ABC transporter protein and cancer drug resistance

Abstract

   Drug resistance imposes a major constraint on the successful treatment of cancer. One of the most significant factors in cancer drug resistance is efflux transporter activity. ABC (ATP-binding cassette) transporters are widely acknowledged as a class of efflux transporters, which actively efflux anticancer agents out of cells by using energy from ATP and play a crucial role on cancer drug resistance. Overexpression of P-glycoprotein (P-gp; ABCB1), breast cancer resistance protein (BCRP; ABCG2) and multidrug resistance-associated protein 1 (MRP1; ABCC1) has been reported in a variety of solid tumours and haematological malignancies and transport a variety of anticancer agents. Here, this article reviews an understanding on ABC transporter proteins in terms of structure, efflux substrate specificity, a role in physiological aspects, potential strategies and modulators to overcome ABC transporters.

Key words: ABC transporter protein, Cancer drug resistance, P-glycoprotein, Breast cancer resistance protein, Multidrug resistance-associated protein 1