Targeting the ABCG2-overexpressing multidrug resistant (MDR) cancer cells by PPARγ agonists.

ABSTRACT:

Background and purpose

Multidrug resistance (MDR), usually mediated by overexpression of efflux transporters such as P-gp, ABCG2 and/or MRP1, remains a major obstacle hindering successful cancer chemotherapy. There has been great interest in the development of inhibitors towards these transporters to circumvent resistance. However, since the inhibition of transporter is not specific to cancer cells, a decrease in the cytotoxic drug dosing may be needed to prevent excess toxicity, thus undermining the potential benefit brought about by a drug efflux inhibitor. The design of potent MDR modulators specific towards resistant cancer cells and devoid of drug-drug interactions will be needed to effect MDR reversal.

Experimental approach

Recent evidence suggests that the PTEN/PI3K/A

SUBMITTER: To KK 

PROVIDER: S-EPMC3949660 | biostudies-literature | 2013 Nov

REPOSITORIES: biostudies-literature