ellipticines

Summary

Summary: Pyrido-CARBAZOLES originally discovered in the bark of OCHROSIA ELLIPTICA. They inhibit DNA and RNA synthesis and have immunosuppressive properties.

Top Publications

  1. doi Ellipticine derivative NSC 338258 represents a potential new antineoplastic agent for the treatment of multiple myeloma
    Erming Tian
    The Donna D and Donald M Lambert Laboratory of Myeloma Genetics, Myeloma Institute for Research and Therapy, University of Arkansas for Medical Sciences, Little Rock, AR, USA
    Mol Cancer Ther 7:500-9. 2008
  2. ncbi Comparison of the pharmacological profile of an olivacine derivative and a potential prodrug
    Laurence Kraus-Berthier
    Institut de Recherches Servier, Division de Cancérologie, 11 rue des Moulineaux, 92150 Suresnes, France
    Cancer Chemother Pharmacol 50:95-103. 2002
  3. ncbi Detection of topoisomerase inhibitor-induced DNA strand breaks and apoptosis by the alkaline comet assay
    Thierry Godard
    GRECAN and INSERM CJF 96 03, Universite de Caen, and Laboratoire de Cancérologie Expérimentale, Centre Francois Baclesse, Route de Lion sur Mer, F 14076 Cedex 05, Caen, France
    Mutat Res 520:47-56. 2002
  4. ncbi Extending nature's leads: the anticancer agent ellipticine
    Nichola C Garbett
    Department of Chemistry, University of Alabama at Birmingham, Birmingham, Alabama 35294, USA
    Curr Med Chem Anticancer Agents 4:149-72. 2004
  5. ncbi Molecular mechanisms of antineoplastic action of an anticancer drug ellipticine
    Marie Stiborova
    Department of Biochemistry, Faculty of Science, Charles University, Albertov 2030, Prague 2, Czech Republic
    Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub 150:13-23. 2006
  6. pmc Sequence effect of self-assembling peptides on the complexation and in vitro delivery of the hydrophobic anticancer drug ellipticine
    Shan Yu Fung
    Department of Chemical Engineering, University of Waterloo, Waterloo, Ontario, Canada
    PLoS ONE 3:e1956. 2008
  7. doi Anthracyclines and ellipticines as DNA-damaging anticancer drugs: recent advances
    Rene Kizek
    Department of Chemistry and Biochemistry, Faculty of Agronomy, Mendel University in Brno, Zemedelska 1, CZ 613 00 Brno, Czech Republic
    Pharmacol Ther 133:26-39. 2012
  8. doi Ellipticines and 9-acridinylamines as inhibitors of D-alanine:D-alanine ligase
    Blaz Vehar
    National Institute of Chemistry, Ljubljana, Slovenia
    Bioorg Med Chem 19:5137-46. 2011
  9. doi Ellipticine-induced apoptosis depends on Akt translocation and signaling in lung epithelial cancer cells
    Kang Fang
    Department of Life Science, National Taiwan Normal University, Taipei, Taiwan
    Lung Cancer 63:227-34. 2009
  10. ncbi Ellipticine induces apoptosis through p53-dependent pathway in human hepatocellular carcinoma HepG2 cells
    Yu Chun Kuo
    Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung, Taiwan
    Life Sci 78:2550-7. 2006

Scientific Experts

Detail Information

Publications128 found, 100 shown here

  1. doi Ellipticine derivative NSC 338258 represents a potential new antineoplastic agent for the treatment of multiple myeloma
    Erming Tian
    The Donna D and Donald M Lambert Laboratory of Myeloma Genetics, Myeloma Institute for Research and Therapy, University of Arkansas for Medical Sciences, Little Rock, AR, USA
    Mol Cancer Ther 7:500-9. 2008
    ..Collectively, our data suggest that EPED3 targets mitochondrial function to rapidly deplete chemical energy and initiate apoptosis in myeloma cells at nanomolar concentrations while leaving stromal cells unharmed...
  2. ncbi Comparison of the pharmacological profile of an olivacine derivative and a potential prodrug
    Laurence Kraus-Berthier
    Institut de Recherches Servier, Division de Cancérologie, 11 rue des Moulineaux, 92150 Suresnes, France
    Cancer Chemother Pharmacol 50:95-103. 2002
    ..Amongst the analogues which were synthesized to improve both therapeutic index and antitumor activity, the most active ones were those esterified on the 9-OH group such as S 30972-1, the glutaric acid monoester derivative...
  3. ncbi Detection of topoisomerase inhibitor-induced DNA strand breaks and apoptosis by the alkaline comet assay
    Thierry Godard
    GRECAN and INSERM CJF 96 03, Universite de Caen, and Laboratoire de Cancérologie Expérimentale, Centre Francois Baclesse, Route de Lion sur Mer, F 14076 Cedex 05, Caen, France
    Mutat Res 520:47-56. 2002
    ..Kinetics studies allowed to discriminate between these early DNA damages and DNA fragmentation related to apoptosis characterised by reappearance of DNA strand breaks 48h after treatment...
  4. ncbi Extending nature's leads: the anticancer agent ellipticine
    Nichola C Garbett
    Department of Chemistry, University of Alabama at Birmingham, Birmingham, Alabama 35294, USA
    Curr Med Chem Anticancer Agents 4:149-72. 2004
    ..Considerable research efforts have been directed towards gaining a greater understanding of the mechanism of action of these drugs that will aid further in the optimization of drug design...
  5. ncbi Molecular mechanisms of antineoplastic action of an anticancer drug ellipticine
    Marie Stiborova
    Department of Biochemistry, Faculty of Science, Charles University, Albertov 2030, Prague 2, Czech Republic
    Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub 150:13-23. 2006
    ..The study forms the basis to further predict the susceptibility of human cancers to ellipticine...
  6. pmc Sequence effect of self-assembling peptides on the complexation and in vitro delivery of the hydrophobic anticancer drug ellipticine
    Shan Yu Fung
    Department of Chemical Engineering, University of Waterloo, Waterloo, Ontario, Canada
    PLoS ONE 3:e1956. 2008
    ..This work provides essential information for peptide sequence design in the development of self-assembling peptide-based delivery of hydrophobic anticancer drugs...
  7. doi Anthracyclines and ellipticines as DNA-damaging anticancer drugs: recent advances
    Rene Kizek
    Department of Chemistry and Biochemistry, Faculty of Agronomy, Mendel University in Brno, Zemedelska 1, CZ 613 00 Brno, Czech Republic
    Pharmacol Ther 133:26-39. 2012
    Over the past forty years, anthracyclines and ellipticines have attracted attention as promising cytostatics. In this review, we focus on their mechanisms of cytoxicity, DNA-damaging effects and adverse side-effects...
