Strategies to overcome or circumvent P-glycoprotein mediated multidrug resistance.
Cancer patients who receive chemotherapy often experience intrinsic or acquired resistance to a broad spectrum of chemotherapeutic agents. The phenomenon, termed multidrug resistance (MDR), is often associated with the over-expression of P-glycoprotein, a transmembrane protein pump, which can enhance efflux of a various chemicals structurally unrelated at the expense of ATP depletion, resulting in decrease of the intracellular cytotoxic drug accumulation. The MDR has been a big threaten to the human health and the war fight for it continues. Although several other mechanisms for MDR are elucidated in recent years, considerable efforts attempting to inverse MDR are involved in exploring P-glycoprotein modulators and suppressing P-glycoprotein expression. In this review, we will report on the recent advances in various strategies for overcoming or circumventing MDR mediated by P-glycoprotein.
Yuan
Hongyu
H
Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong Province, PR China.
Li
Xun
X
Wu
Jifeng
J
Li
Jinpei
J
Qu
Xianjun
X
Xu
Wenfang
W
Tang
Wei
W
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D018432:Drug Resistance, Multiple / Q000187:drug effects*; D019008:Drug Resistance, Neoplasm / Q000187:drug effects; D015870:Gene Expression / Q000187:drug effects; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1