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Epithelial Transfer of the Tyrosine Kinase Inhibitors Erlotinib, Gefitinib, Afatinib, Crizotinib, Sorafenib, Sunitinib, and Dasatinib: Implications for Clinical Resistance

Cancers, 2020-11, Vol.12 (11), p.3322

2020

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RX-3117 (Fluorocyclopentenyl-Cytosine)-Mediated Down-Regulation of DNA Methyltransferase 1 Leads to Protein Expression of Tumor-Suppressor Genes and Increased Functionality of the Proton-Coupled Folate Carrier

International journal of molecular sciences, 2020-04, Vol.21 (8), p.2717

2020

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Schedule-Dependent Synergy Between the Histone Deacetylase Inhibitor Belinostat and the Dihydrofolate Reductase Inhibitor Pralatrexate in T-and B-cell Lymphoma Cells in vitro

Frontiers in cell and developmental biology, 2020-10, Vol.8, p.577215-577215

2020

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The human multidrug resistance protein MRP5 transports folates and can mediate cellular resistance against antifolates

Cancer research (Chicago, Ill.), 2005-05, Vol.65 (10), p.4425-4430

2005

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Oxaliplatin activity in selected and unselected human ovarian and colorectal cancer cell lines

Biochemical pharmacology, 2008-07, Vol.76 (1), p.53-61

2008

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Cellular folate status modulates the expression of BCRP and MRP multidrug transporters in cancer cell lines from different origins

Molecular cancer therapeutics, 2009-03, Vol.8 (3), p.655-664

2009

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ABCG2 harboring the Gly482 mutation confers high-level resistance to various hydrophilic antifolates

Cancer research (Chicago, Ill.), 2005-09, Vol.65 (18), p.8414-8422

2005

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Loss of Multidrug Resistance Protein 1 Expression and Folate Efflux Activity Results in a Highly Concentrative Folate Transport in Human Leukemia Cells

The Journal of biological chemistry, 2003-02, Vol.278 (9), p.6680-6686

2003

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A Structurally Altered Human Reduced Folate Carrier with Increased Folic Acid Transport Mediates a Novel Mechanism of Antifolate Resistance

The Journal of biological chemistry, 1998-11, Vol.273 (46), p.30189-30198

1998

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Folate homeostasis of cancer cells affects sensitivity to not only antifolates but also other non-folate drugs: effect of MRP expression

Pteridines, 2013-06, Vol.24 (1), p.81-86

2013

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Multiple Mechanisms of Resistance to Polyglutamatable and Lipophilic Antifolates in Mammalian Cells: Role of Increased Folylpolyglutamylation, Expanded Folate Pools, and Intralysosomal Drug Sequestration

Molecular pharmacology, 1999-04, Vol.55 (4), p.761-769

1999

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Crizotinib sensitizes the erlotinib resistant HCC827GR5 cell line by influencing lysosomal function

Journal of cellular physiology, 2020-11, Vol.235 (11), p.8085-8097

2020

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Abstract 4725: Inhibition of DNA methyltransferase by RX-3117 (fluorocyclopentenylcytosine) leads to upregulation of hypomethylated targets

Cancer research (Chicago, Ill.), 2016-07, Vol.76 (14_Supplement), p.4725-4725

2016

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Nitric oxide releasing acridone carboxamide derivatives as reverters of doxorubicin resistance in MCF7/Dx cancer cells

Bioorganic chemistry, 2016-02, Vol.64, p.51-58

2016

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Abstract C82: Role of influx and efflux transporters on gut absorption of selected tyrosine kinase inhibitors in a polarized gut epithelium model system

Molecular cancer therapeutics, 2013-11, Vol.12 (11_Supplement), p.C82-C82

2013

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Abstract 4425: Characterisation of cellular transport and accumulation of six clinically approved tyrosine kinase inhibitors (TKIs) in colon cancer cells

Cancer research (Chicago, Ill.), 2013-04, Vol.73 (8_Supplement), p.4425-4425

2013

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Subcellular localization of several structurally different tyrosine kinase inhibitors

ADMET & DMPK, 2018-09, Vol.6 (3), p.258-266

2018

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Transport of six tyrosine kinase inhibitors: active or passive?

