Stephen Howell

Summary

Affiliation: University of California
Country: USA

Publications

  1. pmc Regulation of Cisplatin cytotoxicity by cu influx transporters
    Paolo Abada
    Moores Cancer Center and Department of Medicine, University of California, San Diego, La Jolla, CA 92093, USA
    Met Based Drugs 2010:317581. 2010
  2. pmc Cisplatin induces resistance by triggering differentiation of testicular embryonal carcinoma cells
    Paolo B Abada
    Department of Medicine and the Moores UCSD Cancer Center, University of California San Diego, La Jolla, California, United States of America
    PLoS ONE 9:e87444. 2014
  3. pmc Copper transporter 2 regulates intracellular copper and sensitivity to cisplatin
    Carlos P Huang
    Moores UCSD Cancer Center, University of California, San Diego, 3855 Health Sciences Drive, La Jolla, CA 92093 0819, USA
    Metallomics 6:654-61. 2014
  4. pmc The role of metal binding and phosphorylation domains in the regulation of cisplatin-induced trafficking of ATP7B
    Roohangiz Safaei
    Moores Cancer Center, University of California, San Diego, 3855 Health Sciences Drive, La Jolla, CA 92093 0819, USA
    Metallomics 5:964-72. 2013
  5. pmc Targeting granzyme B to tumor cells using a yoked human chorionic gonadotropin
    Isao Kanatani
    Department of Medicine and the Rebecca and John Moores UCSD Cancer Center, University of California, San Diego, La Jolla, CA 92093 0819, USA
    Cancer Chemother Pharmacol 68:979-90. 2011
  6. pmc Preclinical efficacy studies of a novel nanoparticle-based formulation of paclitaxel that out-performs Abraxane
    Zhongling Feng
    Biogroup, Nitto Denko Technical Corporation, 501 Via Del Monte, Oceanside, CA 92058, USA
    Cancer Chemother Pharmacol 65:923-30. 2010
  7. pmc Pharmacokinetics and tissue distribution of PGG-paclitaxel, a novel macromolecular formulation of paclitaxel, in nu/nu mice bearing NCI-460 lung cancer xenografts
    Xinghe Wang
    Biogroup, Nitto Denko Technical Corporation, 501 Via Del Monte, Oceanside, CA 92058, USA
    Cancer Chemother Pharmacol 65:515-26. 2010
  8. pmc Challenges associated with the targeted delivery of gelonin to claudin-expressing cancer cells with the use of activatable cell penetrating peptides to enhance potency
    Xiaoqin Yuan
    Department of Medicine and Rebecca and John Moores UCSD Cancer Center, University of California San Diego, 3855 Health Sciences Drive, La Jolla, CA 92093 0819, USA
    BMC Cancer 11:61. 2011
  9. pmc Copper transporters and the cellular pharmacology of the platinum-containing cancer drugs
    Stephen B Howell
    Department of Medicine, Moores UCSD Cancer Center, 3855 Health Sciences Drive, La Jolla, CA 92093, USA
    Mol Pharmacol 77:887-94. 2010
  10. ncbi request reprint Resistance to apoptosis in prostate cancer cells
    S B Howell
    Department of Medicine and the Cancer Center, University of California, San Diego, La Jolla, California 92093, USA
    Mol Urol 4:225-9;discussion 231. 2000

Collaborators

Detail Information

Publications59

  1. pmc Regulation of Cisplatin cytotoxicity by cu influx transporters
    Paolo Abada
    Moores Cancer Center and Department of Medicine, University of California, San Diego, La Jolla, CA 92093, USA
    Met Based Drugs 2010:317581. 2010
    ..Insight into the mechanisms by which CTR1 and CTR2 regulate sensitivity to the Pt-containing drugs has served as the basis for novel pharmacologic strategies for improving their efficacy...
  2. pmc Cisplatin induces resistance by triggering differentiation of testicular embryonal carcinoma cells
    Paolo B Abada
    Department of Medicine and the Moores UCSD Cancer Center, University of California San Diego, La Jolla, California, United States of America
    PLoS ONE 9:e87444. 2014
    ..We conclude that cisplatin can acutely induce resistance to itself and paclitaxel by triggering a differentiation response in pluripotent germ cell tumor cells. ..
  3. pmc Copper transporter 2 regulates intracellular copper and sensitivity to cisplatin
    Carlos P Huang
    Moores UCSD Cancer Center, University of California, San Diego, 3855 Health Sciences Drive, La Jolla, CA 92093 0819, USA
    Metallomics 6:654-61. 2014
    ..This study introduces CS3 and related sensors as novel tools for probing and assaying Cu-dependent sensitivity to anticancer therapeutics. ..
