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Bcrp/BCRP

Evaluation of Roflumilast (BCRP Inhibitor) and Methotrexate (BCRP Substrate) on Viability of Primary Squamous Cell Carcinoma – An In Vitro Study

Evaluation of Roflumilast (BCRP Inhibitor) and Methotrexate (BCRP Substrate) on Viability of Primary Squamous Cell Carcinoma – An In Vitro Study

... In this study we evaluated the possible beneficial drug- interaction between Roflumilast (BCRP inhibitor) and Methotrexate (BCRP substrate) on viability of primary squamous cell carcinoma cell line using an ...

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Synergistic and complete reversal of the multidrug resistance of mitoxantrone hydrochloride by three-in-one multifunctional lipid-sodium glycocholate nanocarriers based on simultaneous BCRP and Bcl-2 inhibition

Synergistic and complete reversal of the multidrug resistance of mitoxantrone hydrochloride by three-in-one multifunctional lipid-sodium glycocholate nanocarriers based on simultaneous BCRP and Bcl-2 inhibition

... protein, BCRP) and anti-apoptotic defense (B-cell lymphoma, ...– BCRP inhibitor), and GcNa (Bcl-2 ...by BCRP, and the simultaneous release of CsA with MTO further efficiently inhibited the efflux of ...

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Neoadjuvant Endocrine Therapy in Breast Cancer Upregulates the Cytotoxic Drug Pump ABCG2/BCRP, and May Lead to Resistance to Subsequent Chemotherapy

Neoadjuvant Endocrine Therapy in Breast Cancer Upregulates the Cytotoxic Drug Pump ABCG2/BCRP, and May Lead to Resistance to Subsequent Chemotherapy

... for BCRP protein expression (western blot and densitometry) or ABCG2 transcript expression ...(A) BCRP expression was determined after a single dose of 1µM ...relative BCRP expression on the right. ...

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Human ABC transporter ABCG2/BCRP expression in chemoresistance: basic and clinical perspectives for molecular cancer therapeutics

Human ABC transporter ABCG2/BCRP expression in chemoresistance: basic and clinical perspectives for molecular cancer therapeutics

... receptor; BCRP, breast cancer resistance protein; eGFR, epidermal growth factor receptor; eRBB4, erythroblastic leukemia viral oncogene homolog-4; FLT3, Fms-like tyrosine kinase 3; HeR2, human epidermal growth ...

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Expressions of FHIT, BCRP and Bcl-2 Proteins in Breast Invasive Ductal Carcinoma

Expressions of FHIT, BCRP and Bcl-2 Proteins in Breast Invasive Ductal Carcinoma

... of BCRP protein in breast IDC group was significantly higher than that in the control group ...the BCRP expression up-regulation may play a role in the generation of breast IDC by inhibiting the apoptosis ...

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New trends for overcoming ABCG2/BCRP-mediated resistance to cancer therapies

New trends for overcoming ABCG2/BCRP-mediated resistance to cancer therapies

... ATP-binding cassette (ABC) transporters make up a superfamily of transmembrane proteins that play a critical role in the development of drug resistance. This phenomenon is especially important in oncology, where ...

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Gene and functional up-regulation of the BCRP/ABCG2 transporter in hepatocellular carcinoma

Gene and functional up-regulation of the BCRP/ABCG2 transporter in hepatocellular carcinoma

... We here report on the ABCG2 mRNA level and activity in both in vitro and in vivo models consisting of human hepatic cell lines and human samples of HCC to investi- gate the role of this [r] ...

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ATP-binding cassette (ABC) transporters in normal and pathological lung

ATP-binding cassette (ABC) transporters in normal and pathological lung

... ATP-binding cassette (ABC) transporters are a family of transmembrane proteins that can transport a wide variety of substrates across biological membranes in an energy-dependent manner. Many ABC transporters such as ...

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Key words

Key words

... Another ABC transport protein is MRP1 (multidrug resistance-associated protein 1). This protein mediates in the transport of many anions (MOAT, multispecific organic anion transporter) and cytotoxic drugs such as ...

