Tissue Distribution Of Drugrelated Abc Transporters

MDR1 (ABCB1), MRP2 (ABCC2), and BCRP (ABCG2) are all expressed in the apical side of the intestinal epithelia, where they extrude xenobiotics, including many clinically relevant drugs. Key to the vectorial excretion of drugs into urine or bile, ABC transporters are expressed in polarized tissues, such as kidney and liver: MDR1, MRP2, and MRP4 (ABCC4) on the brush-border membrane of renal epithelia, and MDR1, MRP2, and BCRP on the bile canalicular membrane of hepa-tocytes. Some ABC transporters are expressed specifically on the blood side of the endothelial or epithelial cells that form barriers to the free entrance of toxic compounds into tissues: the BBB (MDR1 and MRP4 on the luminal side of brain capillary endothelial cells), the blood-cerebrospinal fluid (CSF) barrier (MRP1 and MRP4 on the basolateral blood side of choroid plexus epithelia), the blood-testis barrier (MRP1 on the basolateral membrane of mouse Sertoli

Table 2-1

Regulation of Transporter Expression by Nuclear Receptors



Transcription Factor

Ligand (Modulated by Drugs)

MDR1 (P-gp)


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