Yehuda G Assaraf

Summary

Affiliation: Technion-Israel Institute of Technology
Country: Israel

Publications

  1. ncbi request reprint The role of multidrug resistance efflux transporters in antifolate resistance and folate homeostasis
    Yehuda G Assaraf
    The Fred Wyszkowski Cancer Research Laboratory, Department of Biology, Technion Israel Institute of Technology, Haifa, Israel
    Drug Resist Updat 9:227-46. 2006
  2. ncbi request reprint Molecular basis of antifolate resistance
    Yehuda G Assaraf
    The Fred Wyszkowski Cancer Research Laboratory, Department of Biology, Technion Israel Institute of Technology, Haifa, 32000, Israel
    Cancer Metastasis Rev 26:153-81. 2007
  3. ncbi request reprint Computer modelling of antifolate inhibition of folate metabolism using hybrid functional petri nets
    Yehuda G Assaraf
    Department of Biology, The Technion Israel Institute of Technology, Technion, Haifa 32000, Israel
    J Theor Biol 240:637-47. 2006
  4. doi request reprint A novel loss-of-function mutation in the proton-coupled folate transporter from a patient with hereditary folate malabsorption reveals that Arg 113 is crucial for function
    Inbal Lasry
    The Fred Wyszkowski Cancer Research Laboratory, Department of Biology, Technion Israel Institute of Technology, Haifa, Israel
    Blood 112:2055-61. 2008
  5. ncbi request reprint Mutant Gly482 and Thr482 ABCG2 mediate high-level resistance to lipophilic antifolates
    Eran Bram
    Department of Biology, Technion Israel Institute of Technology, 32000, Haifa, Israel
    Cancer Chemother Pharmacol 58:826-34. 2006
  6. ncbi request reprint Coexistence of multiple mechanisms of PT523 resistance in human leukemia cells harboring 3 reduced folate carrier alleles: transcriptional silencing, inactivating mutations, and allele loss
    Yotam Kaufman
    Department of Biology, Technion Israel Institute of Technology, Haifa 32000, Israel
    Blood 107:3288-94. 2006
  7. ncbi request reprint ABCG2 harboring the Gly482 mutation confers high-level resistance to various hydrophilic antifolates
    Assaf Shafran
    Department of Biology, Technion Israel Institute of Technology, Haifa, Israel
    Cancer Res 65:8414-22. 2005
  8. ncbi request reprint Impaired CREB-1 phosphorylation in antifolate-resistant cell lines with down-regulation of the reduced folate carrier gene
    Lilah Rothem
    Department of Biology, The Technion Israel Institute of Technology, Haifa, 32000, Israel
    Mol Pharmacol 66:1536-43. 2004
  9. ncbi request reprint Loss of Sp1 function via inhibitory phosphorylation in antifolate-resistant human leukemia cells with down-regulation of the reduced folate carrier
    Michal Stark
    Department of Biology, Technion Israel Institute of Technology, Haifa 32000, Israel
    Blood 107:708-15. 2006
  10. ncbi request reprint Loss of folylpoly-gamma-glutamate synthetase activity is a dominant mechanism of resistance to polyglutamylation-dependent novel antifolates in multiple human leukemia sublines
    Esti Liani
    Department of Biology, The Technion, Haifa, Israel
    Int J Cancer 103:587-99. 2003

Collaborators

Detail Information

Publications57

  1. ncbi request reprint The role of multidrug resistance efflux transporters in antifolate resistance and folate homeostasis
    Yehuda G Assaraf
    The Fred Wyszkowski Cancer Research Laboratory, Department of Biology, Technion Israel Institute of Technology, Haifa, Israel
    Drug Resist Updat 9:227-46. 2006
    ....
  2. ncbi request reprint Molecular basis of antifolate resistance
    Yehuda G Assaraf
    The Fred Wyszkowski Cancer Research Laboratory, Department of Biology, Technion Israel Institute of Technology, Haifa, 32000, Israel
    Cancer Metastasis Rev 26:153-81. 2007
    ....