  4. pmc The role of metal binding and phosphorylation domains in the regulation of cisplatin-induced trafficking of ATP7B
    Roohangiz Safaei
    Moores Cancer Center, University of California, San Diego, 3855 Health Sciences Drive, La Jolla, CA 92093 0819, USA
    Metallomics 5:964-72. 2013
    ....
  5. pmc Targeting granzyme B to tumor cells using a yoked human chorionic gonadotropin
    Isao Kanatani
    Department of Medicine and the Rebecca and John Moores UCSD Cancer Center, University of California, San Diego, La Jolla, CA 92093 0819, USA
    Cancer Chemother Pharmacol 68:979-90. 2011
    ..To selectively kill LHR-expressing tumors, granzyme B (GrB) was linked to a protein in which both chains of human chorionic gonadotropin were yoked together (YCG)...
  6. pmc Preclinical efficacy studies of a novel nanoparticle-based formulation of paclitaxel that out-performs Abraxane
    Zhongling Feng
    Biogroup, Nitto Denko Technical Corporation, 501 Via Del Monte, Oceanside, CA 92058, USA
    Cancer Chemother Pharmacol 65:923-30. 2010
    ..7-fold relative to that produced by PTX formulated in Cremophor. In this study, the efficacy of PGG-PTX was compared to that of Abraxane, an established nanoparticular formulation of PTX, in three different tumor models...
  7. pmc Pharmacokinetics and tissue distribution of PGG-paclitaxel, a novel macromolecular formulation of paclitaxel, in nu/nu mice bearing NCI-460 lung cancer xenografts
    Xinghe Wang
    Biogroup, Nitto Denko Technical Corporation, 501 Via Del Monte, Oceanside, CA 92058, USA
    Cancer Chemother Pharmacol 65:515-26. 2010
    ..The purpose of this study was to compare the pharmacokinetics and tissue distribution of PTX following injection of either free PTX or PGG-PTX in mice...
  8. pmc Challenges associated with the targeted delivery of gelonin to claudin-expressing cancer cells with the use of activatable cell penetrating peptides to enhance potency
    Xiaoqin Yuan
    Department of Medicine and Rebecca and John Moores UCSD Cancer Center, University of California San Diego, 3855 Health Sciences Drive, La Jolla, CA 92093 0819, USA
    BMC Cancer 11:61. 2011
    ..perfringens enterotoxin (CPE), which binds to claudins 3 and 4, to deliver a toxin in the form of recombinant gelonin (rGel) to the cytoplasm of the human ovarian carcinoma cell line 2008...
  9. pmc Copper transporters and the cellular pharmacology of the platinum-containing cancer drugs
    Stephen B Howell
    Department of Medicine, Moores UCSD Cancer Center, 3855 Health Sciences Drive, La Jolla, CA 92093, USA
    Mol Pharmacol 77:887-94. 2010
    ....
  10. ncbi request reprint Resistance to apoptosis in prostate cancer cells
    S B Howell
    Department of Medicine and the Cancer Center, University of California, San Diego, La Jolla, California 92093, USA
    Mol Urol 4:225-9;discussion 231. 2000
    ..One such example is a recently identified small organic compound that can inhibit p53 function and thus protect normal tissues against radiation-induced apoptosis without impairing killing of p53-deficient tumor cells...
  11. doi request reprint Pharmacologic principles of intraperitoneal chemotherapy for the treatment of ovarian cancer
    S B Howell
    Moores UCSD Cancer Center, University of California, San Diego, California 92093, USA
    Int J Gynecol Cancer 18:20-5. 2008
    ..New information about how cisplatin and carboplatin are transported into ovarian carcinoma cells points to novel strategies for further improving the therapeutic effectiveness of intraperitoneal chemotherapy...
  12. ncbi request reprint Increased expression of the copper efflux transporter ATP7A mediates resistance to cisplatin, carboplatin, and oxaliplatin in ovarian cancer cells
    Goli Samimi
    Department of Medicine, University of California San Diego, La Jolla, California, 92093 0058, USA
    Clin Cancer Res 10:4661-9. 2004
    ..The goal of this study was to determine the effect of small changes in ATP7A expression on the pharmacodynamics of cisplatin, carboplatin, and oxaliplatin in human ovarian carcinoma cells...
  13. ncbi request reprint Confocal microscopic analysis of the interaction between cisplatin and the copper transporter ATP7B in human ovarian carcinoma cells
    Kuniyuki Katano
    Department of Medicine, Chemistry and the Cancer Center, University of California, San Diego, La Jolla, California, USA
    Clin Cancer Res 10:4578-88. 2004
    ..These results provide evidence that DDP directly interacts with ATP7B to trigger its relocalization and that ATP7B mediates resistance to DDP by sequestering it into vesicles of the secretory pathway for export from the cell...
  14. ncbi request reprint Acquisition of resistance to cisplatin is accompanied by changes in the cellular pharmacology of copper
    Kuniyuki Katano
    Department of Medicine and the Cancer Center, University of California, San Diego, La Jolla, California 92093 0058, USA
    Cancer Res 62:6559-65. 2002
    ..These results are consistent with the concept that DDP enters and exits from the cell via transporters that normally mediate copper homeostasis...
  15. ncbi request reprint Modulation of the cellular pharmacology of cisplatin and its analogs by the copper exporters ATP7A and ATP7B
    Goli Samimi
    Department of Medicine, the Rebecca and John Moores University of California San Diego Cancer Center, Biomedical Sciences Graduate Program, University of California, San Diego, La Jolla, USA
    Mol Pharmacol 66:25-32. 2004
    ..However, in this model system, although copper is readily exported after vesicular sequestration, the platinum drugs are not...
  16. ncbi request reprint Modulation of the cellular pharmacology of JM118, the major metabolite of satraplatin, by copper influx and efflux transporters
    Goli Samimi
    Department of Medicine, The Rebecca and John Moores UCSD Cancer Center, Mail code 0819, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA
    Cancer Chemother Pharmacol 57:781-8. 2006
    ..These results suggest that JM118 will retain activity in cells in which DDP resistance is due to the loss of CTR1, but not in cells in which resistance is due to enhanced expression of ATP7A or ATP7B...
  17. pmc The role of the methionines and histidines in the transmembrane domain of mammalian copper transporter 1 in the cellular accumulation of cisplatin
    Christopher A Larson
    Rebecca and John Moores Cancer Center and Department of Medicine, University of California, San Diego, La Jolla, California, USA
    Mol Pharmacol 78:333-9. 2010
    ....
  18. pmc Copper transporter 2 regulates the cellular accumulation and cytotoxicity of Cisplatin and Carboplatin
    Brian G Blair
    Moores Cancer Center and Department of Medicine, University of California, San Diego, La Jolla, California
    Clin Cancer Res 15:4312-21. 2009
    ..We sought to determine the effect of CTR2 on influx, intracellular trafficking, and efflux of cisplatin and carboplatin...
  19. ncbi request reprint The copper influx transporter human copper transport protein 1 regulates the uptake of cisplatin in human ovarian carcinoma cells
    Alison K Holzer
    Department of Medicine, University of California, San Diego, 9500 Gilman Drive, La Jolla 92093 0058, USA
    Mol Pharmacol 66:817-23. 2004
    ....
  20. ncbi request reprint The copper export pump ATP7B modulates the cellular pharmacology of carboplatin in ovarian carcinoma cells
    Kuniyuki Katano
    Department of Medicine, University of California, San Diego, 9500 Gilman Dr, La Jolla, CA 92093 0058, USA
    Mol Pharmacol 64:466-73. 2003
    ..We conclude that expression of ATP7B regulates sensitivity to CBDCA as well as to DDP and copper and that a transporter that normally mediates copper homeostasis modulates the cellular pharmacology of CBDCA...
  21. ncbi request reprint Increase in expression of the copper transporter ATP7A during platinum drug-based treatment is associated with poor survival in ovarian cancer patients
    Goli Samimi
    Department of Medicine and the Cancer Center, University of California San Diego, La Jolla, California 92093 0058, USA
    Clin Cancer Res 9:5853-9. 2003
    ..We examined the expression of ATP7A in the major normal human organs and in several types of human malignancies and sought to determine whether ATP7A expression changed during treatment of ovarian carcinomas with Pt-containing regimens...
  22. ncbi request reprint Cisplatin rapidly down-regulates its own influx transporter hCTR1 in cultured human ovarian carcinoma cells
    Alison K Holzer
    Department of Medicine and the Rebecca and John Moores Cancer Center, University of California at San Diego, La Jolla, California 92093 0058, USA
    Clin Cancer Res 10:6744-9. 2004
    ..The goal of this study was to examine the effect of Cu and DDP on the level and subcellular localization of hCTR1 protein in human ovarian carcinoma cells...
