Recent advances in P-glycoprotein-mediated multidrug resistance reversal mechanisms.
Expression of the multidrug resistance (MDR) phenotype is responsible for chemotherapy failure in numerous cancers. Overexpression of mdr1 gene-encoded permeability glycoprotein (P-gp) is known to play a pivotal role in the development of this phenotype. The role of P-gp has been proposed as an important goal in the design of chemotherapy strategies. However, modulation of P-gp activity by chemotherapy has limited possibilities because of toxicity and poor specificity. In this article, we review the latest advancements in different potential P-gp-mediated MDR reversal mechanisms as well as the methods of evaluating MDR reversal activity, which would be helpful in finding novel MDR reversal agents (or chemosensitizers).
Li
X
X
School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong, People's Republic of China. tjulx2004@sdu.edu.cn
Li
J-P
JP
Yuan
H-Y
HY
Gao
X
X
Qu
X-J
XJ
Xu
W-F
WF
Tang
W
W
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors / Q000096:biosynthesis* / Q000235:genetics; D000970:Antineoplastic Agents / Q000493:pharmacokinetics / Q000494:pharmacology; D017209:Apoptosis / Q000502:physiology; D018432:Drug Resistance, Multiple / Q000235:genetics / Q000276:immunology / Q000502:physiology*; D019008:Drug Resistance, Neoplasm / Q000235:genetics / Q000276:immunology / Q000502:physiology*; D019450:Genes, MDR; D006801:Humans
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000970:Antineoplastic Agents