  3. ncbi request reprint Computer modelling of antifolate inhibition of folate metabolism using hybrid functional petri nets
    Yehuda G Assaraf
    Department of Biology, The Technion Israel Institute of Technology, Technion, Haifa 32000, Israel
    J Theor Biol 240:637-47. 2006
    ..Surprisingly, pemetrexed failed to inhibit DHFR even at high concentrations. This HFPN-based simulation offers an inexpensive, user-friendly, rapid and reliable means of pre-clinical evaluation of the inhibitory profiles of antifolates...
  4. doi request reprint A novel loss-of-function mutation in the proton-coupled folate transporter from a patient with hereditary folate malabsorption reveals that Arg 113 is crucial for function
    Inbal Lasry
    The Fred Wyszkowski Cancer Research Laboratory, Department of Biology, Technion Israel Institute of Technology, Haifa, Israel
    Blood 112:2055-61. 2008
    ..These findings establish a novel loss of function mutation in HFM residing in an intracellular loop of PCFT crucial for folate transport...
  5. ncbi request reprint Mutant Gly482 and Thr482 ABCG2 mediate high-level resistance to lipophilic antifolates
    Eran Bram
    Department of Biology, Technion Israel Institute of Technology, 32000, Haifa, Israel
    Cancer Chemother Pharmacol 58:826-34. 2006
    ..The potential implications to cancer chemotherapy as well as the mechanism of anticancer drug extrusion by these mutant exporters are discussed...
  6. ncbi request reprint Coexistence of multiple mechanisms of PT523 resistance in human leukemia cells harboring 3 reduced folate carrier alleles: transcriptional silencing, inactivating mutations, and allele loss
    Yotam Kaufman
    Department of Biology, Technion Israel Institute of Technology, Haifa 32000, Israel
    Blood 107:3288-94. 2006
    ....
  7. ncbi request reprint ABCG2 harboring the Gly482 mutation confers high-level resistance to various hydrophilic antifolates
    Assaf Shafran
    Department of Biology, Technion Israel Institute of Technology, Haifa, Israel
    Cancer Res 65:8414-22. 2005
    ..These results provide the first evidence that the G482-ABCG2 mutation confers high-level resistance to various hydrophilic antifolates...
  8. ncbi request reprint Impaired CREB-1 phosphorylation in antifolate-resistant cell lines with down-regulation of the reduced folate carrier gene
    Lilah Rothem
    Department of Biology, The Technion Israel Institute of Technology, Haifa, 32000, Israel
    Mol Pharmacol 66:1536-43. 2004
    ....
  9. ncbi request reprint Loss of Sp1 function via inhibitory phosphorylation in antifolate-resistant human leukemia cells with down-regulation of the reduced folate carrier
    Michal Stark
    Department of Biology, Technion Israel Institute of Technology, Haifa 32000, Israel
    Blood 107:708-15. 2006
    ..These findings provide the first evidence that loss of RFC gene expression in antifolate-resistant cells is associated with an inhibitory Sp1 phosphorylation that can be eliminated by a cGMP-dependent activation of PP2A...
  10. ncbi request reprint Loss of folylpoly-gamma-glutamate synthetase activity is a dominant mechanism of resistance to polyglutamylation-dependent novel antifolates in multiple human leukemia sublines
    Esti Liani
    Department of Biology, The Technion, Haifa, Israel
    Int J Cancer 103:587-99. 2003
    ....
  11. ncbi request reprint Folate deprivation results in the loss of breast cancer resistance protein (BCRP/ABCG2) expression. A role for BCRP in cellular folate homeostasis
    Ilan Ifergan
    Department of Biology, The Technion, Haifa 32000, Israel
    J Biol Chem 279:25527-34. 2004
    ..This is the first evidence for the possible role of BCRP in the maintenance of cellular folate homeostasis...
  12. ncbi request reprint Alterations in the expression of transcription factors and the reduced folate carrier as a novel mechanism of antifolate resistance in human leukemia cells
    Lilah Rothem
    Department of Biology, The Rappaport Institute for Research in the Medical Sciences and the B Rappaport Faculty of Medicine, The Technion Israel Institute of Technology, Haifa 31096, Israel
    J Biol Chem 278:8935-41. 2003
    ..These results establish a novel mechanism of antifolate resistance that is based on altered expression and function of transcription factors resulting in transcriptional silencing of the hRFC promoter...