ADMET & DMPK, 2016-04, Vol.4 (1), p.23-34

2016

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Metabolism, mechanism of action and sensitivity profile of fluorocyclopentenylcytosine (RX-3117; TV-1360)

Investigational new drugs, 2013-12, Vol.31 (6), p.1444-1457

2013

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Sensitive liquid chromatography mass spectrometry (LC-MS) assay reveals novel insights on DNA methylation and incorporation of gemcitabine, its metabolite difluorodeoxyuridine, deoxyuridine, and RX-3117 into DNA

Nucleosides, nucleotides & nucleic acids, 2016-12, Vol.35 (10-12), p.652-662

2016

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Folate deprivation induces BCRP (ABCG2) expression and mitoxantrone resistance in Caco‐2 cells

International journal of cancer, 2008-10, Vol.123 (7), p.1712-1720

2008

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Synthesis of 2‐Fluoro N 10 ‐Substituted Acridones and Their Cytotoxicity Studies in Sensitive and Resistant Cancer Cell Lines and Their DNA Intercalation Studies

Archiv der Pharmazie (Weinheim), 2009-11, Vol.342 (11), p.640-650

2009

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Cytotoxicity studies of some novel fluoro acridone derivatives against sensitive and resistant cancer cell lines and their mechanistic studies

European journal of pharmaceutical sciences, 2011-07, Vol.43 (4), p.217-224

2011

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Folates provoke cellular efflux and drug resistance of substrates of the multidrug resistance protein 1 (MRP1)

Cancer chemotherapy and pharmacology, 2014-05, Vol.73 (5), p.911-917

2014

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Synthesis of 2-fluoro N(10)-substituted acridones and their cytotoxicity studies in sensitive and resistant cancer cell lines and their DNA intercalation studies

Archiv der Pharmazie (Weinheim), 2009-11, Vol.342 (11), p.640-650

2009

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Epithelial Transfer of the Tyrosine Kinase Inhibitors Erlotinib, Gefitinib, Afatinib, Crizotinib, Sorafenib, Sunitinib, and Dasatinib: Implications for Clinical Resistance

RX-3117 (Fluorocyclopentenyl-Cytosine)-Mediated Down-Regulation of DNA Methyltransferase 1 Leads to Protein Expression of Tumor-Suppressor Genes and Increased Functionality of the Proton-Coupled Folate Carrier

Schedule-Dependent Synergy Between the Histone Deacetylase Inhibitor Belinostat and the Dihydrofolate Reductase Inhibitor Pralatrexate in T-and B-cell Lymphoma Cells in vitro

The human multidrug resistance protein MRP5 transports folates and can mediate cellular resistance against antifolates

Oxaliplatin activity in selected and unselected human ovarian and colorectal cancer cell lines

Cellular folate status modulates the expression of BCRP and MRP multidrug transporters in cancer cell lines from different origins

ABCG2 harboring the Gly482 mutation confers high-level resistance to various hydrophilic antifolates

Loss of Multidrug Resistance Protein 1 Expression and Folate Efflux Activity Results in a Highly Concentrative Folate Transport in Human Leukemia Cells

A Structurally Altered Human Reduced Folate Carrier with Increased Folic Acid Transport Mediates a Novel Mechanism of Antifolate Resistance

Folate homeostasis of cancer cells affects sensitivity to not only antifolates but also other non-folate drugs: effect of MRP expression

Multiple Mechanisms of Resistance to Polyglutamatable and Lipophilic Antifolates in Mammalian Cells: Role of Increased Folylpolyglutamylation, Expanded Folate Pools, and Intralysosomal Drug Sequestration

Crizotinib sensitizes the erlotinib resistant HCC827GR5 cell line by influencing lysosomal function

Abstract 4725: Inhibition of DNA methyltransferase by RX-3117 (fluorocyclopentenylcytosine) leads to upregulation of hypomethylated targets

Nitric oxide releasing acridone carboxamide derivatives as reverters of doxorubicin resistance in MCF7/Dx cancer cells

Abstract C82: Role of influx and efflux transporters on gut absorption of selected tyrosine kinase inhibitors in a polarized gut epithelium model system

Abstract 4425: Characterisation of cellular transport and accumulation of six clinically approved tyrosine kinase inhibitors (TKIs) in colon cancer cells

Subcellular localization of several structurally different tyrosine kinase inhibitors

Transport of six tyrosine kinase inhibitors: active or passive?

Metabolism, mechanism of action and sensitivity profile of fluorocyclopentenylcytosine (RX-3117; TV-1360)

Sensitive liquid chromatography mass spectrometry (LC-MS) assay reveals novel insights on DNA methylation and incorporation of gemcitabine, its metabolite difluorodeoxyuridine, deoxyuridine, and RX-3117 into DNA

Folate deprivation induces BCRP (ABCG2) expression and mitoxantrone resistance in Caco‐2 cells

Synthesis of 2‐Fluoro N 10 ‐Substituted Acridones and Their Cytotoxicity Studies in Sensitive and Resistant Cancer Cell Lines and Their DNA Intercalation Studies

Cytotoxicity studies of some novel fluoro acridone derivatives against sensitive and resistant cancer cell lines and their mechanistic studies

Folates provoke cellular efflux and drug resistance of substrates of the multidrug resistance protein 1 (MRP1)

Synthesis of 2-fluoro N(10)-substituted acridones and their cytotoxicity studies in sensitive and resistant cancer cell lines and their DNA intercalation studies

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