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Repositioning of Tyrosine Kinase Inhibitors as Antagonists of ATP-Binding Cassette Transporters in Anticancer Drug Resistance

Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, NY 11439, USA
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Cancers 2014, 6(4), 1925-1952; https://doi.org/10.3390/cancers6041925
Received: 31 July 2014 / Revised: 4 September 2014 / Accepted: 11 September 2014 / Published: 29 September 2014
(This article belongs to the Special Issue Cancer Drug Resistance)
The phenomenon of multidrug resistance (MDR) has attenuated the efficacy of anticancer drugs and the possibility of successful cancer chemotherapy. ATP-binding cassette (ABC) transporters play an essential role in mediating MDR in cancer cells by increasing efflux of drugs from cancer cells, hence reducing the intracellular accumulation of chemotherapeutic drugs. Interestingly, small-molecule tyrosine kinase inhibitors (TKIs), such as AST1306, lapatinib, linsitinib, masitinib, motesanib, nilotinib, telatinib and WHI-P154, have been found to have the capability to overcome anticancer drug resistance by inhibiting ABC transporters in recent years. This review will focus on some of the latest and clinical developments with ABC transporters, TKIs and anticancer drug resistance. View Full-Text
Keywords: multidrug resistance; ABC transporters; tyrosine kinase inhibitor; clinical relevance; pharmacogenomics multidrug resistance; ABC transporters; tyrosine kinase inhibitor; clinical relevance; pharmacogenomics
MDPI and ACS Style

Wang, Y.-J.; Zhang, Y.-K.; Kathawala, R.J.; Chen, Z.-S. Repositioning of Tyrosine Kinase Inhibitors as Antagonists of ATP-Binding Cassette Transporters in Anticancer Drug Resistance. Cancers 2014, 6, 1925-1952.

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Cancers, EISSN 2072-6694, Published by MDPI AG
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