Publications of lab members: (last update 6/4/09)

  1. Bram, E.E., Adar, Y., Mesika, N., Sabisz, M., Skladanowski, A. and Assaraf, Y.G. (2009)  Mol Pharmacol. 2009 Mar 3. [Epub ahead of print]. Pub Med

  2. Ifergan, I., Goler-Baron, V. and Assaraf, Y.G. (2009) Riboflavin concentration within ABCG2-rich extracellular vesicles is a novel marker for multidrug resistance in malignant cells. Biochem Biophys Res Commun. 380: 5-10.Pub Med

  3. Stark, M., Wichman, C., Avivi, I. and Assaraf, Y.G. (2009) Aberrant splicing of folylpolyglutamate synthetase as a novel mechanism of antifolate resistance in leukemia.  Blood. 2009 Jan 8. [Epub ahead of print].Pub Med

  4. Gonen, N., Bram, E.E. and Assaraf, Y.G. (2008) PCFT/SLC46A1 promoter methylation and restoration of gene expression in human leukemia cells. Biochem Biophys Res Commun. 376: 787-792.Pub Med

  5. Lasry, I., Berman, B., Straussberg, R., Sofer, Y., Bessler, H., Sharkia, M., Glaser, F., Jansen, G., Drori, S. and Assaraf, Y.G. (2008) 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. Blood. 112: 2055-2061.Pub Med

  6. Ifergan, I., Jansen, G. and Assaraf, Y.G. (2008) The reduced folate carrier (RFC) is cytotoxic to cells under conditions of severe folate deprivation: RFC as a double-edged sword in folate homeostasis. J Biol Chem. [Epub ahead of print]. Pub Med

  7. Bram, E., Ifergan, I., Grimberg, M., Lemke, K., Skladanowski, A., and Assaraf, Y.G. (2007) C421 allele-specific ABCG2 gene amplification confers resistance to the antitumor triazoloacridone C-1305 in human lung cancer cells. Biochem Pharmacol. 74: 41-53. Pub Med

  8. Bram, E., Ifergan, I., Shafran, A., Berman, B., Jansen, G., and Assaraf, Y.G. (2006) Mutant Gly482 and Thr482 ABCG2 mediate high-level resistance to lipophilic antifolates. Cancer Chemother Pharmacol. 58: 826-834.Pub Med

  9. Kaufman, Y., Ifergan, I., Rothem, L., Jansen, G., and Assaraf, Y.G. (2006) Coexistence of multiple mechanisms of PT523 resistance in human leukemia cells harboring 3 reduced folate carrier alleles: transcriptional silencing, inactivating mutations, and allele loss. Blood. 107: 3288-3294. Pub Med

  10. Stark, M., and Assaraf, Y.G. (2006) Loss of Sp1 function via inhibitory phosphorylation in antifolate-resistant human leukemia cells with down-regulation of the reduced folate carrier. Blood. 107: 708-715. Pub Med

  11. Ifergan, I., Scheffer, G.L., and Assaraf, Y.G. (2005) Novel extracellular vesicles mediate an ABCG2-dependent anticancer drug sequestration and resistance. Cancer Res. 65: 10952-10958.Pub Med

  12. Shafran, A., Ifergan, I., Bram, E., Jansen, G., Kathmann, I., Peters, G.J., Robey, R.W., Bates, S.E., and Assaraf, Y.G. (2005) ABCG2 harboring the Gly482 mutation confers high level resistance to various antifolates.  Cancer Res. 65: 8414-8422.Pub Med

  13. Rothem, L., Berman, B., Stark, M., Jansen, G., and Assaraf, Y.G. (2005) The reduced folate carrier gene is a novel selectable marker for recombinant protein overexpression. Mol Pharmacol. 68: 616-624.Pub Med

  14. Ifergan, I., Jansen, G., and Assaraf, Y.G. (2005) Cytoplasmic confinement of breast cancer resistance protein (BCRP/ABCG2) as a novel mechanism of adapation to short-term folate deprivation. Mol. Pharmacol. 67: 1349-1359.Pub Med

  15. Rothem, L.*, Stark, M.*, and Assaraf, Y.G. (2004) Impaired CREB-1 phosphorylation in antifolate-resistant cell lines with down regulation of the reduced folate carrier gene. Mol. Pharmacol. 66: 1536-1543. * Both authors equally contributed. Pub Med

  16. Ifergan, I., Shafran, A., Jansen, G., Hooijberg, J.H., Scheffer, G.L., and Assaraf, Y.G. (2004) Folate deprivation results in the loss of breast cancer resistance protein (ABCG2) expression: a role for BCRP in cellular folate homeostasis.  J. Biol. Chem. 279: 25527-25534.Pub Med

  17. Kaufman, Y., Drori, S., Cole, P.D., Kamen, B.A., Sirota, J., Ifergan, I., Rechavi, G., Toren, A., Weyl Ben-Arush, M., Elhasid, R., Sahar, D., Kaspers, G.J.L., Matherly, L.H., Jansen, G.,  and Assaraf, Y.G. (2004) Reduced folate carrier mutations are not the mechanism underlying methotrexate resistance in childhood acute lymphoblastic leukemia. Cancer 100: 773-782.Pub Med

  18. Rothem, L.*, Stark, M.*, Kaufman, Y., Mayo, L., and Assaraf, Y.G. (2004) 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. J. Biol. Chem. 279: 374-384. * Both authors equally contributed.Pub Med

