BIOCHEMICAL, CELLULAR, AND PHARMACOLOGICAL ASPECTS OF THE MULTIDRUG TRANSPORTER

Author:

Ambudkar Suresh V.1,Dey Saibal1,Hrycyna Christine A.1,Ramachandra Muralidhara1,Pastan Ira1,Gottesman Michael M.1

Affiliation:

1. Laboratory of Cell Biology and +Laboratory of Molecular Biology, Division of Basic Sciences, National Cancer Institute, National Institutes of Health, Bethesda, Maryland 20892;and

Abstract

▪ Abstract  Considerable evidence has accumulated indicating that the multidrug transporter or P-glycoprotein plays a role in the development of simultaneous resistance to multiple cytotoxic drugs in cancer cells. In recent years, various approaches such as mutational analyses and biochemical and pharmacological characterization have yielded significant information about the relationship of structure and function of P-glycoprotein. However, there is still considerable controversy about the mechanism of action of this efflux pump and its function in normal cells. This review summarizes current research on the structure-function analysis of P-glycoprotein, its mechanism of action, and facts and speculations about its normal physiological role.

Publisher

Annual Reviews

Subject

Pharmacology,Toxicology

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