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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Strategies to Overcome or Circumvent P-Glycoprotein Mediated Multidrug Resistance

Author(s): Xun Li, Hongyu Yuan, Jifeng Wu, Jinpei Li, Xianjun Qu, Wenfang Xu and Wei Tang

Volume 15, Issue 5, 2008

Page: [470 - 476] Pages: 7

DOI: 10.2174/092986708783503258

Price: $65


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 Pglycoprotein, 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.

Keywords: MDR, P-glycoprotein, cancer, P-glycoprotein modulators, rational drug design

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