  8. doi Ellipticines and 9-acridinylamines as inhibitors of D-alanine:D-alanine ligase
    Blaz Vehar
    National Institute of Chemistry, Ljubljana, Slovenia
    Bioorg Med Chem 19:5137-46. 2011
    ..New members of both families were obtained through similarity search and synthesis. Ellipticines and 9-acridinylamines were both found to possess inhibitory activity against Ddl from Escherichia coli and ..
  9. doi Ellipticine-induced apoptosis depends on Akt translocation and signaling in lung epithelial cancer cells
    Kang Fang
    Department of Life Science, National Taiwan Normal University, Taipei, Taiwan
    Lung Cancer 63:227-34. 2009
    ..Being a topoisomerase II inhibitor, ellipticine proved a regulator in autophagy-related cell death through corporation of p53 and Akt...
  10. ncbi Ellipticine induces apoptosis through p53-dependent pathway in human hepatocellular carcinoma HepG2 cells
    Yu Chun Kuo
    Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung, Taiwan
    Life Sci 78:2550-7. 2006
    ..Taken together, ellipticine decreased the cell growth and induced apoptosis in HepG2 cell...
  11. ncbi Oxidation pattern of the anticancer drug ellipticine by hepatic microsomes - similarity between human and rat systems
    M Stiborova
    Department of Biochemistry, Faculty of Science, Charles University, Albertov 2030, 128 40 Prague 2, Czech Republic
    Gen Physiol Biophys 25:245-61. 2006
    ..The results underline the suitability of rat species as a model to evaluate human susceptibility to ellipticine...
  12. ncbi The mechanism of ellipticine-induced apoptosis and cell cycle arrest in human breast MCF-7 cancer cells
    Po Lin Kuo
    Department of Biotechnology, Chia Nan University of Pharmacy and Science, Tainan, Taiwan, ROC
    Cancer Lett 223:293-301. 2005
    ....
  13. ncbi Correlating gene expression with chemical scaffolds of cytotoxic agents: ellipticines as substrates and inhibitors of MDR1
    Y Huang
    Department of Pharmacology, Comprehensive Cancer Center, College of Medicine and Public Health, The Ohio State University, Columbus, OH 4321 1239, USA
    Pharmacogenomics J 5:112-25. 2005
    ..To determine MDR1 interactions of five ellipticines with diverse MDR1-r values, we employed MDR1-transport and cytotoxicity assays, using MDR1 inhibitors and siRNA-..
  14. ncbi Rescue of mutant p53 transcription function by ellipticine
    Yanhua Peng
    Molecular Oncology Program, H Lee Moffitt Comprehensive Cancer Center and Research Institute, 12902 Magnolia Drive, Tampa, FL 33612, USA
    Oncogene 22:4478-87. 2003
    ..These results demonstrate that ellipticine can restore transcription function to mutant p53. This property may contribute to the selectivity of ellipticine-derived compounds against tumor cell lines expressing mutant p53...
  15. ncbi Polymer-drug compatibility: a guide to the development of delivery systems for the anticancer agent, ellipticine
    Jubo Liu
    Department of Pharmaceutical Sciences, University of Toronto, 19 Russell St, Rom 315G, Toronto, Ontario M5S 2S2 Canada
    J Pharm Sci 93:132-43. 2004
    ..Overall, a good correlation was obtained between drug formulation characteristics and findings from our polymer-drug compatibility studies. Further optimization of the PEO-b-PCL micelle formulation for Ellipticine was also performed...
  16. ncbi The anticancer agent ellipticine unwinds DNA by intercalative binding in an orientation parallel to base pairs
    Albert Canals
    Institut de Biologia Molecular de Barcelona, Consejo Superior de Investigaciones Cientificas, Parc Cientific de Barcelona, Baldiri Reixac 10 12, 08028 Barcelona, Spain
    Acta Crystallogr D Biol Crystallogr 61:1009-12. 2005
    ..The 1.5 A resolution structure of ellipticine complexed to a 6 bp oligonucleotide unveils its mode of binding and enables a detailed analysis of the distorting effects of the drug on the DNA...
  17. ncbi The anticancer agent ellipticine on activation by cytochrome P450 forms covalent DNA adducts
    M Stiborova
    Department of Biochemistry, Faculty of Science, Charles University, Albertov 2030, 128 40 2, The, Prague, Czech Republic
    Biochem Pharmacol 62:1675-84. 2001
    ..The DNA adduct formation we describe is a novel mechanism for the ellipticine action and might in part explain its tumor specificity...
  18. ncbi 9-hydroxyellipticine and derivatives as chemotherapy agents
    Margaret M Harding
    School of Chemistry, The University of Sydney, N S W 2006, Australia
    Mini Rev Med Chem 3:67-76. 2003
    ..quinone-imine intermediates, phosphorylation of p53 suppressor proteins and cytotoxicity relative to the parent ellipticines. Recent studies have focused on the mechanism of inhibition of phosphorylation of the mutant type of p53 ..
  19. ncbi Solvent effect on the photophysical properties of the anticancer agent ellipticine
    S Y Fung
    Department of Chemical Engineering, University of Waterloo, 200 University Avenue West, Waterloo, Ontario N2L 3G1, Canada
    J Phys Chem A 110:11446-54. 2006
    ..A relatively large red shift of emission in liposomes indicated that ellipticine may be in a more polar environment with respect to the lipid bilayer, possibly close to the hydrophilic interface...
  20. ncbi DNA adduct formation by the anticancer drug ellipticine in rats determined by 32P postlabeling
    Marie Stiborova
    Department of Biochemistry, Faculty of Science, Charles University, Albertov 2030 40 Prague 2, Czech Republic
    Int J Cancer 107:885-90. 2003
    ..The results presented here are the first report showing the formation of CYP-mediated covalent DNA adducts by ellipticine in vivo and confirm the formation of covalent DNA adducts as a new mode of ellipticine action...
  21. ncbi Target cells for cytochrome p450-catalysed irreversible binding of 7,12-dimethylbenz[a]anthracene (DMBA) in rodent adrenal glands
    Orjan Lindhe
    Department of Environmental Toxicology, Evolutionary Biology Center, Uppsala University, Norbyvagen 18A, S 752 36 Uppsala, Sweden
    Arch Toxicol 76:460-6. 2002
    ..We suggest that the adrenocorticolytic effect of DMBA is the result of a dual mode of action, targeting both endothelial and parenchymal cells in the rat adrenal cortex...
  22. ncbi 8-Methyl-4-(3-diethylaminopropylamino) pyrimido [4',5';4,5] thieno (2,3-b) quinoline (MDPTQ), a quinoline derivate that causes ROS-mediated apoptosis in leukemia cell lines
    Sudheer Shenoy
    Reliance Life Sciences Pvt Ltd, Dhirubhai Ambani Life Sciences Centre, Thane Belapur Road, Navi Mumbai, 400701, India
    Toxicol Appl Pharmacol 222:80-8. 2007
    ..However, there are lot of questions that need to be answered in terms of signalling pathways and its effects on animal models...
