antitumor drug screening assays

Summary

Summary: Methods of investigating the effectiveness of anticancer cytotoxic drugs and biologic inhibitors. These include in vitro cell-kill models and cytostatic dye exclusion tests as well as in vivo measurement of tumor growth parameters in laboratory animals.

Top Publications

  1. ncbi Chemistry and biology of the tetrahydroisoquinoline antitumor antibiotics
    Jack D Scott
    Department of Chemistry, Colorado State University, Fort Collins, CO 80523, USA
    Chem Rev 102:1669-730. 2002
  2. ncbi Antitumor activity of the antimicrobial peptide magainin II against bladder cancer cell lines
    Jan Lehmann
    Department of Urology and Pediatric Urology, Saarland University, Homburg Saar, Germany
    Eur Urol 50:141-7. 2006
  3. ncbi Discovery of embelin as a cell-permeable, small-molecular weight inhibitor of XIAP through structure-based computational screening of a traditional herbal medicine three-dimensional structure database
    Zaneta Nikolovska-Coleska
    University of Michigan Comprehensive Cancer Center, Departments of Internal Medicine and Medicinal Chemistry, University of Michigan, Ann Arbor, Michigan 48109 0934, USA
    J Med Chem 47:2430-40. 2004
  4. ncbi Prediction of chemotherapeutic response by collagen gel droplet embedded culture-drug sensitivity test in human breast cancers
    Yuuki Takamura
    Department of Surgical Oncology, Osaka University Medical School, Yamada oka, Suita, Osaka, Japan
    Int J Cancer 98:450-5. 2002
  5. ncbi Molecular modes of action of artesunate in tumor cell lines
    Thomas Efferth
    Center for Molecular Biology of the University of Heidelberg ZMBH, Heidelberg, Germany
    Mol Pharmacol 64:382-94. 2003
  6. ncbi Eusynstyelamides A, B, and C, nNOS inhibitors, from the ascidian Eusynstyela latericius
    Dianne M Tapiolas
    Australian Institute of Marine Science, PMB No 3, Townsville MC, Queensland, 4810, Australia
    J Nat Prod 72:1115-20. 2009
  7. pmc Systematic discovery of multicomponent therapeutics
    Alexis A Borisy
    CombinatoRx Incorporated, 650 Albany Street, Boston, MA 02118, USA
    Proc Natl Acad Sci U S A 100:7977-82. 2003
  8. pmc Actinomycetes for marine drug discovery isolated from mangrove soils and plants in China
    Kui Hong
    Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agriculture Sciences, Haikou 571101, PR China
    Mar Drugs 7:24-44. 2009
  9. ncbi Activity of the dual kinase inhibitor lapatinib (GW572016) against HER-2-overexpressing and trastuzumab-treated breast cancer cells
    Gottfried E Konecny
    Division of Hematology Oncology, Department of Medicine, David Geffen School of Medicine, University of California at Los Angeles, 12 145 Factor Building, 10945 Le Conte Avenue, Los Angeles, CA 90095 1678, USA
    Cancer Res 66:1630-9. 2006
  10. ncbi Histone deacetylases and cancer: causes and therapies
    P Marks
    Memorial Sloan Kettering Cancer Center, New York, New York 10021, USA
    Nat Rev Cancer 1:194-202. 2001