  13. ncbi request reprint Reduced folate carrier gene silencing in multiple antifolate-resistant tumor cell lines is due to a simultaneous loss of function of multiple transcription factors but not promoter methylation
    Lilah Rothem
    Department of Biology, The Technion Israel Institute of Technology, Haifa 32000, Israel
    J Biol Chem 279:374-84. 2004
    ....
  14. pmc Chemotherapeutic drug-induced ABCG2 promoter demethylation as a novel mechanism of acquired multidrug resistance
    Eran E Bram
    The Fred Wyszkowski Cancer Research Laboratory, Department of Biology, Technion Israel Institute of Technology, Haifa, Israel
    Neoplasia 11:1359-70. 2009
    ..These findings have important implications for the emergence, clonal selection, and expansion of malignant cells with the MDR phenotype during chemotherapy...
  15. ncbi request reprint Reduced folate carrier mutations are not the mechanism underlying methotrexate resistance in childhood acute lymphoblastic leukemia
    Yotam Kaufman
    Department of Biology, The Technion, Haifa, Israel
    Cancer 100:773-82. 2004
    ..Impaired drug transport is a documented mechanism of MTX resistance in patients with ALL; however, to the authors' knowledge it is not known whether inactivating RFC mutations are a contributing factor...
  16. ncbi request reprint C421 allele-specific ABCG2 gene amplification confers resistance to the antitumor triazoloacridone C-1305 in human lung cancer cells
    Eran E Bram
    The Fred Wyszkowski Cancer Research Laboratory, Faculty of Biology, Technion Israel Institute of Technology, Haifa 32000, Israel
    Biochem Pharmacol 74:41-53. 2007
    ..These findings have important implications for the selection and expansion of malignant anticancer drug resistant clones during chemotherapy with ABCG2 drugs...
  17. doi request reprint Structural determinants of imidazoacridinones facilitating antitumor activity are crucial for substrate recognition by ABCG2
    Eran E Bram
    The Fred Wyszkowski Cancer Research Laboratory, Department of Biology, Technion Israel Institute of Technology, Haifa 32000, Israel
    Mol Pharmacol 75:1149-59. 2009
    ..The possible clinical implications for the future design of novel acridines that overcome ABCG2-dependent multidrug resistance are discussed...
  18. ncbi request reprint Targeting an extracellular epitope of the human multidrug resistance protein 1 (MRP1) in malignant cells with a novel recombinant single chain Fv antibody
    Liat Binyamin
    Department of Biology, Technion Israel Institute of Technology, Technion City, Room 333, Haifa 32000, Israel
    Int J Cancer 110:882-90. 2004
    ..These novel small Fv-based recombinant antibodies that possess superior tumor penetration capabilities may possibly be used to selectively target drugs or tumor cells that express MRP-1...
  19. pmc The reduced folate carrier (RFC) is cytotoxic to cells under conditions of severe folate deprivation. RFC as a double edged sword in folate homeostasis
    Ilan Ifergan
    The Fred Wyszkowski Cancer Research Laboratory, Department of Biology, Technion Israel Institute of Technology, Haifa, Israel
    J Biol Chem 283:20687-95. 2008
    ..Hence down-regulation of RFC and GGH may serve as a novel adaptive response to severe folate deficiency...
  20. ncbi request reprint Probing ATP-dependent conformational changes in the multidrug resistance protein 1 (MRP1/ABCC1) in live tumor cells with a novel recombinant single-chain Fv antibody targeted to the extracellular N-terminus
    Liat Binyamin
    Department of Biology, Technion, Haifa, Israel
    Int J Cancer 116:703-9. 2005
    ..Furthermore, although ATP binding occurs in the cytosolic nucleotide binding domains of MRP1, significant conformational changes are apparently propagated to the N-terminus residing at the extracellular compartment...
  21. pmc Overcoming multidrug resistance via photodestruction of ABCG2-rich extracellular vesicles sequestering photosensitive chemotherapeutics
    Vicky Goler-Baron
    The Fred Wyszkowski Cancer Research Laboratory, Department of Biology, Technion Israel Institute of Technology, Haifa, Israel
    PLoS ONE 7:e35487. 2012
    ..Thus, MDR modalities including ABCG2-dependent drug sequestration within EVs can be rationally converted to a pharmacologically lethal Trojan horse to selectively eradicate MDR cancer cells...