  23. ncbi Pattern recognition methods investigation of ellipticines structure-activity relationships
    Louraine C de Melo
    Centro Brasileiro de Pesquisas Fisicas, Rua Dr Xavier Sigaud, 150, 22290 180 Rio de Janeiro, RJ, Brazil
    J Mol Graph Model 25:912-20. 2007
    ..These descriptors have been only recently discussed in the literature as new possible universal parameters for defining the biological activity of several classes of compounds...
  24. ncbi Induction of endoplasmic reticulum stress by ellipticine plant alkaloids
    Maria Hägg
    Department of Oncology and Pathology, Cancer Center Karolinska, Karolinska Institute and Hospital, Stockholm, Sweden
    Mol Cancer Ther 3:489-97. 2004
    ..In this study, we examined apoptosis induction by ellipticines, a class of cytotoxic plant alkaloids known to inhibit topoisomerase II...
  25. ncbi Oxidation of an antitumor drug ellipticine by peroxidases
    Jitka Poljakova
    Department of Biochemistry, Charles University, Albertov 2030, Prague 2, Czech Republic
    Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub 149:449-53. 2005
    ..The implication of the oxidation of ellipticine by peroxidases in its mechanism of action is discussed...
  26. ncbi Effect of a single nucleotide polymorphism in the murine double minute 2 promoter (SNP309) on the sensitivity to topoisomerase II-targeting drugs
    Mamatha S Nayak
    Department of Pharmacology, The Cancer Institute of New Jersey, University of Medicine and Dentistry of New Jersey Robert Wood Johnson Medical School, New Brunswick, New Jersey 08901, USA
    Cancer Res 67:5831-9. 2007
    ..Given the frequency of SNP309 in the general population (40% in heterozygous T/G and 12% in homozygous G/G condition), our observation may have important implications for the individualization of cancer chemotherapy...
  27. ncbi Synthesis and biological evaluation of indoloquinolines and pyridocarbazoles: a new example of unexpected photoreduction accompanying photocyclization
    Pierre Jean Aragon
    Laboratoire de Chimie Organique Pharmaceutique, EA 2414, Faculte de Pharmacie, Montpellier, France
    Chem Pharm Bull (Tokyo) 55:1349-55. 2007
    ..All compounds were less effective than doxorubicin in sensitive cells but their activity wasn't decreased by MDR resistance...
  28. ncbi Restoration of p53 to limit tumor growth
    Wenge Wang
    Department of Medicine, University of Pennsylvania School of Medicine, Philadelphia 19104, USA
    Curr Opin Oncol 20:90-6. 2008
    ..Therefore, p53 serves as a unique molecular target for cancer therapy. This review focuses on the current progress regarding restoration of p53 function in human tumors for molecularly targeted therapy...
  29. ncbi The anticancer drug ellipticine is a potent inducer of rat cytochromes P450 1A1 and 1A2, thereby modulating its own metabolism
    Dagmar Aimová
    Department of Biochemistry, Faculty of Science, Charles University, Albertov 2030, 128 40 Prague 2, Czech Republic
    Drug Metab Dispos 35:1926-34. 2007
    ....
  30. ncbi Cytotoxic and antitumoral properties in a series of new, ring D modified, olivacine analogues
    Claude Guillonneau
    Servier, Division Chimie A, 11 rue des Moulineaux, 92150 Suresnes, France
    Bioorg Med Chem 13:175-84. 2005
    ....
  31. ncbi The anticancer drug ellipticine forms covalent DNA adducts, mediated by human cytochromes P450, through metabolism to 13-hydroxyellipticine and ellipticine N2-oxide
    Marie Stiborova
    Department of Biochemistry, Faculty of Science, Charles University, Prague, Czech Republic
    Cancer Res 64:8374-80. 2004
    ..Homologue modeling and docking of ellipticine to the CYP3A4 active center was used to explain the predominance of ellipticine oxidation by CYP3A4 to 13-hydroxyellipticine and N(2)-oxide...
  32. ncbi Chemosensitization of endometrial cancer cells through AKT inhibition involves FOXO1
    Anna V Hoekstra
    Department of Obstetrics and Gynecology, Division of Gynecologic Oncology, Northwestern University, Chicago, IL 60611, USA
    Gynecol Oncol 108:609-18. 2008
    ..Endometrial cancer is the most common type of gynecologic cancer in the United States. In this study, we propose that inhibition of the AKT pathway sensitizes cells to chemotherapeutic agents by increasing FOXO1 expression...
  33. ncbi Covalent binding of the anticancer drug ellipticine to DNA in V79 cells transfected with human cytochrome P450 enzymes
    Eva Frei
    Division of Molecular Toxicology, German Cancer Research Center, Im Neuenheimer Feld 280, 69120 Heidelberg, Germany
    Biochem Pharmacol 64:289-95. 2002
    ..The results presented here are the first report showing the formation of CYP-mediated covalent DNA adducts by ellipticine in cells in culture, and confirm the formation of covalent DNA adducts as a new mechanism of ellipticine action...
  34. ncbi The olivacine S16020 enhances the antitumor effect of ionizing radiation without increasing radio-induced mucositis
    L Maggiorella
    , , Institut Gustave Roussy, 94805 Villejuif Cedex, France
    Clin Cancer Res 7:2091-5. 2001
    ..In conclusion, the combination of IR and S16020 seems promising to enhance antitumor activity without increasing deleterious effect in normal tissues and to provide the basis for a new radio-chemotherapy combination...
  35. ncbi Bacteriophage T4, a model system for understanding the mechanism of type II topoisomerase inhibitors
    K N Kreuzer
    Department of Microbiology, Duke University Medical Center, Durham, NC 27710, USA
    Biochim Biophys Acta 1400:339-47. 1998
    ..sensitive to many of the same antitumor agents that inhibit mammalian type II topoisomerase, including m-AMSA, ellipticines, mitoxantrone and epipodophyllotoxins...
  36. ncbi Interfacial inhibitors of protein-nucleic acid interactions
    Yves Pommier
    Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Heath, Bethesda, Maryland 20892 4255, USA
    Curr Med Chem Anticancer Agents 5:421-9. 2005
    ..examples generalizing the interfacial inhibitor concept to inhibitors of topoisomerase II (anthracyclines, ellipticines, epipodophyllotoxins), gyrase (quinolones, ciprofloxacin, norfloxacin), RNA polymerases (alpha-amanitin and ..
  37. doi Tolbutamide hydroxylation by hepatic microsomes from Atlantic salmon (Salmo salar L.)
    Annalotta Schiller Vestergren
    Department of Food Science, Biocenter, Swedish University of Agricultural Sciences, Uppsala, Sweden
    Mol Biol Rep 39:6867-73. 2012
    ..Incubation of diclofenac with the microsomes yielded no metabolite formation, suggesting that salmon does not possess diclofenac-metabolizing activity...
  38. doi The date palm (Phoenix dactylifera L.) micropropagation using completely mature female flowers
    Walid Kriaâ
    Laboratory of Plant Biotechnology, Department of Biology, Route Soukra, Sfax, Tunisia
    C R Biol 335:194-204. 2012
    ....
