The FLT3 inhibitor quizartinib inhibits ABCG2 at pharmacologically relevant concentrations, with implications for both chemosensitization and adverse drug interactions

scientific article (publication date: 2013)

The FLT3 inhibitor quizartinib inhibits ABCG2 at pharmacologically relevant concentrations, with implications for both chemosensitization and adverse drug interactions is …
instance of (P31):
scholarly articleQ13442814

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P819ADS bibcode2013PLoSO...871266B
P356DOI10.1371/JOURNAL.PONE.0071266
P932PMC publication ID3743865
P698PubMed publication ID23967177
P5875ResearchGate publication ID256072865

P50authorKarthika NatarajanQ59685417
P2093author name stringMaria R Baer
Suresh V Ambudkar
Mariola Sadowska
Suneet Shukla
Trevor J Mathias
Jasjeet Bhullar
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P-glycoprotein inhibition using valspodar (PSC-833) does not improve outcomes for patients younger than age 60 years with newly diagnosed acute myeloid leukemia: Cancer and Leukemia Group B study 19808Q34124919
VX-710 (biricodar) increases drug retention and enhances chemosensitivity in resistant cells overexpressing P-glycoprotein, multidrug resistance protein, and breast cancer resistance proteinQ34304819
Zosuquidar, a novel modulator of P-glycoprotein, does not improve the outcome of older patients with newly diagnosed acute myeloid leukemia: a randomized, placebo-controlled trial of the Eastern Cooperative Oncology Group 3999Q34360283
The presence of a FLT3 internal tandem duplication in patients with acute myeloid leukemia (AML) adds important prognostic information to cytogenetic risk group and response to the first cycle of chemotherapy: analysis of 854 patients from the UniteQ34517403
Analysis of FLT3 length mutations in 1003 patients with acute myeloid leukemia: correlation to cytogenetics, FAB subtype, and prognosis in the AMLCG study and usefulness as a marker for the detection of minimal residual diseaseQ34524219
Cladribine, but not fludarabine, added to daunorubicin and cytarabine during induction prolongs survival of patients with acute myeloid leukemia: a multicenter, randomized phase III study.Q34637551
Results from a randomized trial of salvage chemotherapy followed by lestaurtinib for patients with FLT3 mutant AML in first relapseQ34754344
Identification of a urate transporter, ABCG2, with a common functional polymorphism causing goutQ34985649
Evidence for a requirement for ATP hydrolysis at two distinct steps during a single turnover of the catalytic cycle of human P-glycoproteinQ35076190
ABC of oral bioavailability: transporters as gatekeepers in the gut.Q35591517
Breast cancer resistance protein is localized at the plasma membrane in mitoxantrone- and topotecan-resistant cell lines.Q52828279
Expression of the hematopoietic growth factor receptor FLT3 (STK-1/Flk2) in human leukemiasQ58290358
Human FLT3/FLK2 receptor tyrosine kinase is expressed at the surface of normal and malignant hematopoietic cellsQ71094131
Regulation of ciprofloxacin uptake in human promyelocytic leukemia cells and polymorphonuclear leukocytesQ73292917
Chemoprotection of hematopoietic cells by a mutant P-glycoprotein resistant to a potent chemosensitizer of multidrug-resistant cancersQ73563720
ABCB1 modulation does not circumvent drug extrusion from primitive leukemic progenitor cells and may preferentially target residual normal cells in acute myelogenous leukemiaQ83895091
Combination of cytarabine and topotecan in patients treated for acute myeloid leukemia with persistent disease after frontline inductionQ84124203
Structure, function and regulation of P-glycoprotein and its clinical relevance in drug dispositionQ94705289
Targeting the multidrug resistance-1 transporter in AML: molecular regulation and therapeutic strategiesQ35817464
Collateral sensitivity as a strategy against cancer multidrug resistanceQ35946556
Tyrosine kinase inhibitors as modulators of ABC transporter-mediated drug resistanceQ35946822
Randomized phase II study of two schedules of flavopiridol given as timed sequential therapy with cytosine arabinoside and mitoxantrone for adults with newly diagnosed, poor-risk acute myelogenous leukemiaQ36366636
Evidence for dual mode of action of a thiosemicarbazone, NSC73306: a potent substrate of the multidrug resistance linked ABCG2 transporter.Q36496944
Human multidrug resistance ABCB and ABCG transporters: participation in a chemoimmunity defense systemQ36610461
The novel BCR-ABL and FLT3 inhibitor ponatinib is a potent inhibitor of the MDR-associated ATP-binding cassette transporter ABCG2Q36933169
Sunitinib (Sutent, SU11248), a small-molecule receptor tyrosine kinase inhibitor, blocks function of the ATP-binding cassette (ABC) transporters P-glycoprotein (ABCB1) and ABCG2.Q37188016
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML)Q37373040
Interaction of nilotinib, dasatinib and bosutinib with ABCB1 and ABCG2: implications for altered anti-cancer effects and pharmacological propertiesQ37447522
Bench to bedside targeting of FLT3 in acute leukemiaQ37724957
Tyrosine kinase inhibitors as modulators of ATP binding cassette multidrug transporters: substrates, chemosensitizers or inducers of acquired multidrug resistance?Q37853578
