Abstract |
The ATP-binding cassette ( ABC) transporters are members of a protein superfamily that are known to translocate various substrates across membranes, including metabolic products, lipids and sterols, and xenobiotic drugs. Multidrug resistance proteins (MRPs) belong to the subfamily C in the ABC transporter superfamily. MRPs have been implicated in mediating multidrug resistance by actively extruding chemotherapeutic substrates. Moreover, some MRPs are known to be essential in physiological excretory or regulatory pathways. The importance of MRPs in cancer therapy is also implied by their clinical insights. Modulating the function of MRPs to re-sensitize chemotherapeutic agents in cancer therapy shows great promise in cancer therapy; thus, multiple MRP inhibitors have been developed recently. This review article summarizes the structure, distribution, and physiological as well as pharmacological function of MRP1-MRP9 in cancer chemotherapy. Several novel modulators targeting MRPs in cancer therapy are also discussed.
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Authors | Yun-Kai Zhang, Yi-Jun Wang, Pranav Gupta, Zhe-Sheng Chen |
Journal | The AAPS journal
(AAPS J)
Vol. 17
Issue 4
Pg. 802-12
(Jul 2015)
ISSN: 1550-7416 [Electronic] United States |
PMID | 25840885
(Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't, Review)
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Chemical References |
- ATP-Binding Cassette Transporters
- Antineoplastic Agents
- Multidrug Resistance-Associated Proteins
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Topics |
- ATP-Binding Cassette Transporters
(metabolism)
- Animals
- Antineoplastic Agents
(pharmacology)
- Biological Transport
(physiology)
- Drug Resistance, Neoplasm
(drug effects)
- Humans
- Multidrug Resistance-Associated Proteins
(metabolism)
- Neoplasms
(drug therapy, pathology)
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