  39. doi Study of DNA-ellipticine interaction by capillary electrophoresis with laser-induced fluorescence detection
    Marketa Ryvolova
    Department of Chemistry and Biochemistry, Faculty of Agronomy, Mendel University in Brno, Brno, Czech Republic
    Electrophoresis 33:1545-9. 2012
    ..Signal corresponding to ellipticine was decreasing and a new peak appeared and was growing. It can be concluded that CE-LIF is a method applicable to in vitro studies of ellipticine-DNA complexes...
  40. pmc Self-assembling peptide-based nanoparticles enhance anticancer effect of ellipticine in vitro and in vivo
    Yan Wu
    Department of Pharmacy, No 3 People s Hospital Affiliated to Shanghai Jiao Tong University School of Medicine, Shanghai, People s Republic of China
    Int J Nanomedicine 7:3221-33. 2012
    ..Here, the anticancer activity of ellipticine encapsulated in EAK16-II (EAK-EPT) was evaluated in vitro and in vivo...
  41. doi Synthesis and evaluation of novel ellipticines as potential anti-cancer agents
    Fiona M Deane
    Department of Chemistry and Analytical and Biological Chemistry Research Facility, University College Cork, Cork, Ireland
    Org Biomol Chem 11:1334-44. 2013
    ..04-5.2 μM). 6-Methylellipticine was the most potent growth inhibitory compound assessed (GI(50) = 0.47-0.9 μM). N-Alkylation of 6-methylellipticine was found to reduce this response with GI(50) values in the range of 1.3-28 μM...
  42. ncbi Synthesis and biological evaluation of novel isoellipticine derivatives and salts
    Charlotte M Miller
    Department of Chemistry, Analytical and Biological Chemistry Research Facility, University College Cork, Western Road, Cork, Ireland
    Org Biomol Chem 10:7912-21. 2012
    ..Two compounds display significant specificity towards CNS cancer cell lines and are lead compounds for future development...
  43. pmc Old drug, new target: ellipticines selectively inhibit RNA polymerase I transcription
    William J Andrews
    School of Biological Sciences, The Queen s University Belfast, Belfast BT9 7BL, United Kingdom
    J Biol Chem 288:4567-82. 2013
    ..Here we report that a number of the ellipticines, including 9-hydroxyellipticine, are potent and specific inhibitors of Pol-I transcription, with IC(50) in ..
  44. doi Mechanisms of ellipticine-mediated resistance in UKF-NB-4 neuroblastoma cells
    Pavel Prochazka
    Department of Pediatric Hematology and Oncology, 2nd Medical School, Charles University and University Hospital Motol, Prague, Czech Republic
    Cancer Sci 103:334-41. 2012
    ..Some changes are expressed at the DNA level, including gains, amplifications or deletions. The present study demonstrates that resistance to ellipticine is caused by a combination of mechanisms...
  45. ncbi Synthesis of poly-(3-hydroxybutyrate-co-12 mol % 3-hydroxyvalerate) by Bacillus cereus FB11: its characterization and application as a drug carrier
    Farha Masood
    Department of Microbiology, Quaid i Azam University QAU, Islamabad, Pakistan
    J Mater Sci Mater Med 24:1927-37. 2013
    ..This drug delivery system offers exciting possibilities for cancer therapy by increasing the bioavailability of anti-neoplastic drug to the tumor site...
  46. ncbi Role of hepatic cytochromes P450 in bioactivation of the anticancer drug ellipticine: studies with the hepatic NADPH:cytochrome P450 reductase null mouse
    Marie Stiborova
    Department of Biochemistry, Faculty of Science, Charles University, Albertov 2030, 128 40 Prague 2, Czech Republic
    Toxicol Appl Pharmacol 226:318-27. 2008
    ....
  47. pmc Demonstration that drug-targeted down-regulation of MYC in non-Hodgkins lymphoma is directly mediated through the promoter G-quadruplex
    Robert V Brown
    College of Pharmacy, University of Arizona, Tucson, Arizona 85721, USA
    J Biol Chem 286:41018-27. 2011
    ..Most importantly, these data present, as far as we are aware, the most direct evidence of intracellular G4-mediated control of a particular promoter...
  48. ncbi Dual fluorescence of ellipticine: excited state proton transfer from solvent versus solvent mediated intramolecular proton transfer
    Sanghamitra Banerjee
    School of Chemistry, University of Hyderabad, Hyderabad 500 046, India
    J Phys Chem A 115:9217-25. 2011
    ....
  49. pmc Synthesis and biological activity of 5-aza-ellipticine derivatives
    Deborah L Moody
    Structural Biophysics Laboratory, Molecular Aspects of Drug Design Section, Structural Biophysics Laboratory, NCI Frederick, PO Box B Frederick, MD 21702, USA
    Bioorg Med Chem Lett 17:2380-4. 2007
    ....
  50. doi A novel structural derivative of natural alkaloid ellipticine, MDPSQ, induces necrosis in leukemic cells
    M S Shahabuddin
    Department of Biochemistry, Indian Institute of Science, Bangalore, 560 012, India
    Invest New Drugs 29:523-33. 2011
    ..Besides, Annexin V/PI staining revealed that MDPSQ induces cell death by triggering necrosis rather than apoptosis...
  51. ncbi Cytochromes P450 reconstituted with NADPH: P450 reductase mimic the activating and detoxicating metabolism of the anticancer drug ellipticine in microsomes
    Vera Kotrbova
    Department of Biochemistry, Faculty of Science, Charles University, Prague, Czech Republic
    Neuro Endocrinol Lett 27:18-22. 2006
    ..Recently, we found that after cytochrome P450 (CYP)-mediated oxidation ellipticine forms covalent DNA adducts. Ellipticine oxidation by isolated CYP and its binding to DNA is the target of this study...
  52. ncbi Blockade of AKT activation in prostate cancer cells with a small molecule inhibitor, 9-chloro-2-methylellipticinium acetate (CMEP)
    Manchao Zhang
    Department of Biochemistry and Molecular Pharmacology, West Virginia University, 1 Medical Center Drive, Morgantown, WV 26506 9142, United States
    Biochem Pharmacol 73:15-24. 2007
    ..In conclusion, by specific blockade of the activation of AKT, CMEP preferentially inhibits growth and induces apoptosis in prostate cancer cells which have high-levels of AKT activation...
  53. doi Synthesis and cytotoxic activity of 5,6-heteroaromatically annulated pyridine-2,4-diamines
    C Willemann
    Department Chemie und Pharmazie, Universitat Erlangen Nurnberg, Lehrstuhl für Pharmazeutische Chemie, Erlangen, Germany
    Bioorg Med Chem 17:4406-19. 2009
    ..Surprisingly, pyrido[2,3-b]indolediamines 13 and 14 without benzo[g] annulation were inactive. None of the new compounds were as potent as ellipticine, the reference compound...