Detail Information

Publications285 found, 100 shown here

  1. ncbi Chemistry and biology of the tetrahydroisoquinoline antitumor antibiotics
    Jack D Scott
    Department of Chemistry, Colorado State University, Fort Collins, CO 80523, USA
    Chem Rev 102:1669-730. 2002
  2. ncbi Antitumor activity of the antimicrobial peptide magainin II against bladder cancer cell lines
    Jan Lehmann
    Department of Urology and Pediatric Urology, Saarland University, Homburg Saar, Germany
    Eur Urol 50:141-7. 2006
    ..In this study, we evaluated the cytotoxic and antiproliferative potency of magainin II in bladder tumor cells and normal fibroblasts...
  3. ncbi Discovery of embelin as a cell-permeable, small-molecular weight inhibitor of XIAP through structure-based computational screening of a traditional herbal medicine three-dimensional structure database
    Zaneta Nikolovska-Coleska
    University of Michigan Comprehensive Cancer Center, Departments of Internal Medicine and Medicinal Chemistry, University of Michigan, Ann Arbor, Michigan 48109 0934, USA
    J Med Chem 47:2430-40. 2004
    ....
  4. ncbi Prediction of chemotherapeutic response by collagen gel droplet embedded culture-drug sensitivity test in human breast cancers
    Yuuki Takamura
    Department of Surgical Oncology, Osaka University Medical School, Yamada oka, Suita, Osaka, Japan
    Int J Cancer 98:450-5. 2002
    ..These results demonstrate that CD-DST can predict the response to CE and DOC therapy with a high accuracy in breast cancer patients and seems to be superior to the conventional predictors...
  5. ncbi Molecular modes of action of artesunate in tumor cell lines
    Thomas Efferth
    Center for Molecular Biology of the University of Heidelberg ZMBH, Heidelberg, Germany
    Mol Pharmacol 64:382-94. 2003
    ..ART acts via p53-dependent and- independent pathways in isogenic p53+/+ p21WAF1/CIP1+/+, p53-/- p21WAF1/CIP1+/+, and p53+/+ p21WAF1/CIP1-/- colon carcinoma cells...
  6. ncbi Eusynstyelamides A, B, and C, nNOS inhibitors, from the ascidian Eusynstyela latericius
    Dianne M Tapiolas
    Australian Institute of Marine Science, PMB No 3, Townsville MC, Queensland, 4810, Australia
    J Nat Prod 72:1115-20. 2009
    ..6 and 6.5 mM, respectively) and mild inhibitory activity toward the C(4) plant regulatory enzyme pyruvate phosphate dikinase (PPDK) (IC(50) values of 19 and 20 mM, respectively)...
  7. pmc Systematic discovery of multicomponent therapeutics
    Alexis A Borisy
    CombinatoRx Incorporated, 650 Albany Street, Boston, MA 02118, USA
    Proc Natl Acad Sci U S A 100:7977-82. 2003
    ..Systematic combination screening may ultimately be useful for exploring the connectivity of biological pathways and, when performed with reference-listed drugs, may result in the discovery of new combination drug regimens...
  8. pmc Actinomycetes for marine drug discovery isolated from mangrove soils and plants in China
    Kui Hong
    Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agriculture Sciences, Haikou 571101, PR China
    Mar Drugs 7:24-44. 2009
    ..We conclude that actinomycetes isolated from mangrove habitats are a potentially rich source for the discovery of anti-infection and anti-tumor compounds, and of agents for treating neurodegenerative diseases and diabetes...
  9. ncbi Activity of the dual kinase inhibitor lapatinib (GW572016) against HER-2-overexpressing and trastuzumab-treated breast cancer cells
    Gottfried E Konecny
    Division of Hematology Oncology, Department of Medicine, David Geffen School of Medicine, University of California at Los Angeles, 12 145 Factor Building, 10945 Le Conte Avenue, Los Angeles, CA 90095 1678, USA
    Cancer Res 66:1630-9. 2006
    ..These observations provide a clear biological rationale to test lapatinib as a single agent or in combination with trastuzumab in HER-2-overexpressing breast cancer and in patients with clinical resistance to trastuzumab...
  10. ncbi Histone deacetylases and cancer: causes and therapies
    P Marks
    Memorial Sloan Kettering Cancer Center, New York, New York 10021, USA
    Nat Rev Cancer 1:194-202. 2001
    ..HDAC inhibitors are proving to be an exciting therapeutic approach to cancer, but how do they exert this effect?..
  11. ncbi Chemotherapy sensitivity and response assays: are the ASCO guidelines for clinical trial design too restrictive?
    H Samuel Wieand
    J Clin Oncol 23:3643-4; author reply 3646-8. 2005
  12. ncbi An information-intensive approach to the molecular pharmacology of cancer
    J N Weinstein
    Laboratory of Molecular Pharmacology LMP, Division of Basic Science, National Cancer Institute NCI, National Institutes of Health, Bethesda, MD 20892, USA
    Science 275:343-9. 1997
    ..It remains to be seen how effective this information-intensive strategy will be at generating new clinically active agents...