Targeting the FMS-like tyrosine kinase 3 in acute myeloid leukemiaQ38011962
FLT3 inhibition as therapy in acute myeloid leukemia: a record of trials and tribulationsQ39513601
Breast cancer resistance protein and P-glycoprotein limit sorafenib brain accumulationQ39747662
Contribution of the drug transporter ABCG2 (breast cancer resistance protein) to resistance against anticancer nucleosides.Q39944267
Inhibition of ABCG2-mediated transport by protein kinase inhibitors with a bisindolylmaleimide or indolocarbazole structure.Q40118559
The calcium channel blockers, 1,4-dihydropyridines, are substrates of the multidrug resistance-linked ABC drug transporter, ABCG2.Q40254927
Breast cancer resistance protein (BCRP/ABCG2) transports fluoroquinolone antibiotics and affects their oral availability, pharmacokinetics, and milk secretionQ40325508
Breast cancer resistance protein in drug resistance of primitive CD34+38- cells in acute myeloid leukemiaQ40442997
Cyclosporin A is a broad-spectrum multidrug resistance modulatorQ40443016
Gefitinib reverses breast cancer resistance protein-mediated drug resistanceQ40515752
Breast cancer resistance protein (BCRP/MXR/ABCG2) in acute myeloid leukemia: discordance between expression and functionQ40543176
FLT3 ligand causes autocrine signaling in acute myeloid leukemia cellsQ40635369
Identification and characterization of the MDR1 promoter-enhancing factor 1 (MEF1) in the multidrug resistant HL60/VCR human acute myeloid leukemia cell lineQ40907899
Multiple mechanisms confer drug resistance to mitoxantrone in the human 8226 myeloma cell line.Q40968389
Human P-glycoprotein exhibits reduced affinity for substrates during a catalytic transition stateQ41043571
Correlation between steady-state ATP hydrolysis and vanadate-induced ADP trapping in Human P-glycoprotein. Evidence for ADP release as the rate-limiting step in the catalytic cycle and its modulation by substratesQ42497379
Drug-stimulatable ATPase activity in crude membranes of human MDR1-transfected mammalian cellsQ42827076
P-Glycoprotein and Breast Cancer Resistance Protein Affect Disposition of Tandutinib, A Tyrosine Kinase InhibitorQ42952483
European development of clofarabine as treatment for older patients with acute myeloid leukemia considered unsuitable for intensive chemotherapyQ43102335
Concomitant ABCG2 overexpression and FLT3-ITD mutation identify a subset of acute myeloid leukemia patients at high risk of relapseQ43797937
Phase 3 study of the multidrug resistance modulator PSC-833 in previously untreated patients 60 years of age and older with acute myeloid leukemia: Cancer and Leukemia Group B Study 9720.Q44083625
Prognostic significance of activating FLT3 mutations in younger adults (16 to 60 years) with acute myeloid leukemia and normal cytogenetics: a study of the AML Study Group Ulm.Q44189526
Proof without prejudice: use of the Kolmogorov-Smirnov test for the analysis of histograms from flow systems and other sourcesQ44578925
The expression of P-glycoprotein in AML cells with FLT3 internal tandem duplications is associated with reduced apoptosis in response to FLT3 inhibitorsQ45072250
Breast cancer resistance protein and P-glycoprotein in 149 adult acute myeloid leukemiasQ45178457
Salvage chemotherapy regimens for acute myeloid leukemia: Is one better? Efficacy comparison between CLAG and MEC regimens.Q46531521
The value of the MDR1 reversal agent PSC-833 in addition to daunorubicin and cytarabine in the treatment of elderly patients with previously untreated acute myeloid leukemia (AML), in relation to MDR1 status at diagnosisQ46580597
P275copyright licenseCreative Commons Attribution 4.0 InternationalQ20007257
P6216copyright statuscopyrightedQ50423863
P433issue8
P407language of work or nameEnglishQ1860
P921main subjectpharmacologyQ128406
quizartinibQ7272714
P304page(s)e71266
P577publication date2013-01-01
P1433published inPLOS OneQ564954
P1476titleThe FLT3 inhibitor quizartinib inhibits ABCG2 at pharmacologically relevant concentrations, with implications for both chemosensitization and adverse drug interactions
P478volume8

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cites work (P2860)
Q39049159ABCG2/BCRP: Specific and Nonspecific Modulators.
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Q41172549Coexpression of Multiple ABC-Transporters is Strongly Associated with Treatment Response in Childhood Acute Myeloid Leukemia
Q54977469Flt3 Regulation in the Mononuclear Phagocyte System Promotes Ocular Neovascularization.
Q35940547Gold nanoparticles enhance the effect of tyrosine kinase inhibitors in acute myeloid leukemia therapy.
Q92485655Practical Considerations for Treatment of Relapsed/Refractory FLT3-ITD Acute Myeloid Leukaemia with Quizartinib: Illustrative Case Reports
Q48263650Preventing chemotherapy-induced myelosuppression by repurposing the FLT3 inhibitor quizartinib.
Q47139045Quizartinib (AC220) reverses ABCG2-mediated multidrug resistance: In vitro and in vivo studies
Q33688129Role of NF-E2 related factor 2 (Nrf2) on chemotherapy resistance in acute myeloid leukemia (AML) and the effect of pharmacological inhibition of Nrf2
Q48371869The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations

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