  54. doi Release of hydrophobic anticancer drug from a newly designed self-assembling peptide
    Min Wu
    West China Hospital Nanomedicine Laboratory and Institute for Nanobiomedical Technology and Membrane Biology, West China Hospital, Sichuan University, Chengdu, 610041, P R China
    Mol Biosyst 7:2040-7. 2011
    ..The results described herein provide further incentives for basic studies on self-assembling peptide-based delivery of hydrophobic anticancer drugs...
  55. ncbi Synthesis of new 1-phenyl-6H-pyrido[4,3-b]carbazole derivatives with potential cytostatic activity
    Beata Tylińska
    Wrocław Medical University, Faculty of Pharmacy, Department of Organic Chemistry, Grodzka 9 St, 50 137 Wrocław, Poland
    Acta Pol Pharm 68:31-7. 2011
    ..One particular compound 6f exhibited over 20 times better activity against L1210 tumor cell line than the reference ellipticine...
  56. ncbi Tyrosine kinase inhibition: Ligand binding and conformational change in c-Kit and c-Abl
    Eamonn F Healy
    Department of Chemistry, St Edward s University, Austin, TX 78704, USA
    FEBS Lett 583:2899-906. 2009
    ..Both experimental and molecular modeling studies of the active state inhibitor of the tyrosine kinase c-Abl indicate that solvent exclusion also plays a role in this system...
  57. pmc Identification of new 2-amino-3-methylimidazo[4,5-f]quinoline urinary metabolites from beta-naphthoflavone-treated mice
    Vijaya M Lakshmi
    Veterans Affairs Medical Center, St Louis, MO 63125, USA
    Drug Metab Dispos 37:1690-7. 2009
    ..Results from BNF-treated mice showed significant IQ metabolism by hepatic P450s. Therefore, differences in metabolism between mice treated with and without BNF may affect IQ tumorigenicity...
  58. ncbi The combination of 5-fluorouracil plus p53 pathway restoration is associated with depletion of p53-deficient or mutant p53-expressing putative colon cancer stem cells
    Catherine Huang
    Laboratory of Molecular Oncology and Cell Cycle Regulation, Departments of Medicine Hematology Oncology, Genetics and Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, PA, USA
    Cancer Biol Ther 8:2186-93. 2009
    ..Our results support the feasibility of therapeutic targeting of mutant p53 in putative cancer stem cells as well as the potential to enhance cytotoxic chemotherapy...
  59. doi Labdane-type diterpenes from Hedychium gardnerianum with potent cytotoxicity against human small cell lung cancer cells
    Iyared Kumrit
    Department of Chemistry and Center of Excellence for Innovation in Chemistry, Faculty of Science, Chiang Mai University, Chiang Mai, 50200, Thailand
    Phytother Res 24:1009-13. 2010
    ..The very high cytotoxicity against the NCI-H187 cells and the exceptionally high selectivity index (>416) of villosin suggested that this compound may be used as a potential lead molecule for antitumor therapeutic development...
  60. doi DNA binding ellipticine analogues: synthesis, biological evaluation, and structure-activity relationships
    Maria Grazia Ferlin
    Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Padova, Via Marzolo 5, 35131 Padova, Italy
    ChemMedChem 4:363-77. 2009
    ..Herein we discuss interesting structure-activity relationships with respect to molecular size and planarity, as well as the substitution and position of one side chain on the PyC nucleus, in comparison with corresponding smaller PQs...
  61. pmc Non-genotoxic anti-neoplastic effects of ellipticine derivative NSC176327 in p53-deficient human colon carcinoma cells involve stimulation of p73
    Chao Lu
    Laboratory of Molecular Oncology and Cell Cycle Regulation, The Institute for Translational Medicine and Therapeutics, The Abramson Comprehensive Cancer Center, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania, USA
    Cancer Biol Ther 7:2039-46. 2008
    ....
  62. pmc Molecular recognition of poly(A) by small ligands: an alternative method of analysis reveals nanomolar, cooperative and shape-selective binding
    Ozgül Persil Cetinkol
    School of Chemistry and Biochemistry, Parker H Petit Institute of Bioengineering and Bioscience, Georgia Institute of Technology, Atlanta, GA 30332 0400, USA
    Nucleic Acids Res 37:611-21. 2009
    ..The ligands described here may also find biological or medicinal applications, owing to the 3'-polyadenylation of mRNA in living cells...
  63. ncbi Cytotoxicity of and DNA adduct formation by ellipticine in human U87MG glioblastoma cancer cells
    Eva Martinkova
    Department of Biochemistry, Faculty of Science, Charles University, Prague, Czech Republic
    Neuro Endocrinol Lett 30:60-6. 2009
    ..The toxicity of ellipticine to U87MG glioblastoma cells and mechanisms of its action to these cells are aims of this study...
  64. ncbi Synthesis and anticancer activity of new 1-substituted-6H-pyrido[4,3-b]carbazole derivatives
    Beata Tylińska
    Wroclaw Medical University, Faculty of Pharmacy, Department of Organic Chemistry, Wroclaw, Poland
    Arch Pharm (Weinheim) 341:351-6. 2008
    ..One particular compound 3c was about four times more active on A498 than ellipticine with similar activity on the A549 cell line, and outperformed cisplatin activity on both tumor cell lines...
  65. doi Cytochrome P450- and peroxidase-mediated oxidation of anticancer alkaloid ellipticine dictates its anti-tumor efficiency
    M Stiborova
    Department of Biochemistry, Faculty of Science, Charles University, Albertov 2030, 12840 Prague 2, Czech Republic
    Biochim Biophys Acta 1814:175-85. 2011
    ..It also suggests ellipticine reactive metabolites 13-hydroxyellipticine and 12-hydroxyellipticine to be good candidates for targeting to tumors absent from the CYP and peroxidase activation enzymes...
  66. doi Glycosylation protects proteins against free radicals generated from toxic xenobiotics
    Vaclav Martinek
    Department of Biochemistry, Faculty of Science, Charles University Prague, 12840 Prague 2, Czech Republic
    Toxicol Sci 117:359-74. 2010
    ..The results indicate that carbohydrates protect polypeptides against modification by free radicals derived from toxic xenobiotics and provide passive shielding of the protein moiety...
  67. ncbi N-(2-hydroxypropyl)methacrylamide copolymer-6-(3-aminopropyl)-ellipticine conjugates. Synthesis, in vitro, and preliminary in vivo evaluation
    F Searle
    Centre for Polymer Therapeutics, School of Pharmacy, University of London, 29/39 Brunswick Square, London WC1N 1AX, UK
    Bioconjug Chem 12:711-8. 2001
    ..p. was somewhat more active (highest T/C value of 143%) than free APE (1 mg/kg) (T/C =127%). HPMA copolymer-APE conjugates warrant further evaluation as potential anticancer agents...
