Identification of anticancer OATP2B1 substrates by an in vitro triple-fluorescence-based cytotoxicity screen.

ABSTRACT: Membrane transporters play an important role in the absorption, distribution, metabolism and excretion of drugs. The cellular accumulation of many drugs is the result of the net function of efflux and influx transporters. Efflux transporters such as P-glycoprotein/ABCB1 have been shown to confer multidrug resistance in cancer. Although expression of uptake transporters has been confirmed in cancer cells, their role in chemotherapy response has not been systematically investigated. In the present study we have adapted a fluorescence-based cytotoxic assay to characterize the influence of key drug-transporters on the toxicity of approved anticancer drugs. Co-cultures of fluorescently labeled parental and transporter-expressing cells (expressing ABCB1, ABCG2 or OATP2B1) were screened against 1

SUBMITTER: Windt T 

PROVIDER: S-EPMC6510822 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature