6533b82efe1ef96bd12927b0

RESEARCH PRODUCT

Non-genomic effects of progesterone on the signaling function of G protein-coupled receptors

Falk FahrenholzKatja BurgerGerald Gimpl

subject

Receptors Neuropeptidemedicine.medical_specialtyReceptors VasopressinTime FactorsBiophysicsStimulationCHO CellsCycloheximideBiologyNon-genomic effectCalcium signalBiochemistryCell Linechemistry.chemical_compoundStructure-Activity RelationshipSpecies SpecificityStructural BiologyInternal medicineCricetinaeProgesterone receptorGeneticsmedicineTumor Cells CulturedAnimalsHumansG protein-coupled receptorCycloheximideReceptorMolecular BiologyProgesteroneG protein-coupled receptorCalcium signalingProtein Synthesis InhibitorsDose-Response Relationship DrugCell BiologyLigand (biochemistry)Oxytocin receptorKineticsEndocrinologychemistryReceptors OxytocinAnisotropyCalciumReceptors CholecystokininSignal Transduction

description

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.

10.1016/s0014-5793(99)01668-3http://dx.doi.org/10.1016/S0014-5793(99)01668-3