Molecular modelling study of the role of cholesterol in the stimulation of the oxytocin receptor.

• Authors: Ewa Politowska , Rajmund Kaźmierkiewicz , Volker Wiegand , Falk Fahrenholz , Jerzy Ciarkowski
• Languages of publication: EN

Abstracts

EN

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 β (CCKRβ) 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, CCKRβ and a chimeric oxytocin/cholecystokinin receptor. Consequently, we suggest residues on the surface of OTR which are potentially significant in the OTR/cholesterol interaction.

Keywords

EN

cholesterol; AutoDock 2.4; cholecystokinin receptor type β; oxytocin receptor; GPCR; sterols

• Publisher: Polish Biochemical Society
• Journal: Acta Biochimica Polonica
• Year: 2001
• Volume: 48
• Issue: 1
• Pages: 83-93

Dates

published

2001

received

2000-11-2

revised

2001-02-1

accepted

2001-02-20

Contributors

author

Ewa Politowska

• Faculty of Chemistry, University of Gdańsk, Gdańsk, Poland

author

Rajmund Kaźmierkiewicz

• Faculty of Chemistry, University of Gdańsk, Gdańsk, Poland

author

Volker Wiegand

• Institute of Biochemistry, Johannes-Gutenberg-University, Mainz, Germany

author

Falk Fahrenholz

• Institute of Biochemistry, Johannes-Gutenberg-University, Mainz, Germany

author

Jerzy Ciarkowski

• Faculty of Chemistry, University of Gdańsk, Gdańsk, Poland

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