  22. doi request reprint Hereditary folate malabsorption: a positively charged amino acid at position 113 of the proton-coupled folate transporter (PCFT/SLC46A1) is required for folic acid binding
    Inbal Lasry
    The Fred Wyszkowski Cancer Research Laboratory, Dept of Biology, Technion Israel Institute of Technology, Haifa 32000, Israel
    Biochem Biophys Res Commun 386:426-31. 2009
    ..These findings constitute the first demonstration that a basic amino acid at position 113 is required for folate substrate binding...
  23. doi request reprint Beta-casein nanoparticles as an oral delivery system for chemotherapeutic drugs: impact of drug structure and properties on co-assembly
    Alina Shapira
    Russell Berrie Nanotechnology Institute, Technion Israel Institute of Technology, Haifa 32000, Israel
    Pharm Res 27:2175-86. 2010
    ..The efficient gastric digestibility of β-CN suggests possible targeting to gastric cancers...
  24. ncbi request reprint Cytoplasmic confinement of breast cancer resistance protein (BCRP/ABCG2) as a novel mechanism of adaptation to short-term folate deprivation
    Ilan Ifergan
    Department of Biology, Technion Israel Institute of Technology, Haifa 32000, Israel
    Mol Pharmacol 67:1349-59. 2005
    ..These results constitute a novel mechanism of cellular adaptation to short-term folate deprivation and provide further support to the possible role of BCRP in the maintenance of cellular folate homeostasis...
  25. ncbi request reprint Antifolate resistance associated with loss of MRP1 expression and function in Chinese hamster ovary cells with markedly impaired export of folate and cholate
    Michal Stark
    Department of Biology, The Technion Israel Institute of Technology, Haifa 32000, Israel
    Mol Pharmacol 64:220-7. 2003
    ..The data also suggest that MRP1, and possibly other MRPs that transport folates, can play a role in the maintenance of cellular folate homeostasis...
  26. ncbi request reprint Disruption of transport activity in a D93H mutant thiamine transporter 1, from a Rogers Syndrome family
    Dana Baron
    Department of Molecular Genetics, The Rappaport Institute for Research in the Medical Sciences and the B Rappaport Faculty of Medicine, Haifa, Israel
    Eur J Biochem 270:4469-77. 2003
    ..Hence, this functional characterization of the D93H mutation provides a molecular basis for Rogers syndrome...
  27. pmc The obligatory intestinal folate transporter PCFT (SLC46A1) is regulated by nuclear respiratory factor 1
    Nitzan Gonen
    Fred Wyszkowski Cancer Research Laboratory, Faculty of Biology, Technion Israel Institute of Technology, Haifa 32000, Israel
    J Biol Chem 285:33602-13. 2010
    ..The implications of this linkage between folate transport and metabolism with mitochondria biogenesis and respiration are discussed...
  28. ncbi request reprint The reduced folate carrier gene is a novel selectable marker for recombinant protein overexpression
    Lilah Rothem
    Department of Biology, Technion Israel Institute of Technology, Haifa 32000, Israel
    Mol Pharmacol 68:616-24. 2005
    ..Furthermore, the possible implications to subcellular transporter localization and restoration of MTX sensitivity in drug-resistant tumors by RFC-based gene therapy are discussed...
  29. doi request reprint Riboflavin concentration within ABCG2-rich extracellular vesicles is a novel marker for multidrug resistance in malignant cells
    Ilan Ifergan
    The Fred Wyszkowski Cancer Research Lab, Department of Biology, Technion Israel Institute of Technology, Haifa 32000, Israel
    Biochem Biophys Res Commun 380:5-10. 2009
    ..e. based on vitamin accumulation) functional marker for the quantification of the levels of MDR mediated by ABCG2-rich extracellular vesicles in multiple malignant cells...
  30. doi request reprint Aberrant splicing of folylpolyglutamate synthetase as a novel mechanism of antifolate resistance in leukemia
    Michal Stark
    The Fred Wyszkowski Cancer Research Laboratory, Department of Biology, Rambam Medical Center, and Rappaport Facultyof Medicine, Technion Israel Institute of Technology, Haifa, Israel
    Blood 113:4362-9. 2009
    ..The clinical ramifications of these novel findings are discussed...