  68. doi Antitumor activity of pyridocarbazole and benzopyridoindole derivatives that inhibit protein kinase CK2
    Renaud Prudent
    INSERM, U873, Grenoble, France
    Cancer Res 70:9865-74. 2010
    ..Our work lays the foundation for development of clinically useful CK2 inhibitors derived from a well-studied scaffold with suitable pharmacokinetics parameters...
  69. ncbi A high-content chemical screen identifies ellipticine as a modulator of p53 nuclear localization
    G Wei Xu
    Ontario Cancer Institute, Princess Margaret Hospital, 610 University Ave, M5G 2M9, Toronto, ON, Canada
    Apoptosis 13:413-22. 2008
    ..Thus, a chemical biology approach has identified a molecule that shifts the localization of p53 and enhances its nuclear activity...
  70. ncbi Bioinformatics-based discovery and characterization of an AKT-selective inhibitor 9-chloro-2-methylellipticinium acetate (CMEP) in breast cancer cells
    Manchao Zhang
    Department of Biochemistry and Molecular Pharmacology, West Virginia University, 1 Medical Center Drive, Morgantown, WV 26506 9142, USA
    Cancer Lett 252:244-58. 2007
    ..CMEP inhibits growth and induces apoptosis in cancer cells which have high-levels of AKT activation and lack PTEN or harbor PTEN mutation...
  71. ncbi Patterns of strongly protein-associated simian virus 40 DNA replication intermediates resulting from exposures to specific topoisomerase poisons
    C G Shin
    Department of Radiology, Ohio State University, Columbus 43210 1214
    Biochemistry 29:10934-9. 1990
    ..The protein associated with form I DNA may represent a drug-stabilized "topological complex" between type II topoisomerase and SV40 DNA...
  72. ncbi The development of VIP-ellipticine conjugates
    Terry W Moody
    Department of Health and Human Services, NCI Office of the Director, CCR, Building 31, Room 3A34, 31 Center Drive, Bethesda, MD 20892, USA
    Regul Pept 123:187-92. 2004
    ..These results suggest that VIP-E conjugates are internalized in lung cancer cells as a result of VPAC1 receptor-mediated endocytosis...
  73. ncbi Synthesis, electrochemistry, and bioactivity of the cyanobacterial calothrixins and related quinones
    Paul H Bernardo
    Department of Chemistry and School of Biochemistry and Molecular Biology, Centre for the Study of Bioactive Molecules, Australian National University, ACT 0200, Australia
    J Med Chem 47:4958-63. 2004
    ..6 microM undergo reduction to their respective semiquinones readily, with their E(1/2) values being more positive than -0.5 V versus the standard hydrogen electrode (SHE)...
  74. ncbi Synthesis and cytotoxic activity of pyranocarbazole analogues of ellipticine and acronycine
    Hong Anh Tran-Thi
    Laboratoire de pharmacognosie de l Université René Descartes, U M R C N R S n degrees 8638, Faculte des Sciences Pharmaceutiques et Biologiques, Paris, France
    Chem Pharm Bull (Tokyo) 52:540-5. 2004
    ..The study of the biological properties of the new pyrano[3,2-b]carbazole derivatives was carried out in vitro on L1210 murine leukaemia cell line. The three (+/-)-cis-diol diesters 15, 16, and 18 were the most active compounds...
  75. ncbi Effect of LNA modifications on small molecule binding to nucleic acids
    V Marin
    Santaris Pharma A S, Boge Alle 3, DK 2970 Horsholm, Denmark
    J Biomol Struct Dyn 21:841-50. 2004
    ..The lone exception is the alkaloid ellipticine, which intercalates into LNA-DNA and LNA-RNA duplexes with affinities comparable to unmodified DNA-DNA and RNA-DNA duplexes...
  76. ncbi Small molecules that reactivate mutant p53
    V J N Bykov
    Department of Oncology Pathology, Cancer Center Karolinska, SE 171 76 Stockholm, Sweden
    Eur J Cancer 39:1828-34. 2003
    ..Various types of small molecules have been identified that can restore native conformation and wild-type function to mutant p53. Such molecules may serve as leads for the development of novel efficient anticancer drugs...
  77. ncbi Rat microsomes activating the anticancer drug ellipticine to species covalently binding to deoxyguanosine in DNA are a suitable model mimicking ellipticine bioactivation in humans
    Marie Stiborova
    Department of Biochemistry, Faculty of Science, Charles University, Albertov 2030, 12840 Prague 2, Czech Republic
    Chem Res Toxicol 16:38-47. 2003
    ..The results strongly suggest that rats are more suitable models than rabbits mimicking the metabolic activation of ellipticine in humans...
  78. ncbi Identification of new drug sensitivity genes using genetic suppressor elements: protein arginine N-methyltransferase mediates cell sensitivity to DNA-damaging agents
    Laurent Gros
    Centre National de la Recherche Scientifique UMR 8532, Institut Gustave Roussy, 94805 Villejuif, France
    Cancer Res 63:164-71. 2003
    ..Our data indicate that down-regulation of these enzymes in the GSE-expressing cells would alter one or several steps downstream of the drug-target interaction in the drug-response pathway...
  79. ncbi Clinical phase I and pharmacokinetic study of S 16020, a new olivacine derivative: report on three infusion schedules
    A Awada
    Jules Bordet Institute, Brussels, Belgium
    Ann Oncol 13:1925-34. 2002
    ..Based on the overall data of the three infusion schedules of S 16020, the dose of 100 mg/m(2) over 3 h every 3 weeks was selected for phase II studies...
  80. ncbi Cardioprotective effects of 9-hydroxyellipticine on ischemia and reperfusion in isolated rat heart
    Kazuhiko Saeki
    Discovery Research Laboratory, Tanabe Seiyaku Co, Toda shi, Saitama, Japan
    Jpn J Pharmacol 89:21-8. 2002
    ..Unlike nifedipine, an L-type Ca2+-channel blocker, 9HE did not suppress the contraction of rat papillary muscles. Thus, 9HE exerts the cardioprotective effects against ischemia /reperfusion injury without changing hemodynamic indices...
  81. ncbi A unique type II topoisomerase mutant that is hypersensitive to a broad range of cleavage-inducing antitumor agents
    Erin K O'Reilly
    Department of Biochemistry, Duke University Medical Center, Box 3020, Durham, NC 27710, USA
    Biochemistry 41:7989-97. 2002
    ..We believe that this mutant defines a new category of type II topoisomerase mutants, namely, those that are hypersensitive to all inhibitors that stabilize the cleavage complex...
  82. ncbi Potent inhibition of DNA unwinding and ATPase activities of pea DNA helicase 45 by DNA-binding agents
    Xuan Hoi Pham
    Plant Molecular Biology Group, International Centre for Genetic Engineering and Biotechnology, P O Box 10504, Aruna Asaf Ali Marg, New Delhi 110 067, India
    Biochem Biophys Res Commun 294:334-9. 2002
    ..This study would be useful to obtain a better understanding of the mechanism of plant nuclear DNA helicase unwinding and the mechanism by which these agents can disturb genome integrity...