  23. pmc Regulation of copper transporter 2 expression by copper and cisplatin in human ovarian carcinoma cells
    Brian G Blair
    Moores Cancer Center, Department of Medicine, University of California, La Jolla, CA 92093 0819, USA
    Mol Pharmacol 77:912-21. 2010
    ..Therefore, these two copper transporters have opposite effects on DDP sensitivity. CTR2 expression is regulated by copper availability via the copper-dependent regulator ATOX1...
  24. ncbi request reprint Contribution of the major copper influx transporter CTR1 to the cellular accumulation of cisplatin, carboplatin, and oxaliplatin
    Alison K Holzer
    Department of Medicine and the Rebecca and John Moores UCSD Cancer Center, 3855 Health Sciences Drive, Room 3344, La Jolla, CA 92093 0819, USA
    Mol Pharmacol 70:1390-4. 2006
    ..We conclude that L-OHP is a substrate for some other cellular entry mechanism, a feature consistent with its different clinical spectrum of activity...
  25. ncbi request reprint Cross-resistance to cisplatin in cells with acquired resistance to copper
    Roohangiz Safaei
    Department of Medicine 0058, University of California San Diego, 9500 Gilman Drive, La Jolla, CA 92093 0058, USA
    Cancer Chemother Pharmacol 53:239-46. 2004
    ..We sought to determine whether cells selected for resistance to Cu are cross-resistant to DDP...
  26. pmc The role of the mammalian copper transporter 1 in the cellular accumulation of platinum-based drugs
    Christopher A Larson
    Department of Medicine, Moores Cancer Center, University of California, San Diego, La Jolla, California 92093, USA
    Mol Pharmacol 75:324-30. 2009
    ..We conclude that CTR1 mediates the initial influx of DDP, CBDCA, and L-OHP and is a major determinant of responsiveness to DDP both in vitro and in vivo...
  27. pmc Enhanced delivery of cisplatin to intraperitoneal ovarian carcinomas mediated by the effects of bortezomib on the human copper transporter 1
    Danielle D Jandial
    Department of Medicine and the Rebecca and John Moores Cancer Center, University of California, San Diego, La Jolla, California, USA
    Clin Cancer Res 15:553-60. 2009
    ..We sought to determine whether proteasome inhibition using bortezomib would prevent human CTR1 (hCTR1) degradation and increase platinum accumulation in ovarian cancer cells...
  28. ncbi request reprint cDNA microarray-based identification of genes and pathways associated with oxaliplatin resistance
    Goli Samimi
    Department of Medicine and the Cancer Center, University of California, 9500 Gilman Drive, La Jolla, San Diego, 92093 0058, CA, USA
    Cancer Chemother Pharmacol 55:1-11. 2005
    ....
  29. ncbi request reprint Intracellular localization and trafficking of fluorescein-labeled cisplatin in human ovarian carcinoma cells
    Roohangiz Safaei
    Department of Medicine, and the Rebecca and John Moores Cancer Center, University of California San Diego, San Diego, CA 92093, USA
    Clin Cancer Res 11:756-67. 2005
    ..We sought to identify the subcellular compartments in which cisplatin [cis-diamminedichloroplatinum (DDP)] accumulates in human ovarian carcinoma cells and define its export pathways...
  30. ncbi request reprint Copper transporters regulate the cellular pharmacology and sensitivity to Pt drugs
    Roohangiz Safaei
    Department of Medicine and the Rebecca and John Moores Cancer Center, University of California, San Diego, La Jolla, CA 92093 0058, USA
    Crit Rev Oncol Hematol 53:13-23. 2005
    ..Appreciation of the role of the Cu transporters in the development of resistance to DDP, CBDCA, and L-OHP offers novel insights into strategies for preventing or reversing resistance to this very important family of anticancer drugs...
  31. ncbi request reprint The internalization and degradation of human copper transporter 1 following cisplatin exposure
    Alison K Holzer
    Department of Medicine and the Rebecca and John Moores Cancer Center, University of California at San Diego, La Jolla, California, USA
    Cancer Res 66:10944-52. 2006
    ..Because hCTR1 is a major determinant of early DDP uptake, prevention of its degradation offers a potential approach to enhancing tumor sensitivity...
  32. ncbi request reprint Abnormal lysosomal trafficking and enhanced exosomal export of cisplatin in drug-resistant human ovarian carcinoma cells
    Roohangiz Safaei
    Rebecca and John Moore University of California at San Diego Cancer Center, University of California at San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA
    Mol Cancer Ther 4:1595-604. 2005
    ....