  31. ncbi request reprint Novel extracellular vesicles mediate an ABCG2-dependent anticancer drug sequestration and resistance
    Ilan Ifergan
    Department of Biology, Technion Israel Institute of Technology, Haifa, Israel
    Cancer Res 65:10952-8. 2005
    ..This constitutes a novel modality of anticancer drug resistance...
  32. doi request reprint Beta-casein-based nanovehicles for oral delivery of chemotherapeutic drugs: drug-protein interactions and mitoxantrone loading capacity
    Alina Shapira
    Russell Berrie Nanotechnology Institute, Technion, Israel Institute of Technology, Haifa, Israel
    Nanomedicine 6:547-55. 2010
    ..This study investigates the basic properties of a mitoxantrone delivery system based on the above principles...
  33. ncbi request reprint Loss of multidrug resistance protein 1 expression and folate efflux activity results in a highly concentrative folate transport in human leukemia cells
    Yehuda G Assaraf
    Department of Biology, The Technion, Haifa 32000, Israel
    J Biol Chem 278:6680-6. 2003
    ..These findings suggest a functional role for MRP1 in the maintenance of cellular folate homeostasis...
  34. doi request reprint Functional elements in the minimal promoter of the human proton-coupled folate transporter
    Michal Stark
    Dept of Biology, Technion Israel Institute of Technology, Haifa, Israel
    Biochem Biophys Res Commun 388:79-85. 2009
    ..This is the first functional identification of the minimal PCFT promoter harboring crucial GC-box elements that markedly contribute to its transcriptional activation via putative interaction with distal YY1 and AP1 enhancer elements...
  35. doi request reprint Nanomedicine for targeted cancer therapy: towards the overcoming of drug resistance
    Alina Shapira
    Russell Berrie Nanotechnology Institute, Technion, Haifa, Israel
    Drug Resist Updat 14:150-63. 2011
    ..This targeted strategy holds promise in paving the way for the introduction of highly effective nanoscopic vehicles for cancer therapeutics while overcoming drug resistance...
  36. ncbi request reprint Reduced folate carrier protein expression in osteosarcoma: implications for the prediction of tumor chemosensitivity
    Ilan Ifergan
    Department of Biology, The Technion, Haifa, Israel
    Cancer 98:1958-66. 2003
    ..Although MTX uptake proceeds primarily through the reduced folate carrier (RFC) protein and efflux occurs via multidrug resistance protein 1 (MRP1), RFC protein expression in osteosarcoma remains unexamined...
  37. doi request reprint β-Casein nanoparticle-based oral drug delivery system for potential treatment of gastric carcinoma: stability, target-activated release and cytotoxicity
    Alina Shapira
    Russell Berrie Nanotechnology Institute, Technion, Israel Institute of Technology, Haifa, Israel
    Eur J Pharm Biopharm 80:298-305. 2012
    ..We conclude that β-CN shows promise to be useful for target-activated oral delivery of hydrophobic chemotherapeutics in the treatment of gastric carcinoma, one of the leading causes of cancer mortality worldwide...
  38. doi request reprint Molecular mechanisms of adaptation to folate deficiency
    Ilan Ifergan
    Department of Biology, Technion Israel Institute of Technology, Haifa 32000, Israel
    Vitam Horm 79:99-143. 2008
    ..Moreover, the intricate interplay between various components of the adaptive response to folate deprivation is also discussed...
  39. doi request reprint PCFT/SLC46A1 promoter methylation and restoration of gene expression in human leukemia cells
    Nitzan Gonen
    The Fred Wyszkowski Cancer Research Laboratory, Department of Biology, Technion Israel Institute of Technology, Haifa 32000, Israel
    Biochem Biophys Res Commun 376:787-92. 2008
    ..The potential translational implications of the restoration of PCFT expression in chemotherapy of leukemia are discussed...
  40. pmc A dominant negative heterozygous G87R mutation in the zinc transporter, ZnT-2 (SLC30A2), results in transient neonatal zinc deficiency
    Inbal Lasry
    The Fred Wyszkowski Cancer Research Laboratory, Department of Biology, Technion Israel Institute of Technology, Haifa 32000, Israel
    J Biol Chem 287:29348-61. 2012
    ..These findings establish that inactivating ZnT-2 mutations are an underlying basis of TNZD and provide the first evidence for the dominant inheritance of heterozygous ZnT-2 mutations via negative dominance due to homodimer formation...
