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Integrated application of enhanced replacement method and ensemble learning for the prediction of BCRP/ABCG2 substrates
(Bentham Science Publishers, 2017-06)
Background: Breast Cancer Resistance Protein (BCRP or ABCG2) is a polyspecific efflux transporter which belongs to the ATP-binding Cassette superfamily. Up-regulation of BCRP is associated to multi-drug resistance in a ...
Induction of ABCG2/BCRP restricts the distribution of zidovudine to the fetal brain in rats
(Academic Press Inc Elsevier Science, 2017-09)
Safety concerns for fetus development of zidovudine (AZT) administration as prophylaxis of vertical transmission of HIV persist. We evaluated the participation of the ATP-binding cassette efflux transporter ABCG2 in the ...
The phytoestrogens daidzein and equol inhibit the drug transporter BCRP/ABCG2 in breast cancer cells: potential chemosensitizing effect
(Dr Dietrich Steinkopff Verlag, 2017-11)
PURPOSE: The soy isoflavone genistein has been described to up-regulate breast cancer resistance protein (BCRP) and, thus, enhance chemoresistance in breast cancer cells. The aim of this work was to assess the effect of ...
ABCG2 c.421C>A polymorphism alters nifedipine transport to breast milk in hypertensive breastfeeding women
(2019-04-01)
Nifedipine, a known substrate to breast cancer resistance protein (ABCG2/BCRP), is used for the treatment of hypertension during breastfeeding. This study aimed to evaluate the effect of ABCG2 c.421C>A on nifedipine transfer ...
Increased delivery of chemotherapy to the vitreous by inhibition of the blood-retinal barrier
(Elsevier Science, 2017-10)
Treatment of retinoblastoma -a pediatric cancer of the developing retina- might benefit from strategies to inhibit the blood-retinal barrier (BRB). The potent anticancer agent topotecan is a substrate of efflux transporters ...
Development and Validation of a Computational Model Ensemble for the Early Detection of BCRP/ABCG2 Substrates during the Drug Design Stage
(American Chemical Society, 2017-08)
Breast Cancer Resistance Protein (BCRP) is an ATP-dependent efflux transporter linked to the multidrug resistance phenomenon in many diseases such as epilepsy and cancer and a potential source of drug interactions. For ...