6533b857fe1ef96bd12b5125
RESEARCH PRODUCT
Molecular modelling study of the role of cholesterol in the stimulation of the oxytocin receptor.
Jerzy CiarkowskiRajmund KaźmierkiewiczEwa PolitowskaFalk FahrenholzVolker Wiegandsubject
Models MolecularSequence Homology Amino AcidProtein ConformationMolecular Sequence DataBiologyCholecystokinin receptorOxytocin receptorGeneral Biochemistry Genetics and Molecular BiologySterolSterolsCholesterolBiochemistryReceptors OxytocinMutationBiophysicsMembrane fluidityHumansAmino Acid SequenceReceptorCholecystokininIntegral membrane proteinhormones hormone substitutes and hormone antagonistsCholecystokininG protein-coupled receptorProtein Bindingdescription
Cholesterol, an integral component of membranes in Eucaryota, is a modifier of membrane properties. In vivo studies have demonstrated that cholesterol can also modulate activities of some G protein-coupled receptors (GPCRs), which are integral membrane proteins. This can result either from an effect of cholesterol on the membrane fluidity or from specific interactions of the membrane cholesterol with the receptor, as recently demonstrated for the cholecystokinin type beta (CCKRbeta) or the oxytocin receptor (OTR). Using molecular modelling, we studied conformational preferences of cholesterol and several of its analogues. Subsequently, we simulated the distributions of their preferred conformations around the surface of OTR, CCKRbeta and a chimeric oxytocin/cholecystokinin receptor. Consequently, we suggest residues on the surface of OTR which are potentially significant in the OTR/cholesterol interaction.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2001-07-07 | Acta biochimica Polonica |