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Molecules 2012, 17(5), 5442-5458; doi:10.3390/molecules17055442

FG020326 Sensitized Multidrug Resistant Cancer Cells to Docetaxel-Mediated Apoptosis via Enhancement of Caspases Activation

State Key Laboratory of Oncology in Southern China, Cancer Center, Sun Yat-Sen University of Medical Sciences, Guangzhou 510060, China
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Received: 13 March 2012 / Revised: 21 April 2012 / Accepted: 28 April 2012 / Published: 9 May 2012
(This article belongs to the Section Medicinal Chemistry)
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Abstract

Apoptotic resistance is the main obstacle for treating cancer patients with chemotherapeutic drugs. Multidrug resistance (MDR) is often characterized by the expression of P-glycoprotein (P-gp), a 170-KD ATP-dependent drug efflux protein. Functional P-gp can confer resistance to activate caspase-8 and -3 dependent apoptosis induced by a range of different stimuli, including tumor necrosis and chemotherapeutic drugs such as docetaxel and vincristine. We demonstrated here that comparison of sensitive KB cells, P-gp positive (P-gp+ve) KBv200 cells were extremely resistant to apoptosis induced by docetaxel. FG020326, a pharmacological inhibitor of P-gp function, could enhance concentration-dependently the effect of docetaxel on cell apoptosis and sensitize caspase-8, -9 and -3 activation in P-gp overexpressing KBv200 cells, but not in KB cells. Therefore, the enhancement of caspase-8, -9 and -3 activation induced by docetaxel may be one of the key mechanisms of the reversal of P-gp mediated docetaxel resistance by FG020326.
Keywords: cancer; multiple drug resistance; FG020326; P-glycoprotein; apoptosis; caspase cancer; multiple drug resistance; FG020326; P-glycoprotein; apoptosis; caspase
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Wang, X.-W.; Wang, X.-K.; Zhang, X.; Liang, Y.-J.; Shi, Z.; Chen, L.-M.; Fu, L.-W. FG020326 Sensitized Multidrug Resistant Cancer Cells to Docetaxel-Mediated Apoptosis via Enhancement of Caspases Activation. Molecules 2012, 17, 5442-5458.

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