Title : Microtubule-targeting anticancer drug eribulin induces drug efflux transporter P-glycoprotein.

Pub. Date : 2020 Mar

PMID : 31993509






5 Functional Relationships(s)
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1 This study examined the effects of microtubule-targeting anticancer drugs (paclitaxel, cabazitaxel, and eribulin) on the expression of drug efflux transporter P-glycoprotein, which is encoded by MDR1. Paclitaxel ATP binding cassette subfamily B member 1 Homo sapiens
2 This study examined the effects of microtubule-targeting anticancer drugs (paclitaxel, cabazitaxel, and eribulin) on the expression of drug efflux transporter P-glycoprotein, which is encoded by MDR1. Paclitaxel ATP binding cassette subfamily B member 1 Homo sapiens
3 Paclitaxel and eribulin induced MDR1 promoter activity in a concentration-dependent manner, while cabazitaxel had little effect in human intestinal epithelial LS174T cells. Paclitaxel ATP binding cassette subfamily B member 1 Homo sapiens
4 Overexpression of the nuclear receptor pregnane X receptor (PXR) gene (NR1I2) enhanced paclitaxel- and eribulin-induced MDR1 activation, but expression of the nuclear receptor co-repressor silencing mediator for retinoid and thyroid receptors (SMRT) gene (NCOR2) repressed MDR1 activation. Paclitaxel ATP binding cassette subfamily B member 1 Homo sapiens
5 Cellular uptake of rhodamine 123 and calcein-acetoxymethyl ester (calcein-AM), P-glycoprotein substrates, decreased in paclitaxel- or eribulin-treated LS174T cells. Paclitaxel ATP binding cassette subfamily B member 1 Homo sapiens