Considerable evidence has accumulated indicating that the multidrug transpo
rter or P-glycoprotein plays a role in the development of simultaneous resi
stance to multiple cytotoxic drugs in cancer cells. In recent years, variou
s approaches such as mutational analyses and biochemical and pharmacologica
l characterization have yielded significant information about the relations
hip of structure and function of P-glycoprotein. However, there is still co
nsiderable controversy about the mechanism of action of this efflux pump an
d 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 ifs normal physiological role.