TY - JOUR
T1 - Reversers of the multidrug resistance transporter P-glycoprotein
AU - Stein, Wilfred D.
PY - 2002/5/1
Y1 - 2002/5/1
N2 - Multidrug resistance can arise from the presence of the membrane-bound pump, P-glycoprotein, in a tumor. Major efforts have been made to develop inhibitors of this pump, and a number of promising blockers have reached late stages of clinical trials. The kinetics of the inhibition of P-glycoprotein is complex, with numerous binding sites that can interact synergistically. Reversers of increased affinity and specificity could, in principle, be developed on the basis of these synergies, and offer some promise in cancer therapeutics.
AB - Multidrug resistance can arise from the presence of the membrane-bound pump, P-glycoprotein, in a tumor. Major efforts have been made to develop inhibitors of this pump, and a number of promising blockers have reached late stages of clinical trials. The kinetics of the inhibition of P-glycoprotein is complex, with numerous binding sites that can interact synergistically. Reversers of increased affinity and specificity could, in principle, be developed on the basis of these synergies, and offer some promise in cancer therapeutics.
KW - Chemosensitizer
KW - Membrane pump
KW - Multidrug resistance
KW - P-glycoprotein
UR - http://www.scopus.com/inward/record.url?scp=0036591187&partnerID=8YFLogxK
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C2 - 12090558
AN - SCOPUS:0036591187
SN - 1472-4472
VL - 3
SP - 812
EP - 817
JO - Current Opinion in Investigational Drugs
JF - Current Opinion in Investigational Drugs
IS - 5
ER -
