For most cancers, the treatment of choice is still chemotherapy despite its severe
adverse effects, systemic toxicity and limited efficacy due to the development of
multidrug resistance (MDR). MDR leads to chemotherapy failure generally associated
with a decrease in drug concentration inside cancer cells, frequently due to the overexpression
of ABC transporters such as P-glycoprotein (P-gp/MDR1/ABCB1), multidrug
resistance-associated proteins (MRPs/ABCCs), and breast cancer resistance protein
(BCRP/ABCG2), which limits the efficacy of chemotherapeutic drugs. The aim of this
review is to compile information about transcriptional and post-transcriptional regulation
of ABC transporters and discuss their role in mediating MDR in cancer cells.
This review also focuses on drug resistance by ABC efflux transporters in cancer cells,
particularly hepatocellular carcinoma (HCC) and colorectal carcinoma (CRC) cells. Some
aspects of the chemotherapy failure and future directions to overcome this problem are
Keywords: ABCB1, ABCC2, ABCG2, chemotherapy, hepatocellular carcinoma, colorectal carcinoma, multidrug
resistance, transcriptional regulation.
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