P-glycoprotein

P-glycoprotein (also known as permeability glycoprotein, or P-gp) is a well-characterized protein of the ATP-binding cassette transporter superfamily. It is an important component of the cell membrane that contributes to the multidrug resistance of cells, often by extruding drugs out of the cell.

Structure

P-glycoprotein is a 170 kDa protein that has two homologous halves, each with six transmembrane segments and an ATP-binding cassette. It is encoded by the MDR1 gene in humans.

Function

P-glycoprotein plays a crucial role in limiting drug absorption and distribution, as well as facilitating the excretion of drugs in the urine and bile. It is also involved in the transport of various endogenous substances, such as steroids and lipids, across the cell membrane.

Clinical significance

P-glycoprotein is often overexpressed in cancer cells, leading to multidrug resistance. Inhibition of P-glycoprotein can increase the absorption of many drugs and improve their bioavailability.

See also

• ATP-binding cassette transporter
• Multidrug resistance
• MDR1 gene

References

P-glycoprotein Resources
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