  33. ncbi request reprint Novel mechanisms of platinum drug resistance identified in cells selected for resistance to JM118 the active metabolite of satraplatin
    Goli Samimi
    Department of Medicine and Rebecca and John Moores UCSD Cancer Center, 0819, University of California San Diego, 3855 Health Sciences Drive, La Jolla, CA 92093 0819, USA
    Cancer Chemother Pharmacol 59:301-12. 2007
    ..The goal of this study was to identify molecular determinants of sensitivity and resistance to JM118, the active metabolite of satraplatin, an orally bioavailable cisplatin analog that has activity in prostate cancer...
  34. ncbi request reprint The role of copper transporters in the development of resistance to Pt drugs
    Roohangiz Safaei
    Department of Medicine and the Rebecca and John Moores Cancer Center, University of California, 9500 Gilman Drive, San Diego, La Jolla, CA 92093 0058, USA
    J Inorg Biochem 98:1607-13. 2004
    ..Negative associations between the expression of ATP7A and ATP7B and the outcome of Pt therapy further support the significance of the Cu homeostasis proteins as both markers of and contributors to Pt resistance...
  35. pmc The role of the N-terminus of mammalian copper transporter 1 in the cellular accumulation of cisplatin
    Christopher A Larson
    Moores Cancer Center and Department of Medicine, University of California, San Diego, La Jolla, 92093, United States
    Biochem Pharmacol 80:448-54. 2010
    ..We conclude that cDDP interacts with hCTR1 both at (40)MXXM(45) and at sites outside the N-terminal domain that produce the conformational changes that trigger degradation...
  36. ncbi request reprint The copper transporter CTR1 regulates cisplatin uptake in Saccharomyces cerevisiae
    Xinjian Lin
    Department of Medicine and the Cancer Center, University of California, San Diego, La Jolla, California 92093, USA
    Mol Pharmacol 62:1154-9. 2002
    ..These results indicate that CTR1 function markedly influences the uptake of all of the clinically used platinum-containing drugs and suggest that this copper transporter may also transport DDP...
  37. ncbi request reprint Transport of cisplatin by the copper efflux transporter ATP7B
    Roohangiz Safaei
    Department of Medicine, University of California, San Diego, 3855 Health Sciences Drive, La Jolla, CA 92093 0819, USA
    Mol Pharmacol 73:461-8. 2008
    ..Copper and DDP each inhibited the ATP-dependent transport of the other. These results establish that DDP is a substrate for ATP7B but is transported at a much slower rate than copper...
  38. pmc Effects of the loss of Atox1 on the cellular pharmacology of cisplatin
    Roohangiz Safaei
    Moores UCSD Cancer Center, University of California, San Diego, 3855 Health Sciences Drive, La Jolla, CA 92093 0819, United States
    J Inorg Biochem 103:333-41. 2009
    ..Ctr1 was found to be polyubiquitinated in an Atox1-dependent manner during CDDP exposure. In conclusion, Atox1 is required for the polyubiquitination of Ctr1 and the Ctr1-mediated uptake of CDDP...
  39. ncbi request reprint DNA polymerase zeta regulates cisplatin cytotoxicity, mutagenicity, and the rate of development of cisplatin resistance
    Fang Wu
    Department of Medicine and the Cancer Center, University of California San Diego, La Jolla, California 92093, USA
    Cancer Res 64:8029-35. 2004
    ..We conclude that when cisplatin adducts are present in the DNA, polymerase zeta is an important contributor to cisplatin-induced genomic instability and the subsequent emergence of resistance to this chemotherapeutic agent...
  40. pmc Tumor platinum concentration following intraperitoneal administration of cisplatin versus carboplatin in an ovarian cancer model
    Danielle D Jandial
    Moores Cancer Center, University of California, San Diego, 3855 Health Sciences Drive, La Jolla, CA 92093 0819, USA
    Gynecol Oncol 115:362-6. 2009
    ..We compared the uptake of IP administered DDP and CBDCA into human ovarian carcinoma nodules of various sizes growing on the peritoneal surface of nu/nu mice...
  41. ncbi request reprint DNA polymerase zeta accounts for the reduced cytotoxicity and enhanced mutagenicity of cisplatin in human colon carcinoma cells that have lost DNA mismatch repair
    Xinjian Lin
    Department of Medicine and the Cancer Center, University of California San Diego, La Jolla, CA 92093, USA
    Clin Cancer Res 12:563-8. 2006
    ....
  42. ncbi request reprint Identification of genes whose expression is associated with cisplatin resistance in human ovarian carcinoma cells
    Timothy C Cheng
    Department of Medicine, The University of California Medical Center, La Jolla, San Diego, 92093 0819, USA
    Cancer Chemother Pharmacol 58:384-95. 2006
    ..The genes discovered by this extensively replicated analysis are candidates for prediction of DDP responsiveness in ovarian cancer patients...