  41. pmc Structure and function of ABCG2-rich extracellular vesicles mediating multidrug resistance
    Vicky Goler-Baron
    The Fred Wyszkowski Cancer Research Laboratory, Department of Biology, Technion Israel Institute of Technology, Haifa, Israel
    PLoS ONE 6:e16007. 2011
    ..We propose a composite model for the structure and function of MDR pump-rich EVs in cancer cells and their ability to confer multiple anticancer drug resistance...
  42. doi request reprint Antifolates in cancer therapy: structure, activity and mechanisms of drug resistance
    Nitzan Gonen
    The Fred Wyszkowski Cancer Research Laboratory, Faculty of Biology, Technion Israel Institute of Technology, Haifa 32000, Israel
    Drug Resist Updat 15:183-210. 2012
    ..g. BGC 945). Hence, targeting mechanisms of antifolate-resistance could facilitate the development of rationally-based novel antifolates and strategies that overcome chemoresistance...
  43. doi request reprint Inhibition of the PI3K-Akt signaling pathway disrupts ABCG2-rich extracellular vesicles and overcomes multidrug resistance in breast cancer cells
    Vicky Goler-Baron
    The Fred Wyszkowski Cancer Research Laboratory, Department of Biology, Technion Israel Institute of Technology, Haifa 32000, Israel
    Biochem Pharmacol 83:1340-8. 2012
    ..We propose that Akt signaling inhibitors which disrupt ABCG2 targeting and EVs biogenesis may readily overcome MDR thus warranting in vivo studies with these promising drug combinations...
  44. doi request reprint Host-defense peptide mimicry for novel antitumor agents
    Viktoria Held-Kuznetsov
    Department of Biotechnology and Food Engineering, Technion, Haifa 32000, Israel
    FASEB J 23:4299-307. 2009
    ..Collectively, the current findings establish the potential of an HDP-mimetic approach for developing simplified yet robust antitumor agents that bear a key advantage of overcoming MDR phenomena...
  45. pmc Heterogeneous nuclear ribonucleoprotein H1/H2-dependent unsplicing of thymidine phosphorylase results in anticancer drug resistance
    Michal Stark
    The Fred Wyszkowski Cancer Research Laboratory, Technion Israel Institute of Technology, Haifa 32000, Israel
    J Biol Chem 286:3741-54. 2011
    ..Thus, this is the first study identifying altered function of hnRNP H1/H2 in tumor cells as a novel determinant of aberrant TP splicing thereby resulting in acquired chemoresistance to TP-activated fluoropyrimidine anticancer drugs...
  46. pmc Resistance to multiple novel antifolates is mediated via defective drug transport resulting from clustered mutations in the reduced folate carrier gene in human leukaemia cell lines
    Lilah Rothem
    Department of Biology, The Technion, Haifa 32000, Israel
    Biochem J 367:741-50. 2002
    ..This is the first molecular characterization of human RFC-associated modalities of resistance to various novel antifolates in multiple leukaemia sublines...
  47. ncbi request reprint Disruption of P-glycoprotein anticancer drug efflux activity by a small recombinant single-chain Fv antibody fragment targeted to an extracellular epitope
    Maya Haus-Cohen
    Department of Biology, Technion Israel Institute of Technology, Technion City, Haifa 32000, Israel
    Int J Cancer 109:750-8. 2004
    ..Hence, these small recombinant antibody fragments may be applied in combination chemotherapy to overcome MDR in various human cancers...
  48. doi request reprint Beta-casein nanovehicles for oral delivery of chemotherapeutic drugs
    Alina Shapira
    Russell Berrie Nanotechnology Institute, Technion, Israel Institute of Technology, Haifa, Israel
    Nanomedicine 6:119-26. 2010
    ..beta-CN nanoparticles may serve as effective oral-delivery nanovehicles for solubilization and stabilization of hydrophobic drugs, as demonstrated in this study utilizing methotrexate...
