000819:agonists* / Q000235:genetics / Q000502:physiology; D014162:Transfection; D014966:Xanthenes / Q000737:chemistry / Q000493:pharmacokinetics
D000596:Amino Acids; D000814:Aniline Compounds; C409648:Fluo 4; D005456:Fluorescent Dyes; D018035:Receptors, Odorant; D014966:Xanthenes; D002118:Calcium