  43. ncbi request reprint DNA mismatch repair and p53 function are major determinants of the rate of development of cisplatin resistance
    Xinjian Lin
    Department of Medicine 0058, University of California, San Diego, La Jolla, CA 92093, USA
    Mol Cancer Ther 5:1239-47. 2006
    ..The DNA damage response activated by cisplatin is accompanied by a p53- and MMR-dependent increase in homologous recombination even between adduct-free sequences...
  44. doi request reprint CD44-targeted microparticles for delivery of cisplatin to peritoneal metastases
    Shyh Dar Li
    Moores Cancer Center, University of California, San Diego, La Jolla, California 92093 0819, USA
    Mol Pharm 7:280-90. 2010
    ..Hyplat was more effective than cisplatin at slowing the growth of intraperitoneally inoculated A2780 ovarian cancer cells and improving survival thus demonstrating the potential of Hyplat to enhance the efficacy of ip chemotherapy...
  45. ncbi request reprint Identification of transdominant-negative genetic suppressor elements derived from hMSH2 that mediate resistance to 6-thioguanine
    Maida M de las Alas
    Cancer Center, University of California, San Diego, La Jolla, California, USA
    Mol Pharmacol 62:1198-206. 2002
    ..The results suggest that this region is important to the ability of the mismatch repair system to mediate drug sensitivity and to maintain genomic stability...
  46. doi request reprint Recombinant CPE fused to tumor necrosis factor targets human ovarian cancer cells expressing the claudin-3 and claudin-4 receptors
    Xiaoqin Yuan
    Department of Medicine and the Rebecca and John Moores University of California San Diego Cancer Center, University of California San Diego, La Jolla, CA 92093, USA
    Mol Cancer Ther 8:1906-15. 2009
    ..We conclude that CPE(290-319) effectively targeted TNF to ovarian cancer cells and is an attractive targeting moiety for development of CPE-based toxins for therapy of ovarian carcinomas that overexpress CLDN3 and CLDN4...
  47. pmc Acidic hydrolysis of N-Ethoxybenzylimidazoles (NEBIs): potential applications as pH-sensitive linkers for drug delivery
    Seong Deok Kong
    Department of Chemistry and Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, California 92093 0358, USA
    Bioconjug Chem 18:293-6. 2007
    ....
  48. ncbi request reprint Human REV1 modulates the cytotoxicity and mutagenicity of cisplatin in human ovarian carcinoma cells
    Xinjian Lin
    Department of Medicine and the Moores UCSD Cancer Center, University of California, San Diego, 3855 Health Sciences Drive, La Jolla, CA 92093 0819, USA
    Mol Pharmacol 69:1748-54. 2006
    ..We conclude that hREV1-dependent processes are important determinants of DDP-induced genomic instability and the development of resistance...
  49. pmc Copper transporter 2 regulates endocytosis and controls tumor growth and sensitivity to cisplatin in vivo
    Brian G Blair
    Moores Cancer Center and Department of Medicine, University of California, San Diego, La Jolla, California, USA
    Mol Pharmacol 79:157-66. 2011
    ..CTR2 regulates the transport of cDDP in part through control of the rate of macropinocytosis via activation of Rac1 and cdc42. Selective knockdown of CTR2 in tumors offers a strategy for enhancing the efficacy of cDDP...
  50. pmc NMR and mutagenesis of human copper transporter 1 (hCtr1) show that Cys-189 is required for correct folding and dimerization
    Sangwon Lee
    Department of Chemistry and Biochemistry, University of California, San Diego, La Jolla, CA, USA
    Biochim Biophys Acta 1768:3127-34. 2007
    ....
  51. ncbi request reprint Expression of the human copper influx transporter 1 in normal and malignant human tissues
    Alison K Holzer
    Department of Medicine and Pathology and the Rebecca and John Moores Cancer Center, University of California, San Diego, 3855 Health Sciences Drive, La Jolla, CA 92093 0819, USA, and Department of Surgery, Umea University Hospital, Sweden
    J Histochem Cytochem 54:1041-9. 2006
    ..No hCTR1 expression was found in several common types of cancer, suggesting that hCTR1 expression is not commonly enhanced by transformation...
