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Cancer Lett. 2016 Jan 1;370(1):153-64. doi: 10.1016/j.canlet.2015.10.010. Epub 2015 Oct 20.

Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade.

Author information

1
Department of Pharmacy, Anhui Provincial Hospital, 17 Lujiang Road, Hefei, Anhui 230001, China; Institute for Liver Diseases of Anhui Medical University (AMU), Anhui Institute of Innovative Drugs, Anhui Key Laboratory of Bioactivity of Natural Products, School of Pharmacy, Anhui Medical University, Hefei, Anhui 230032, China.
2
Department of Pharmacy, Anhui Provincial Hospital, 17 Lujiang Road, Hefei, Anhui 230001, China.
3
Institute for Liver Diseases of Anhui Medical University (AMU), Anhui Institute of Innovative Drugs, Anhui Key Laboratory of Bioactivity of Natural Products, School of Pharmacy, Anhui Medical University, Hefei, Anhui 230032, China.
4
Department of Pharmacy, Anhui Provincial Hospital, 17 Lujiang Road, Hefei, Anhui 230001, China. Electronic address: ahslyyjl@126.com.
5
Institute for Liver Diseases of Anhui Medical University (AMU), Anhui Institute of Innovative Drugs, Anhui Key Laboratory of Bioactivity of Natural Products, School of Pharmacy, Anhui Medical University, Hefei, Anhui 230032, China. Electronic address: lj@ahmu.edu.cn.

Abstract

Multidrug resistance (MDR) is a serious phenomenon employed by cancer cells which hampers the success of cancer pharmacotherapy. One of the common mechanisms of MDR is the overexpression of ATP-binding cassette (ABC) efflux transporters in cancer cells such as P-glycoprotein (P-gp/ABCB1), multidrug resistance-associated protein 2 (MRP2/ABCC2), and breast cancer resistance protein (BCRP/ABCG2) that limits the prolonged and effective use of chemotherapeutic drugs. Researchers have found that developing inhibitors of ABC efflux transporters as chemosensitizers could overcome MDR. But the clinical trials have shown that most of these chemosensitizers are merely toxic and only show limited or no benefits to cancer patients, thus new inhibitors are being explored. Recent findings also suggest that efflux pumps of the ABC transporter family are subject to epigenetic gene regulation. In this review, we summarize recent findings of the role of ABC efflux transporters in MDR.

KEYWORDS:

ABC transporters; Cancer therapy; Inhibitors; Multidrug resistance

PMID:
26499806
DOI:
10.1016/j.canlet.2015.10.010
[Indexed for MEDLINE]

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