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Deekshitha H S, K. Natarajan, Vineeth Chandy



The review is done on how P-glycoprotein recognizes various substrates and plays a key role in cancer. Chemotherapy is used for cancer treatment but multidrug resistance of cancerous cell is the major obstacle in therapy and also an important aspect which causes failure in the treatment by effluxion of a xenobiotic on the plasma membrane. In humans, P-glycoprotein is important transmembrane transporter. It is located on the apical surface of the intestine, epithelial cells, bile canaliculi, renal tubular cells, placenta and found to show overexpression of tumour cells. P-glycoprotein is a protein encoded by the MDR1 gene and it causes alteration by competition inhibition. Clinical studies prove that P-glycoprotein inhibitors decrease the clearance rate of anticancer agents. The protein excretes cytotoxic drugs into the gastrointestinal tract, bile, and urine which cause failure in the cancer treatment, and also take part in the function of the blood brain barrier. P-gp substrates vary widely in their structure and practicality range from small molecules to large molecules. Substrate specificity is important to target tumour cells, but it is altered by the amino acid substitutions of P- glycoprotein found dispersed throughout the molecule. Substrate amphipathy decides whether it can be intercalated into the lipid bilayer of the membrane. Further studies are warranted to justify the physiological function and pharmacological role of P-gp / MDR1 in cancer. Further development of potent P-glycoprotein modulators should decrease the impact on drug interaction and result in increased therapeutic specificity and efficacy.

Keywords: ABC transporter, MDR1, P-glycoprotein, Resistance, +Transmembrane

Cite this Article

Deekshitha H.S., K. Natarajan, Vineeth Chandy. A Review: P-Glycoprotein and Its Role in Cancer. Trends in Drug Delivery. 2020; 7(2): 26–34p.

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