The Pim kinase inhibitor SGI-1776 decreases cell surface expression of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and drug transport by Pim-1-dependent and -independent mechanisms

scientific article published on 19 December 2012

The Pim kinase inhibitor SGI-1776 decreases cell surface expression of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and drug transport by Pim-1-dependent and -independent mechanisms is …
instance of (P31):
scholarly articleQ13442814

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P356DOI10.1016/J.BCP.2012.12.006
P932PMC publication ID3821043
P698PubMed publication ID23261525

P2093author name stringMaria R Baer
Zhe-Sheng Chen
Suresh V Ambudkar
Mehmet Burcu
Suneet Shukla
Karthika Natarajan
Jasjeet Bhullar
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The pim-1 oncogene encodes two related protein-serine/threonine kinases by alternative initiation at AUG and CUGQ24311816
The 44 kDa Pim-1 kinase directly interacts with tyrosine kinase Etk/BMX and protects human prostate cancer cells from apoptosis induced by chemotherapeutic drugsQ24336934
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miR-328 functions as an RNA decoy to modulate hnRNP E2 regulation of mRNA translation in leukemic blastsQ30496174
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Overexpression of the ATP-binding cassette half-transporter, ABCG2 (Mxr/BCrp/ABCP1), in flavopiridol-resistant human breast cancer cellsQ32016277
Chemoprotection of hematopoietic cells by a mutant P-glycoprotein resistant to a potent chemosensitizer of multidrug-resistant cancersQ73563720
Evidence for the interaction of imatinib at the transport-substrate site(s) of the multidrug-resistance-linked ABC drug transporters ABCB1 (P-glycoprotein) and ABCG2Q80777899
Biochemical characterization of TAK-593, a novel VEGFR/PDGFR inhibitor with a two-step slow binding mechanismQ83016190
ABCB1 modulation does not circumvent drug extrusion from primitive leukemic progenitor cells and may preferentially target residual normal cells in acute myelogenous leukemiaQ83895091
Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pumpQ33204719
The prognostic value of P-glycoprotein (ABCB) and breast cancer resistance protein (ABCG2) in adults with de novo acute myeloid leukemia with normal karyotypeQ33243645
Comparison of ATP-binding cassette transporter interactions with the tyrosine kinase inhibitors imatinib, nilotinib, and dasatinibQ33566582
Pharmacologic inhibition of Pim kinases alters prostate cancer cell growth and resensitizes chemoresistant cells to taxanesQ33597393
Mitoxantrone, etoposide, and cytarabine with or without valspodar in patients with relapsed or refractory acute myeloid leukemia and high-risk myelodysplastic syndrome: a phase III trial (E2995)Q33758413
Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase includQ34118184
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
MicroRNA-16 is down-regulated in mutated FLT3 expressing murine myeloid FDC-P1 cells and interacts with Pim-1.Q34412520
Understanding polyspecificity of multidrug ABC transporters: closing in on the gaps in ABCB1Q35007411
Evidence for a requirement for ATP hydrolysis at two distinct steps during a single turnover of the catalytic cycle of human P-glycoproteinQ35076190
Mechanisms of cytotoxicity to Pim kinase inhibitor, SGI-1776, in acute myeloid leukemiaQ35125923
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
Pim kinase inhibitor, SGI-1776, induces apoptosis in chronic lymphocytic leukemia cellsQ37414714
The proto-oncogene Pim-1 is a target of miR-33aQ39509450
MicroRNA replacement therapy for miR-145 and miR-33a is efficacious in a model of colon carcinomaQ39521098
Breast cancer resistance protein and P-glycoprotein limit sorafenib brain accumulationQ39747662
Nilotinib (AMN107, Tasigna) reverses multidrug resistance by inhibiting the activity of the ABCB1/Pgp and ABCG2/BCRP/MXR transportersQ39854362
Brain accumulation of dasatinib is restricted by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by elacridar treatmentQ39874804
Constitutively activated FLT3 phosphorylates BAD partially through pim-1.Q40251345
The calcium channel blockers, 1,4-dihydropyridines, are substrates of the multidrug resistance-linked ABC drug transporter, ABCG2.Q40254927
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
Imatinib mesylate is a potent inhibitor of the ABCG2 (BCRP) transporter and reverses resistance to topotecan and SN-38 in vitroQ40571040
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
Pim-1 kinase protects P-glycoprotein from degradation and enables its glycosylation and cell surface expressionQ42163903
Addition of cyclosporin-A to chemotherapy in secondary (post-MDS) AML in the elderly. A multicenter randomized trial of the Leukemia Working Group of the Hellenic Society of Hematology.Q42678165
Drug-stimulatable ATPase activity in crude membranes of human MDR1-transfected mammalian cellsQ42827076
Discovery of imidazo[1,2-b]pyridazine derivatives as IKKβ inhibitors. Part 1: Hit-to-lead study and structure–activity relationshipQ42950439
P-Glycoprotein and Breast Cancer Resistance Protein Affect Disposition of Tandutinib, A Tyrosine Kinase InhibitorQ42952483
Benefit of cyclosporine modulation of drug resistance in patients with poor-risk acute myeloid leukemia: a Southwest Oncology Group studyQ43806484
Flow cytometric analysis of breast cancer resistance protein expression and function.Q44063189
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
Proof without prejudice: use of the Kolmogorov-Smirnov test for the analysis of histograms from flow systems and other sourcesQ44578925
P-glycoprotein-mediated drug efflux is a resistance mechanism of chronic myelogenous leukemia cells to treatment with imatinib mesylateQ44729076
Pheophorbide a is a specific probe for ABCG2 function and inhibition.Q44769964
Imidazo[1,2-b]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitorsQ44841683
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
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
Interleukin-5 regulates genes involved in B-cell terminal maturation.Q53606509
P433issue4
P407language of work or nameEnglishQ1860
P304page(s)514-524
P577publication date2012-12-19
P1433published inBiochemical PharmacologyQ864229
P1476titleThe Pim kinase inhibitor SGI-1776 decreases cell surface expression of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and drug transport by Pim-1-dependent and -independent mechanisms
P478volume85

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cites work (P2860)
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