Non-genomic effects of progesterone on the signaling function of G protein-coupled receptors.
Progesterone at concentrations between 10 microM and 200 microM affected the calcium signaling evoked by ligand stimulation of G protein-coupled receptors expressed in several cell lines. At 160 microM progesterone the signaling of all receptors was completely abolished. The effect of progesterone was fast, reversible and was not prevented by cycloheximide indicating its non-genomic nature. Overall, the action of progesterone was more cell type-specific than receptor-specific. Our results are in contrast to a recent report [Grazzini, E., Guillon, G., Mouillac, B. and Zingg, H.H. (1998) Nature 392, 509-512] in which a direct high-affinity interaction between the oxytocin receptor and progesterone was suggested.
Burger
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Johannes Gutenberg-Universität Mainz, Institut für Biochemie, Becherweg 30, 55099, Mainz, Germany.
Fahrenholz
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Gimpl
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D000818:Animals; D016466:CHO Cells; D002118:Calcium / Q000378:metabolism; D002460:Cell Line; D006224:Cricetinae; D003513:Cycloheximide / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007700:Kinetics; D011374:Progesterone / Q000494:pharmacology*; D011500:Protein Synthesis Inhibitors / Q000494:pharmacology; D011949:Receptors, Cholecystokinin / Q000187:drug effects; D018013:Receptors, Neuropeptide / Q000187:drug effects*; D018045:Receptors, Oxytocin / Q000187:drug effects; D017483:Receptors, Vasopressin / Q000187:drug effects; D015398:Signal Transduction / Q000187:drug effects*; D013045:Species Specificity; D013329:Structure-Activity Relationship; D013997:Time Factors; D014407:Tumor Cells, Cultured
D011500:Protein Synthesis Inhibitors; D011949:Receptors, Cholecystokinin; D018013:Receptors, Neuropeptide; D018045:Receptors, Oxytocin; D017483:Receptors, Vasopressin; D011374:Progesterone; D003513:Cycloheximide; D002118:Calcium