G protein-coupled receptors (GPCRs) help cells to respond to external stimuli. This study investigated how cholesterol influences the oxytocin receptor (OXTR). It looked at where exactly cholesterol binds to the receptor and how this influences the effect of other molecules that bind to the same receptor. With the help of computer simulations, several sites were found where cholesterol docks – depending on whether the receptor is currently active or inactive, the sites are distributed differently. Particularly important are certain areas on the outside and inside of the cell that transmit the signal. These findings help to better understand the effect of cholesterol on the OXTR and may be useful for future drug developments.
Link to publication
Marlow B, Vogel A, Kuenze G, Pankonin M, Reinhardt F, Stadler PF, Hildebrand PW, Meiler J. Cholesterol Allosteric Modulation of the Oxytocin Receptor. Biophys J. 2025 Apr 29:S0006-3495(25)00250-4. doi: 10.1016/j.bpj.2025.04.023. Epub ahead of print. PMID: 40308029.