  83. ncbi Complex formation in the indolo[2,3-b]quinolines--methylene blue systems in aqueous solutions
    N Sadlej-Sosnowska
    Drug Institute, Warsaw, Poland
    Spectrochim Acta A Mol Biomol Spectrosc 57:199-205. 2001
    ..The estimated association constants were correlated with the ab initio calculated electronic properties of indolo[2,3-b]quinolines...
  84. ncbi Indications for the involvement of a CYP3A-like iso-enzyme in the metabolism of chlorobornane (Toxaphene) congeners in seals from inhibition studies with liver microsomes
    C M van Hezik
    Netherlands Institute for Sea Research NIOZ, P O Box 59, 1790 AB Den Burg, Texel, The Netherlands
    Aquat Toxicol 51:319-33. 2001
    ..Stereochemical preferences of biotransformation enzymes can have an influence on the environmental distribution of both enantiomers of optically active compounds...
  85. ncbi Combinations of three or four HIV virostatics applied in short sequences which differ from each other by drug rotation. Preliminary results of the viral loads and CD4 numbers
    G Mathe
    Institut de Cancérologie et d Immunologie and Hôpital Suisse de Paris, Issy les Moulineaux, France
    Biomed Pharmacother 51:417-26. 1997
    ..This CD4 restoration limitation can be due to persisting virus, as indicated in some patients by small peaks which may appear on some VL plateaus, though they disappear without treatment change...
  86. ncbi Induction of somatic mutation and recombination by four inhibitors of eukaryotic topoisomerases assayed in the wing spot test of Drosophila melanogaster
    H Frei
    Institute of Toxicology, Swiss Federal Institute of Technology ETH and University of Zurich, Schorenstrasse 16, CH 8603 Schwerzenbach, Switzerland
    Mutagenesis 11:315-25. 1996
    ..Only suggestions can be proffered at present as to how these proportions could be related to the primary damage produced by the respective compounds on the chromosomes...
  87. ncbi Analysis of the DNA topoisomerase-II-mediated cleavage of the long terminal repeat of Drosophila 1731 retrotransposon
    E Nahon
    URA Centre National de la Recherche Scientifique, Universite Pierre et Marie Curie, Paris, France
    Eur J Biochem 218:95-102. 1993
    ..Our results suggest that DNA topoisomerase II, through its ability to alter the degree of DNA supercoiling, might be involved in the control of different functions of the LTR...
  88. ncbi Novel partitioning of DNA cleavage sites for Drosophila topoisomerase II
    A Udvardy
    Cell 40:933-41. 1985
    ..In addition, most of the major topoisomerase II cleavage sites closely corresponded to naked DNA hypersensitive sites for the prokaryotic enzyme, micrococcal nuclease...
  89. ncbi Synthesis, structure, and cytostatic properties of new olivacine derivatives
    Ryszard Jasztold-Howorko
    Wrocław University of Medicine, Faculty of Pharmacy, Department of Organic Chemistry, Wrocław, Poland
    Arch Pharm (Weinheim) 337:599-604. 2004
    ..The newly obtained compounds showed significant cytostatic activity against cultured L1210 cells and high cytotoxicity towards various human tumor cell lines...
  90. ncbi Synthesis, antitumour activity and structure-activity relationships of 5H-benzo[b]carbazoles
    Christian Asche
    LEDSS, UMR CNRS 5616, Universite Joseph Fourier, BP 53, 38041 Grenoble Cedex 9, France
    Bioorg Med Chem 13:819-37. 2005
    A series of novel 5H-benzo[b]carbazoles related to the ellipticines was obtained from the reactions of p-benzoquinones with 2-aminomethylene-1-indanones...
  91. ncbi Influence of serum protein on polycarbonate-based copolymer micelles as a delivery system for a hydrophobic anti-cancer agent
    Jubo Liu
    Department of Pharmaceutical Sciences, University of Toronto, 19 Russell St, Toronto, Ontario, Canada M5S 2S2
    J Control Release 103:481-97. 2005
    ..These studies demonstrate that although there are no significant interactions between micelle and protein, the properties of the micelle as a delivery vehicle may be strongly influenced by protein-drug interactions...
  92. ncbi Type II topoisomerase activities in both the G1 and G2/M phases of the dinoflagellate cell cycle
    Carmen K M Mak
    Biology Department, Hong Kong University of Science and Technology, Clearwater Bay, Kowloon, Hong Kong SAR, People s Republic of China
    Chromosoma 114:420-31. 2005
    ..This was also the first time that topoisomerase II activity in dinoflagellate cells was detected...
  93. ncbi Synthesis of ellipticine: a radical cascade protocol to aryl- and heteroaryl-annulated[b]carbazoles
    Jan M Pedersen
    Department of Chemistry, Loughborough University, Loughborough, Leics LE11 3TU, Great Britain
    J Org Chem 70:10615-8. 2005
    ..The protocol has been exemplified with the high-yielding total synthesis of the anticancer alkaloid ellipticine...
  94. ncbi Regioselective 6-endo cyclizations of 2-indolylacyl radicals: total synthesis of the pyrido[4,3-b]carbazole alkaloid guatambuine
    M Lluïsa Bennasar
    Laboratory of Organic Chemistry, Faculty of Pharmacy, University of Barcelona, Barcelona 08028, Spain
    J Org Chem 71:1746-9. 2006
    ....
  95. ncbi A small molecule compound inhibits AKT pathway in ovarian cancer cell lines
    Huai Jing Tang
    Department of Obstetrics and Gynecology, University of Michigan Comprehensive Cancer Center, Ann Arbor, MI 48109, USA
    Gynecol Oncol 100:308-17. 2006
    ..Therefore, development of potent inhibitors that block AKT pathway is an attractive therapeutic strategy for treating ovarian carcinoma...
  96. ncbi Regioselective intramolecular reactions of 2-indolylacyl radicals with pyridines: a direct synthetic entry to ellipticine quinones
    M Lluïsa Bennasar
    Laboratory of Organic Chemistry, Faculty of Pharmacy, University of Barcelona, Spain
    J Org Chem 70:9077-80. 2005
    ..For substrates bearing a (3-pyridyl)methyl moiety connected to the 3-position of the indole ring, the cyclization provides easy access to ellipticine quinones...
  97. ncbi Lack of CYP1A1 expression is involved in unresponsiveness of the human hepatoma cell line SK-HEP-1 to dioxin
    Kazuhiro Shiizaki
    Environmental Health Sciences Division, National Institute for Environmental Studies, Tsukuba 305 8506, Japan
    Toxicol Lett 160:22-33. 2005
    ..Our findings demonstrated the presence of endogenous ligands in SK-HEP-1 cells due to the absence of the metabolizing enzyme CYP1A1, but not CYP1B1, which allowed the constitutive expression of AhR target genes...
