Effects of GLPG3970 on Sulfasalazine and Methotrexate Pharmacokinetics in Healthy Adults: Two Open‐Label, Phase I, Drug–Drug Interaction Studies
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DOI: 10.1002/cpt.3438
Abstract: GLPG3970 is a selective salt‐inducible kinase 2/3 inhibitor intended for the treatment of inflammatory diseases. In vitro studies suggest GLPG3970 strongly inhibits breast cancer resistance protein (BCRP), indicating a possible interaction with BCRP substrates such… read more here.
Keywords: ssz; bcrp; glpg3970; drug ... See more keywords
Identification and Clinical Evaluation of Potential Biomarkers for Breast Cancer Resistance Protein (BCRP/ ABCG2 )
Sign Up to like & getrecommendations! Published in 2025 at "Clinical Pharmacology and Therapeutics"
DOI: 10.1002/cpt.3657
Abstract: Clinical inhibition and genetic variation of the Breast Cancer Resistance Protein (BCRP/ABCG2) efflux transporter can significantly influence drug exposure, highlighting the need for reliable BCRP functional biomarkers. This study aimed to identify and evaluate biomarkers… read more here.
Keywords: breast cancer; bcrp; function; cancer resistance ... See more keywords
The phytoestrogens daidzein and equol inhibit the drug transporter BCRP/ABCG2 in breast cancer cells: potential chemosensitizing effect
Sign Up to like & getrecommendations! Published in 2017 at "European Journal of Nutrition"
DOI: 10.1007/s00394-017-1578-9
Abstract: PurposeThe 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 long- and… read more here.
Keywords: bcrp; cancer cells; transporter; breast cancer ... See more keywords
Phytochemical mediated-modulation of the expression and transporter function of breast cancer resistance protein at the blood-brain barrier: An in-vitro study
Sign Up to like & getrecommendations! Published in 2017 at "Brain Research"
DOI: 10.1016/j.brainres.2016.10.020
Abstract: Clinical translation of BCRP inhibitors have failed due to neurotoxicity and novel approaches are required to identify suitable modulators of BCRP to enhance CNS drug delivery. In this study we examine 18 compounds, primarily phytochemicals,… read more here.
Keywords: bcrp; study; expression; function ... See more keywords
ROS Increase Chemo-reagent Concentration by the Down Regulation of BCRP During Both Hyperthermia and Chemotherapy
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DOI: 10.1016/j.freeradbiomed.2017.10.138
Abstract: Hyperthermia (HT) is a non-invasive cancer therapy. Treatment temperature between 41 to 44°C has no cytotoxic damage in normal cells, while the temperature does in cancer cells because of the underdeveloped vascular system. HT often… read more here.
Keywords: chemotherapy; bcrp; ros increase; treatment ... See more keywords
Identification of new 2,5-diketopiperazine derivatives as simultaneous effective inhibitors of αβ-tubulin and BCRP proteins: Molecular docking, Structure−Activity Relationships and virtual consensus docking studies
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Molecular Structure"
DOI: 10.1016/j.molstruc.2017.02.049
Abstract: Abstract In the first part of this paper, docking method was employed in order to study the binding mechanism of breast cancer resistance protein (BCRP) with a group of previously synthesized TPS-A derivatives which known… read more here.
Keywords: bcrp; binding site; diketopiperazine derivatives; tubulin bcrp ... See more keywords
Validation of Human MDR1-MDCK and BCRP-MDCK Cell Lines to Improve the Prediction of Brain Penetration.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of pharmaceutical sciences"
DOI: 10.1016/j.xphs.2019.02.005
Abstract: It is of great challenge to predict human brain penetration for substrates of multidrug resistance protein 1 (MDR1) and breast cancer resistance protein (BCRP), 2 major efflux transporters at blood-brain barrier. Thus, a physiologically based… read more here.
Keywords: mdck; bcrp; brain penetration; mdr1 ... See more keywords
Expanding the efflux in vitro assay toolbox: A CRISPR-Cas9 edited MDCK cell line with human BCRP and completely lacking canine MDR1.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of pharmaceutical sciences"
DOI: 10.1016/j.xphs.2020.09.039
Abstract: The Breast Cancer Resistance Protein (BCRP) is a key transporter in drug efflux and drug-drug interactions. However, endogenous expression of Multidrug Resistance Protein 1 (MDR1) confounds the interpretation of BCRP-mediated transport in in vitro models.… read more here.
Keywords: bcrp; cell line; canine; drug ... See more keywords
Development and Validation of a Computational Model Ensemble for the Early Detection of BCRP/ABCG2 Substrates during the Drug Design Stage.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of chemical information and modeling"
DOI: 10.1021/acs.jcim.7b00016
Abstract: 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 these reasons, the… read more here.
Keywords: model ensemble; bcrp; development validation; drug ... See more keywords
Flavonoid Monomers as Potent, Nontoxic, and Selective Modulators of the Breast Cancer Resistance Protein (ABCG2).
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00779
Abstract: We synthesize various substituted triazole-containing flavonoids and identify potent, nontoxic, and highly selective BCRP inhibitors. Ac18Az8, Ac32Az19, and Ac36Az9 possess m-methoxycarbonylbenzyloxy substitution at C-3 of the flavone moiety and substituted triazole at C-4' of the… read more here.
Keywords: potent nontoxic; bcrp; selective modulators; flavonoid monomers ... See more keywords
Bile duct ligation enhances AZT CNS toxicity partly by impairing the expression and function of BCRP in rat brain
Sign Up to like & getrecommendations! Published in 2019 at "Acta Pharmacologica Sinica"
DOI: 10.1038/s41401-019-0242-8
Abstract: Breast cancer resistance protein (BCRP) is one of ATP-binding cassette (ABC) transporters in brain microvessel endothelial cells that transport their substrates from brain to blood, thus limiting substrates to crossing into brain through blood–brain barrier.… read more here.
Keywords: bcrp; brain; expression function; bdl rats ... See more keywords