title: The Pharmacological and Physiological Role of Multidrug-Resistant Protein 4.
abstract: Multidrug-resistant protein 4 (MRP4), a member of the C subfamily of ATP-binding cassette transporters, is distributed in a variety of tissues and a number of cancers. As a drug transporter, MRP4 is responsible for the pharmacokinetics and pharmacodynamics of numerous drugs, especially antiviral drugs, antitumor drugs, and diuretics. In this regard, the functional role of MRP4 is affected by a number of factors, such as genetic mutations; tissue-specific transcriptional regulations; post-transcriptional regulations, including miRNAs and membrane internalization; and substrate competition. Unlike other C family members, MRP4 is in a pivotal position to transport cellular signaling molecules, through which it is tightly connected to the living activity and physiologic processes of cells and bodies. In the context of several cancers in which MRP4 is overexpressed, MRP4 inhibition shows striking effects against cancer progression and drug resistance. In this review, we describe the role of MRP4 more specifically in both healthy conditions and disease states, with an emphasis on its potential as a drug target.
authors.affiliation: Department of Clinical Pharmacology, Xiangya Hospital, Central South University, ChangSha, P.R. China; Institute of Clinical Pharmacology, Central South University, ChangSha, P.R. China; and Hunan Key Laboratory of Pharmacogenetics, ChangSha, P.R. China.
authors.forename: Jiagen
authors.initials: J
authors.lastname: Wen
authors.affiliation: Department of Clinical Pharmacology, Xiangya Hospital, Central South University, ChangSha, P.R. China; Institute of Clinical Pharmacology, Central South University, ChangSha, P.R. China; and Hunan Key Laboratory of Pharmacogenetics, ChangSha, P.R. China.
authors.forename: Jianquan
authors.initials: J
authors.lastname: Luo
authors.affiliation: Department of Clinical Pharmacology, Xiangya Hospital, Central South University, ChangSha, P.R. China; Institute of Clinical Pharmacology, Central South University, ChangSha, P.R. China; and Hunan Key Laboratory of Pharmacogenetics, ChangSha, P.R. China.
authors.forename: Weihua
authors.initials: W
authors.lastname: Huang
authors.affiliation: Department of Clinical Pharmacology, Xiangya Hospital, Central South University, ChangSha, P.R. China; Institute of Clinical Pharmacology, Central South University, ChangSha, P.R. China; and Hunan Key Laboratory of Pharmacogenetics, ChangSha, P.R. China.
authors.forename: Jie
authors.initials: J
authors.lastname: Tang
authors.affiliation: Department of Clinical Pharmacology, Xiangya Hospital, Central South University, ChangSha, P.R. China; Institute of Clinical Pharmacology, Central South University, ChangSha, P.R. China; and Hunan Key Laboratory of Pharmacogenetics, ChangSha, P.R. China.
authors.forename: Honghao
authors.initials: H
authors.lastname: Zhou
authors.affiliation: Department of Clinical Pharmacology, Xiangya Hospital, Central South University, ChangSha, P.R. China; Institute of Clinical Pharmacology, Central South University, ChangSha, P.R. China; and Hunan Key Laboratory of Pharmacogenetics, ChangSha, P.R. China yjsd2003@163.com.
authors.forename: Wei
authors.initials: W
authors.lastname: Zhang
mesh_terms: D018528:ATP-Binding Cassette Transporters / Q000378:metabolism; D000818:Animals; D001692:Biological Transport / Q000502:physiology*; D006801:Humans; D027425:ATP-Binding Cassette, Sub-Family C Proteins / Q000378:metabolism*; D009369:Neoplasms / Q000378:metabolism; D004364:Pharmaceutical Preparations / Q000378:metabolism*; D015398:Signal Transduction / Q000502:physiology
chemical_list: D018528:ATP-Binding Cassette Transporters; D027425:ATP-Binding Cassette, Sub-Family C Proteins; D004364:Pharmaceutical Preparations