TY - JOUR T1 - The Pharmacological and Physiological Role of Multidrug-Resistant Protein 4 JF - Journal of Pharmacology and Experimental Therapeutics JO - J Pharmacol Exp Ther SP - 358 LP - 375 DO - 10.1124/jpet.115.225656 VL - 354 IS - 3 AU - Jiagen Wen AU - Jianquan Luo AU - Weihua Huang AU - Jie Tang AU - Honghao Zhou AU - Wei Zhang Y1 - 2015/09/01 UR - http://jpet.aspetjournals.org/content/354/3/358.abstract N2 - 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. ER -