Abstract: P-glycoprotein (P-gp), as a member of the ABC transporter family, possesses the function of pumping drugs and toxicity out of cells when located on the plasma membrane. This process is regulated by various factors. P-gp is anchored to the cell plasma membrane through the combination effect of the ERM (ezrin/radixin/moesin) protein family. The lipid raft region plays an important role in the formulation of the P-gp transport function on plasma membrane. Caveolin-1 (Cav-1) is located on the caveolae as an important function protein on lipid raft, which combines with P-gp to regulate its structure and function. The article reviews the research progress of proteins involved in the location and function regulation of P-gp on plasma membrane, so as to provide a new direction for the research on the function and expression of P-gp on plasma membrane.