  52. ncbi request reprint Diazonamide A and a synthetic structural analog: disruptive effects on mitosis and cellular microtubules and analysis of their interactions with tubulin
    Zobeida Cruz-Monserrate
    Building 469, Room 104, National Cancer Institute at Frederick, Frederick, MD 21702, USA
    Mol Pharmacol 63:1273-80. 2003
    ..If the latter is correct, diazonamide A and its oxygen analog should have uniquely potent inhibitory effects on the dynamic properties of microtubules...
  53. ncbi request reprint A Phase I and pharmacological study of the platinum polymer AP5280 given as an intravenous infusion once every 3 weeks in patients with solid tumors
    Jeany M Rademaker-Lakhai
    The Netherlands Cancer Institute, Amsterdam, The Netherlands
    Clin Cancer Res 10:3386-95. 2004
    ..In this way, it is anticipated that a higher activity of therapeutic Pt can be reached. The pharmaceutical product contains approximately 8.5% of Pt by weight and has a molecular weight of approximately 25,000...
  54. ncbi request reprint Suppression of hREV1 expression reduces the rate at which human ovarian carcinoma cells acquire resistance to cisplatin
    Tsuyoshi Okuda
    Department of Medicine 0058, University of California San Diego, La Jolla, CA
    Mol Pharmacol 67:1852-60. 2005
    ..Most importantly, hREV1 controls the rate of emergence of resistance to DDP at the population level. Thus, hREV1 is an important contributor to DDP-induced genomic instability and the subsequent emergence of resistance...
  55. pmc Dysregulation of purine nucleotide biosynthesis pathways modulates cisplatin cytotoxicity in Saccharomyces cerevisiae
    David Kowalski
    Department of Cancer Biology, Roswell Park Cancer Institute, Elm and Carlton Streets, Buffalo, NY 14263, USA
    Mol Pharmacol 74:1092-100. 2008
    ..Taken together, our results indicate that dysregulation of the purine nucleotide biosynthesis pathways and the addition of exogenous purines can modulate cisplatin cytotoxicity in Saccharomyces cerevisiae...
  56. ncbi request reprint Intraperitoneal therapy for stage III ovarian cancer: a therapy whose time has come!
    David S Alberts
    J Clin Oncol 20:3944-6. 2002
  57. ncbi request reprint Expression and mutational analysis of tyrosine kinase receptors c-kit, PDGFRalpha, and PDGFRbeta in ovarian cancers
    Sharon P Wilczynski
    Department of Pathology, City of Hope National Medical Center, Duarte, CA 91010, USA
    Hum Pathol 36:242-9. 2005
    ..This study demonstrates that PDGFR alpha, PDGFR beta, and c-kit are expressed in a high percentage of epithelial ovarian cancers suggesting that tyrosine kinase inhibitors may be useful in the treatment of these tumors...
  58. ncbi request reprint Phase I and pharmacokinetic trial of AP5346, a DACH-platinum-polymer conjugate, administered weekly for three out of every 4 weeks to advanced solid tumor patients
    Mario Campone
    Centre Rene Gauducheau, Nantes, France
    Cancer Chemother Pharmacol 60:523-33. 2007
    ..To determine the maximum tolerated dose (MTD) safety and pharmacokinetics of AP5346, a copolymer-linked 1,2-diaminocyclohexane(DACH)-platinum compound, in advanced solid tumor patients...
  59. ncbi request reprint Preclinical efficacy and pharmacokinetics of AP5346, a novel diaminocyclohexane-platinum tumor-targeting drug delivery system
    John R Rice
    Access Pharmaceuticals, Inc, Dallas, Texas, USA
    Clin Cancer Res 12:2248-54. 2006
    ..The goal of these studies was to determine the rate of release of Pt as a function of pH, the antitumor activity, and plasma and tumor pharmacokinetics of AP5346 in preclinical models...

Research Grants23

  1. Control of the cellular pharmacology of the platinum-containing drugs by CTR1
    Stephen B Howell; Fiscal Year: 2010
    ....
  2. Cisplatin resistance mediated by cooper export pathways
    Stephen Howell; Fiscal Year: 2007
    ..These studies will also further elucidate the mechanisms that mediate resistance to this important class of chemotherapeutic agents and suggest clinically relevant strategies for reversing resistance. ..
  3. Cisplatin resistance mediated by cooper export pathways
    Stephen Howell; Fiscal Year: 2005
    ..These studies will also further elucidate the mechanisms that mediate resistance to this important class of chemotherapeutic agents and suggest clinically relevant strategies for reversing resistance. ..
  4. Cisplatin resistance mediated by cooper export pathways
    Stephen Howell; Fiscal Year: 2009
    ..These studies will also further elucidate the mechanisms that mediate resistance to this important class of chemotherapeutic agents and suggest clinically relevant strategies for reversing resistance. ..
