Plasma membrane cholesterol as a regulator of human and rodent P2X7 receptor activation and sensitization

Abstract

Background: P2X7 receptors are important in inflammation and immunity, but excessive activation results in cell death. Results: Facilitation of P2X7 receptor currents and dilation of the pore are enhanced by cholesterol depletion and reduced by cholesterol loading. Conclusion: Plasma membrane cholesterol destabilizes the open and dilated states of the receptor pore. Significance: Targeting of P2X7 to cholesterol-rich lipid rafts may protect cells from death.