  49. pmc Lack of plasma membrane targeting of a G172D mutant thiamine transporter derived from Rogers syndrome family
    Dana Baron
    Department of Molecular Genetics, The Rappaport Institute for Research in the Medical Sciences and the B Rappaport Faculty of Medicine, The Technion Israel Institute of Technology, Haifa, Israel
    Mol Med 8:462-74. 2002
    ..The gene associated with Rogers syndrome encodes for a plasma membrane thiamine transporter, THTR-1, a member of the solute carrier family that includes its homologue THTR-2 and the reduced folate carrier...
  50. ncbi request reprint The role of multidrug resistance proteins MRP1, MRP2 and MRP3 in cellular folate homeostasis
    Jan Hendrik Hooijberg
    Department of Pediatric Hematology Oncology, VU University Medical Center VUmc, De Boelelaan 1117, 1007 MB, Amsterdam, The Netherlands
    Biochem Pharmacol 65:765-71. 2003
    ..These results suggest that down- and up-regulation of MRP1 (and MRP3) expression can influence cellular folate homeostasis, in particular when cellular retention by polyglutamylation of folates is attenuated...
  51. ncbi request reprint Folate concentration dependent transport activity of the Multidrug Resistance Protein 1 (ABCC1)
    Jan Hendrik Hooijberg
    Department of Pediatric Hematology Oncology, VU University Medical Center VUmc, De Boelelaan 1117, 1007 MB, Amsterdam, The Netherlands
    Biochem Pharmacol 67:1541-8. 2004
    ..These results have potentially important implications in the understanding of the (patho-)physiological roles of MRP1/ABCC1, and possibly other ABC transporter proteins in cellular folate homeostasis and drug resistance...
  52. ncbi request reprint Multiple mechanisms of resistance to methotrexate and novel antifolates in human CCRF-CEM leukemia cells and their implications for folate homeostasis
    Robert Mauritz
    Department of Medical Oncology, VU Medical Center, Amsterdam, The Netherlands
    Biochem Pharmacol 63:105-15. 2002
    ....
  53. ncbi request reprint Sulfasalazine is a potent inhibitor of the reduced folate carrier: implications for combination therapies with methotrexate in rheumatoid arthritis
    Gerrit Jansen
    Department of Rheumatology, Vrije Universiteit Medisch Centrum, Amsterdam, The Netherlands
    Arthritis Rheum 50:2130-9. 2004
    ....
  54. ncbi request reprint Disparate mechanisms of antifolate resistance provoked by methotrexate and its metabolite 7-hydroxymethotrexate in leukemia cells: implications for efficacy of methotrexate therapy
    Kambiz Fotoohi
    Department of Oncology and Pathology, Cancer Center Karolinska CCK, Karolinska University Hospital, 171 76 Stockholm, Sweden
    Blood 104:4194-201. 2004
    ..The implications of this finding for MTX efficacy and strategies to circumvent MTX resistance are discussed...
  55. ncbi request reprint Acquired resistance to chloroquine in human CEM T cells is mediated by multidrug resistance-associated protein 1 and provokes high levels of cross-resistance to glucocorticoids
    Ruud Oerlemans
    VU University Medical Center, Amsterdam, The Netherlands
    Arthritis Rheum 54:557-68. 2006
    ..To explore the onset and molecular mechanism of resistance to the antimalarial disease-modifying antirheumatic drug (DMARD) chloroquine (CQ) in human CEM T cells...
  56. ncbi request reprint Sulfasalazine down-regulates the expression of the angiogenic factors platelet-derived endothelial cell growth factor/thymidine phosphorylase and interleukin-8 in human monocytic-macrophage THP1 and U937 cells
    Michiel de Bruin
    Department of Medical Oncology, VU University Medical Center, De Boelelaan 1117, 1081 HV Amsterdam, The Netherlands
    Mol Pharmacol 66:1054-60. 2004
    ..However, this may also negatively affect capecitabine efficacy...
  57. doi request reprint Molecular basis of bortezomib resistance: proteasome subunit beta5 (PSMB5) gene mutation and overexpression of PSMB5 protein
    Ruud Oerlemans
    Department of Rheumatology, VUMC Institute for Cancer and Immunology, VU University Medical Center, Amsterdam, The Netherlands
    Blood 112:2489-99. 2008
    ..Collectively, these findings establish a novel mechanism of bortezomib resistance associated with the selective overexpression of a mutant PSMB5 protein...