Structure and function of P-glycoprotein in normal liver and small intestine.

作者: Zenaida C. Gatmaitan , Irwin M. Arias

DOI: 10.1016/S1054-3589(08)60934-5

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摘要: Publisher Summary This chapter discusses the structure and function of P-glycoprotein in normal liver small intestine. Mammalian cells selected for resistance to a single cytotoxic agent display cross-resistance broad spectrum structurally functionally unrelated compounds. is “multidrug resistance” (MDR) phenomenon. The emergence multidrug cultured associated with overexpression membrane glycoprotein called “P-glycoprotein” (or Gp170). P-Glycoprotein appears as an ATP-dependent transporter that pumps drugs out cells. It interacts diverse group substrates most which are hydrophobic lipid-soluble organic cations natural origin including anthracyclines, vinca alkaloids, colchicines. Based on sequence homology between known transport proteins, model has been proposed responsible efflux through plasma channel formed by transmembrane domains one or more molecules. Energy presumably derived from ATP hydrolysis using bound both nucleotide binding sites. levels drug-resistant correlate amount drug transported cell, but whether initial rate affected less established.

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