  19. Ifergan, I., Meller, I., Issakov, J., and  Assaraf, Y.G.  (2003) Reduced folate carrier protein expression in osteosarcoma: implications for the prediction of tumor chemosensitivity. Cancer 98: 1958-1966.Pub Med

  20. Stark, M., Rothem, L., Scheffer, G.L.,  Jansen, G., Goldman, I.D.,  and Assaraf, Y.G. (2003) Antifolate resistance associated with loss of MRP1 expression and function in Chinese hamster ovary cells with markedly impaired export of folate and cholate. Mol. Pharmacol. 64: 220-227.Pub Med

  21. Rothem, L., Aronheim, A., and Assaraf, Y.G. (2003) Alterations in the expression of transcription factors and the reduced folate carrier as a novel mechanism of antifolate resistance in human leukemia cells. J. Biol. Chem. 278: 8935-8941.Pub Med

  22. Liani, E., Rothem, L., Bunni, M.A., Smith, C.A., Jansen, G., and Assaraf, Y.G. (2003) Loss of folylpoly-γ-glutamate synthetase activity is a dominant mechanism of resistance to polyglutamylation-dependent novel antifolates in multiple human leukemia sublines. Int. J. Cancer 103: 587-599.Pub Med

  23. Rothem, L., Ifergan, I., Kaufman, Y., Priest, D.G., Jansen, G., and Assaraf, Y.G. (2002) Resistance to multiple novel antifolates is mediated via defective drug transport resulting from clustered mutations in the reduced folate carrier gene in human leukemia cells. Biochem. J. 367: 741-750.Pub Med

  24. Drori, S., Jansen, G., Mauritz, R., Peters, G.J. and Assaraf, Y.G. (2000) Clustering of mutations in the first transmembrane domain of the human reduced folate carrier in GW1843U89–resistant leukemia cells with impaired antifolate transport and augmented folate uptake.  J. Biol. Chem. 275: 30855-30863.

  25. Drori, S., Sprecher, H., Shemer, G., Jansen, G., Goldman, I.D. and Assaraf, Y.G. (2000) Characterization of a human alternatively spliced truncated reduced folate carrier (RFC) increasing folate accumulation in parental leukemia cells. Eur. J. Biochem. 267: 690-702.

  26. Regev, R., Assaraf, Y.G., and Eytan, G.D.  (1999) Membrane fluidization by ether, other anesthetics, and certain agents abolishes P-glycoprotein ATPase activity and modulates efflux from multidrug resistant cells. Eur. J. Biochem. 259: 18-24.

  27. Eytan, G.D., Regev, R., Oren, G., Hurwitz, C. and Assaraf, Y.G. (1997) Efficiency of P-glycoprotein-mediated exclusion of rhodamine dyes from multidrug resistant cells is determined by their passive transmembrane movement rate.  Eur. J. Biochem. 248: 104-112.

  28. Eytan, G.D., Regev, R., Oren, G. and Assaraf, Y.G. (1996) The  role of passive transbilayer drug movement in multidrug resistance and its modulation. J. Biol. Chem. 271: 12897-12902.

  29. Eytan, G.D., Regev, R. and Assaraf, Y.G. (1996) Functional reconstitution of P-glycoprotein reveals an apparent near stoichiometric drug transport to ATP hydrolysis. J. Biol. Chem. 271: 3172-3178.

  30. Borgnia, M.J., Eytan, G.D. and Assaraf, Y.G. (1996) Competition of hydrophobic peptides, cytotoxic drugs and chemosensitizers on a common P-glycoprotein pharmacophore as revealed by its ATPase activity. J. Biol. Chem. 271: 3163-3171.

  31. Sprecher, H., Barr, H.M., Slotky, J.I., Tzukerman, M., Eytan, G.D. and Assaraf, Y.G. (1995) Alteration of mitochondrial gene expression and disruption of respiratory function by the lipophilic antifolate pyrimethamine in mammalian cells. J. Biol. Chem. 270: 20668-20676.

  32. Drori, S., Eytan, G.D. and Assaraf, Y.G., (1995) Potentiation of anticancer drug cytotoxicity by multidrug resistance chemosensitizers involves alterations in membrane fluidity leading to increased membrane permeability. Eur. J. Biochem. 228: 1020-1029.

  33. Eytan, G.D. Borgnia, M.J., Regev, R. and Assaraf, Y.G. (1994) Transport of polypeptide ionophores into proteoliposomes reconstituted with rat liver P-glycoprotein. J. Biol. Chem. 269: 26058-26065.

  34. Assaraf, Y.G. and Borgnia, M.J. (1994) Probing the interaction of the multidrug resistance phenotype with the polypeptide ionophore gramicidin D via functional channel formation. Eur. J. Biochem. 212: 813-824.

  35. Assaraf, Y.G., Drori, S., Bachrach, U. and Shaugan-Labay, V. (1994) Determination of multidrug resistance levels in cultured mammalian cells using ornithine decarboxylase activity. Anal. Biochem. 216: 97-109.

  36. Assaraf, Y.G. and Borgnia, M.J. (1993) Differential reversal of lipophilic antifolate resistance in mammalian cells with various modulators of the multidrug resistance phenotype. Anti-Cancer Drugs 4: 395-406.

  37. Assaraf, Y.G. and Slotky, J.I. (1993) Characterization of a lipophilic antifolate resistance provoked by treatment of mammalian cells with the antiparasitic agent pyrimethamine. J. Biol. Chem. 268: 4556-4566.