  5. CISPLATIN RESISTANCE DUE TO LOSS OF DNA MISMATCH REPAIR
    Stephen Howell; Fiscal Year: 2004
    ..Thus, it is very likely that the mechanisms underlying the DDP-induced mutagenicity will be of fundamental importance to understanding the genomic instability produced by many types of cellular injury. ..
  6. CISPLATIN RESISTANCE DUE TO LOSS OF DNA MISMATCH REPAIR
    Stephen Howell; Fiscal Year: 2002
    ..Thus, it is very likely that the mechanisms underlying the DDP-induced mutagenicity will be of fundamental importance to understanding the genomic instability produced by many types of cellular injury. ..
  7. Cisplatin resistance mediated by cooper export pathways
    Stephen Howell; Fiscal Year: 2006
    ..These studies will also further elucidate the mechanisms that mediate resistance to this important class of chemotherapeutic agents and suggest clinically relevant strategies for reversing resistance. ..
  8. Cisplatin Resistance mediated by copper export pathways
    Stephen Howell; Fiscal Year: 2002
    ..The results of these studies are expected to be of fundamental importance in identifying novel strategies for overcoming intrinsic resistance and reversing acquired resistance to this very important chemotherapeutic agent. ..
  9. Cisplatin resistance mediated by cooper export pathways
    Stephen Howell; Fiscal Year: 2009
    ..These studies will also further elucidate the mechanisms that mediate resistance to this important class of chemotherapeutic agents and suggest clinically relevant strategies for reversing resistance. ..
  10. CISPLATIN RESISTANCE DUE TO LOSS OF DNA MISMATCH REPAIR
    Stephen Howell; Fiscal Year: 1999
    ..of MMR increase the spontaneous rate of mutation to resistance to other clinically important chemotherapeutic agents?; and 4) does loss of MMR increase the ability of cisplatin to mutagenize tumor cells to other chemotherapeutic agents? ..
  11. Cisplatin Resistance mediated by copper export pathways
    Stephen Howell; Fiscal Year: 2003
    ..The results of these studies are expected to be of fundamental importance in identifying novel strategies for overcoming intrinsic resistance and reversing acquired resistance to this very important chemotherapeutic agent. ..
  12. UCSD Cancer Center Training Program in Drug Development
    Stephen Howell; Fiscal Year: 2007
    ..Special efforts will be made through our partnership grant and other vehicles to recruit and retain exceptional minority and women candidates to the program. ..
  13. CISPLATIN RESISTANCE DUE TO LOSS OF DNA MISMATCH REPAIR
    Stephen Howell; Fiscal Year: 2000
    ..of MMR increase the spontaneous rate of mutation to resistance to other clinically important chemotherapeutic agents?; and 4) does loss of MMR increase the ability of cisplatin to mutagenize tumor cells to other chemotherapeutic agents? ..
  14. Cisplatin Resistance mediated by copper export pathways
    Stephen B Howell; Fiscal Year: 2010
    ....
  15. CISPLATIN RESISTANCE DUE TO LOSS OF DNA MISMATCH REPAIR
    Stephen Howell; Fiscal Year: 2003
    ..Thus, it is very likely that the mechanisms underlying the DDP-induced mutagenicity will be of fundamental importance to understanding the genomic instability produced by many types of cellular injury. ..
  16. CISPLATIN RESISTANCE DUE TO LOSS OF DNA MISMATCH REPAIR
    Stephen Howell; Fiscal Year: 2005
    ..Thus, it is very likely that the mechanisms underlying the DDP-induced mutagenicity will be of fundamental importance to understanding the genomic instability produced by many types of cellular injury. ..
  17. The Center for Cancer Drug Development (C2D2)
    Stephen Howell; Fiscal Year: 2004
    ..abstract_text> ..
  18. Cisplatin Resistance mediated by copper export pathways
    Stephen Howell; Fiscal Year: 2004
    ..The results of these studies are expected to be of fundamental importance in identifying novel strategies for overcoming intrinsic resistance and reversing acquired resistance to this very important chemotherapeutic agent. ..
  19. CISPLATIN RESISTANCE DUE TO LOSS OF DNA MISMATCH REPAIR
    Stephen Howell; Fiscal Year: 2001
    ..of MMR increase the spontaneous rate of mutation to resistance to other clinically important chemotherapeutic agents?; and 4) does loss of MMR increase the ability of cisplatin to mutagenize tumor cells to other chemotherapeutic agents? ..