8

Atovaquone and quinine anti malarials inhibit ATP binding cassette transporter activity

Atovaquone and quinine anti malarials inhibit ATP binding cassette transporter activity

... Direct interaction with ABC transporter capacity of anti- malarial compounds has not been explored in detail. In vitro assays have indicated a possible effect on P- gp-mediated transport or expression after exposure to ...

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N-alkylisatin-based microtubule destabilizers bind to the colchicine site on tubulin and retain efficacy in drug resistant acute lymphoblastic leukemia cell lines with less in vitro neurotoxicity

N-alkylisatin-based microtubule destabilizers bind to the colchicine site on tubulin and retain efficacy in drug resistant acute lymphoblastic leukemia cell lines with less in vitro neurotoxicity

... The current approach to treating relapsed ALL involves many of the same drugs used for newly diag- nosed patients; however they are frequently delivered at increased doses or using alternative schedules. The Vinca ...

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The role of amyloid beta clearance in cerebral amyloid angiopathy: more potential therapeutic targets

The role of amyloid beta clearance in cerebral amyloid angiopathy: more potential therapeutic targets

... ATP-binding cassette transporters (ABC transporters) ABC transporter is a member of the biggest protein superfamilies, existing in all living organism from micro- organism to human. The human ABC transporter is encoded ...

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Multiple common and rare variants of ABCG2 cause gout

Multiple common and rare variants of ABCG2 cause gout

... Objective Previous studies have suggested an association between gout susceptibility and common dysfunctional variants in atP-binding cassette transporter subfamily g member 2/breast cancer resistance protein ...

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MicroRNA: a prognostic biomarker and a possible druggable target for circumventing multidrug resistance in cancer chemotherapy

MicroRNA: a prognostic biomarker and a possible druggable target for circumventing multidrug resistance in cancer chemotherapy

... ABCG2/BCRP: Breast cancer resistance protein; ABC transporters: ATP-binding cassette transporters; CSC: Cancer stem cell; DHFR: Dihydrofolate reductase; EGFR: Epidermal growth factor rec[r] ...

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Role of protein kinase CK2 in antitumor drug resistance

Role of protein kinase CK2 in antitumor drug resistance

... ARC: Apoptosis repressor with caspase recruitment domain; BCRP: Breast cancer resistance protein; BRAF: Serine/threonine-protein kinase B-raf; BRD4: Bromodomain-containing protein 4; BTI[r] ...

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Sensitization of Chemo-Resistant Human Chronic Myeloid Leukemia Stem-Like Cells to Hsp90 Inhibitor by SIRT1 Inhibition

Sensitization of Chemo-Resistant Human Chronic Myeloid Leukemia Stem-Like Cells to Hsp90 Inhibitor by SIRT1 Inhibition

... It has been known that several markers associ- ated with CSCs are involved in multidrug resistances. CD44 is a multifunctional transmembrane glycopro- tein expressed in many cells and tissues [12]. It has been reported ...

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The pharmacogenetics of imatinib

The pharmacogenetics of imatinib

... 4q22. BCRP is expressed not only in hematopoietic stem cells but also in hepatic and intestinal epithelial cells, and this aff ects the bioavailability of IM ...of BCRP and may result in altered ...

8

Molecular chess? Hallmarks of anti cancer drug resistance

Molecular chess? Hallmarks of anti cancer drug resistance

... (2)Expression of drug efflux pumps: The ATP-binding cassette (ABC) superfamily of proteins includes a number of membrane proteins able to transport a wide diversity of substrates. Besides an ability to transport of ...

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Original Article Upregulation of miR-202-3p reverses Icotinib resistance in lung carcinoma A549/Ico cells

Original Article Upregulation of miR-202-3p reverses Icotinib resistance in lung carcinoma A549/Ico cells

... Abstract: Objective(s): Icotinib exerts a good anti-tumor efficacy on non-small cell lung cancer (NSCLC), while Icotinib resistance has become an important limiting factor in the clinical application. Studies have ...

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The restorative role of annexin A1 at the blood–brain barrier

The restorative role of annexin A1 at the blood–brain barrier

... barrier; BCRP: breast cancer resistance protein; CNS: central nerv- ous system; COX2: cyclooxygenase 2; CSF: cerebrospinal fluid; DM: diabetes mellitus; DPN: diarylpropionitrile; ER: estrogen receptor; ERK: ...

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