  98. ncbi The anti-proliferative inhibition of ellipticine in human breast mda-mb-231 cancer cells is through cell cycle arrest and apoptosis induction
    Po Lin Kuo
    Department of Biotechnology, Chia Nan University of Pharmacy and Science, Tainan, Taiwan
    Anticancer Drugs 16:789-95. 2005
    ..Taken together, our study suggests that the inhibition of cell cycle progression signaling and initiation of the mitochondrial apoptotic system may participate in the anti-proliferative activity of ellipticine in MDA-MB-231 cells...
  99. ncbi Blockage of epidermal growth factor receptor-phosphatidylinositol 3-kinase-AKT signaling increases radiosensitivity of K-RAS mutated human tumor cells in vitro by affecting DNA repair
    Mahmoud Toulany
    Divison of Radiobiology and Molecular Environmental Research, Department of Radiation Oncology, University of Tuebingen, Tuebingen, Germany
    Clin Cancer Res 12:4119-26. 2006
    ..In the present study, we investigated whether impaired repair of DNA double-strand breaks (DSB) is responsible for the radiosensitizing effect of EGFR and PI3K inhibition in K-RAS mutated (K-RAS(mt)) cells...
  100. ncbi Antitumor drug ellipticine inhibits the activities of rat hepatic cytochromes P450
    Dagmar Aimová
    Department of Biochemistry, Charles University, Albertov 2030, Prague 2, Czech Republic
    Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub 149:437-40. 2005
    ..The results indicate that inhibition of CYPs by ellipticine cannot be explained only by its differential potency to bind to individual CYPs...
  101. ncbi The role of hydrogen bond acceptor groups in the interaction of substrates with Pdr5p, a major yeast drug transporter
    Leanne Hanson
    Department of Biology, The Catholic University of America, Washington, DC 20064, USA
    Biochemistry 44:9703-13. 2005
    ..The presence of multiple sites with different requirements for substrate-Pdr5p interaction may explain the broad specificity of xenobiotic compounds transported by this protein...

Research Grants24

  1. ANTITUMOR AGENTS AND THE BACTERIOPHAGE T4 TOPOISOMERASE
    Kenneth Kreuzer; Fiscal Year: 2001
    ..is sensitive to many of the antitumor agents that inhibit the mammalian enzyme, including m-AMSA, mitoxantrone, ellipticines and epipodophyllotoxins...
  2. REGULATION OF TOPOISOMERASE I AND II PHOSPHORYLATION
    Thomas Rowe; Fiscal Year: 1993
    ..the camptothecins (topoisomerase I-active drugs) and the anthracyclines, amsacrines, epipodophyllotoxins, and ellipticines (topoisomerase II-active drugs). This proposal will focus on two areas of research...
  3. THIOXANTHENONES AND ELLIPTICINES AS ANTITUMOR AGENTS
    SYDNEY ARCHER; Fiscal Year: 1990
    ..It is suggested that these drugs are involved in the irreversible interaction with the mammalian DNA Topoisomerase II-DNA complex and that this is the cytotoxic event. Experiments are suggested to test the validity of this hypothesis...
  4. Direct analysis of fork blockage and DNA repair in vivo
    Kenneth Kreuzer; Fiscal Year: 2005
    ..We will attempt to deliver DNA with site-specific abasic sites into living E. coli cells, and physically analyze repair and replication fork blockage at these sites. ..
  5. INITIATION OF DNA REPLICATION IN THE PHAGE T4 SYSTEM
    Kenneth Kreuzer; Fiscal Year: 2005
    ....
  6. Direct analysis of fork blockage and DNA repair in vivo
    Kenneth Kreuzer; Fiscal Year: 2006
    ..We will attempt to deliver DNA with site-specific abasic sites into living E. coli cells, and physically analyze repair and replication fork blockage at these sites. [unreadable] [unreadable]..
  7. Direct analysis of fork blockage and DNA repair in vivo
    Kenneth Kreuzer; Fiscal Year: 2007
    ..We will attempt to deliver DNA with site-specific abasic sites into living E. coli cells, and physically analyze repair and replication fork blockage at these sites. [unreadable] [unreadable]..
  8. Duke PREP: Minority Recruitment into Biomedical Sciences
    Kenneth Kreuzer; Fiscal Year: 2007
    ..The PREP scholars will be encouraged to take advantage of the full two-year experience, as long as they perform at an acceptable level and maintain an interest in pursuing a career in science. ..
  9. Processing and consequences of DNA-protein crosslinks in E. coli
    Kenneth Kreuzer; Fiscal Year: 2009
    ..In addition, the pathways of replication fork failure and the repair of DNA- protein crosslinks are issues relevant to the genome instability that can lead to the formation of cancers. ..
  10. Processing and consequences of DNA-protein crosslinks in E. coli
    Kenneth N Kreuzer; Fiscal Year: 2010
    ..In addition, the pathways of replication fork failure and the repair of DNA- protein crosslinks are issues relevant to the genome instability that can lead to the formation of cancers. ..
  11. Processing and consequences of DNA-protein crosslinks in E. coli
    Kenneth N Kreuzer; Fiscal Year: 2010
    ..In addition, the pathways of replication fork failure and the repair of DNA- protein crosslinks are issues relevant to the genome instability that can lead to the formation of cancers. ..
  12. Direct analysis of fork blockage and DNA repair in vivo
    Kenneth Kreuzer; Fiscal Year: 2004
    ..We will attempt to deliver DNA with site-specific abasic sites into living E. coli cells, and physically analyze repair and replication fork blockage at these sites. ..
  13. Direct analysis of fork blockage and DNA repair in vivo
    Kenneth Kreuzer; Fiscal Year: 2003
    ..If the system is validated, many other kinds of DNA damage can presumably be analyzed in-future studies. ..
  14. ANTITUMOR AGENTS AND THE BACTERIOPHAGE T4 TOPOISOMERASE
    Kenneth Kreuzer; Fiscal Year: 1999
    ..is sensitive to many of the antitumor agents that inhibit the mammalian enzyme, including m-AMSA, mitoxantrone, ellipticines and epipodophyllotoxins...
  15. ANTITUMOR AGENTS AND THE BACTERIOPHAGE T4 TOPOISOMERASE
    Kenneth Kreuzer; Fiscal Year: 1993
    ..of the same antitumor agents that inhibit the mammalian type II topoisomerase, including m-AMSA, mitoxantrone, ellipticines and epipodophyllotoxins...
  16. ANTITUMOR AGENTS AND THE BACTERIOPHAGE T4 TOPOISOMERASE
    Kenneth Kreuzer; Fiscal Year: 2000
    ..is sensitive to many of the antitumor agents that inhibit the mammalian enzyme, including m-AMSA, mitoxantrone, ellipticines and epipodophyllotoxins...
  17. Processing and consequences of DNA-protein crosslinks in E. coli
    Kenneth N Kreuzer; Fiscal Year: 2010
    ..In addition, the pathways of replication fork failure and the repair of DNA- protein crosslinks are issues relevant to the genome instability that can lead to the formation of cancers. ..