  13. ncbi Predictive value of the ATP chemosensitivity assay in epithelial ovarian cancer
    A T O'Meara
    Division of Gynecologic Oncology, University of Southern California, Keck School of Medicine, 1240 N Mission Road, Room 1L4, Los Angeles, California 90033, USA
    Gynecol Oncol 83:334-42. 2001
    ....
  14. ncbi Genetically engineered models have advantages over xenografts for preclinical studies
    Oren J Becher
    Department of Cancer Biology and Genetics, Memorial Sloan Kettering Cancer Center, 1275 York Avenue, New York, NY 10021, USA
    Cancer Res 66:3355-8, discussion 3358-9. 2006
    ..These new technologies will hopefully support the use of GEMs in preclinical trials and help determine if trials in GEMs are more predicative than xenografts of human responses...
  15. pmc Anticancer drug clustering in lung cancer based on gene expression profiles and sensitivity database
    Akihiko Gemma
    The Fourth Department of Medicine, Nippon Medical School, 1 1 5, Sendagi, Bunkyo ku, Tokyo, 113 8602, Japan
    BMC Cancer 6:174. 2006
    ..It is consequently desirable to find more appropriate therapeutic opportunities based on informed insights. A molecular pharmacological analysis was undertaken to design an improved chemotherapeutic strategy for advanced lung cancer...
  16. pmc In vitro and in vivo activity and cross resistance profiles of novel ruthenium (II) organometallic arene complexes in human ovarian cancer
    R E Aird
    Cancer Research UK, Edinburgh Oncology Unit, Western General Hospital, Crewe Road South, Edinburgh EH4 2XR, UK
    Br J Cancer 86:1652-7. 2002
    ..High activity coupled to non cross-resistance in cisplatin resistant models merit further development of this novel group of anticancer compounds...
  17. ncbi Predicting drug sensitivity and resistance: profiling ABC transporter genes in cancer cells
    Gergely Szakacs
    Laboratory of Cell Biology, Center for Cancer Research, NCI, NIH, Bethesda, MD, 20892, USA
    Cancer Cell 6:129-37. 2004
    ..Unexpectedly, we also found and validated compounds whose activity is potentiated, rather than antagonized, by the MDR1 multidrug transporter. Such compounds may serve as leads for development...
  18. ncbi Impact of adjuvant inhibition of vascular endothelial growth factor receptor tyrosine kinases on tumor growth delay and local tumor control after fractionated irradiation in human squamous cell carcinomas in nude mice
    Daniel Zips
    Department of Radiation Oncology, Medical Faculty Carl Gustav Carus, University of Technology Dresden, Fetscherstrasse 74, 01307 Dresden, Germany
    Int J Radiat Oncol Biol Phys 61:908-14. 2005
    ..To test the latter hypothesis, local tumor control experiments were performed...
  19. ncbi Orthotopic metastatic mouse models for anticancer drug discovery and evaluation: a bridge to the clinic
    R M Hoffman
    AntiCancer, Inc, San Diego, CA 92111, USA
    Invest New Drugs 17:343-59. 1999
    ..These unique SOI models have been used for innovative drug discovery and mechanism studies and serve as a bridge linking pre-clinical and clinical research and drug development...
  20. ncbi Influence of p53 and p21(WAF1) expression on sensitivity of cancer cells to cladribine
    Carlos Maria Galmarini
    INSERM 453 8 Avenue Rockefeller, 69373 Lyon Cedex 08, France
    Biochem Pharmacol 65:121-9. 2003
    ..We conclude that p53 and p21(WAF1) status of cancer cells influences their sensitivity to 2-CdA cytotoxicity. This may involve alterations in the apoptotic cascade as well as in PARP-1-dependent cell death...
  21. ncbi Development of an in vitro multicellular tumor spheroid model using microencapsulation and its application in anticancer drug screening and testing
    Xulang Zhang
    Laboratory of Biomedical Material Engineering, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, 457 Zhongshan Road, Dalian 116023, China
    Biotechnol Prog 21:1289-96. 2005
    ..It demonstrated that the MMTS has the potential to be a rapid and valid in vitro model to screen chemotherapeutic drugs with a feature to mimic in vivo three-dimensional (3-D) cell growth pattern...
  22. ncbi Antitumor effects due to irreversible stoppage of tumor tissue blood flow: evaluation of a novel combretastatin A-4 derivative, AC7700
    K Hori
    Department of Vascular Biology, Institute of Development, Aging and Cancer, Tohoku University, Sendai
    Jpn J Cancer Res 90:1026-38. 1999
    ..AC7700 has been demonstrated to be a promising anticancer compound which has such an action...
  23. ncbi Synthesis of chlorin e6-transferrin and demonstration of its light-dependent in vitro breast cancer cell killing ability
    Philip G Cavanaugh
    The Institute for Molecular Medicine, Huntington Beach, CA 92649, USA
    Breast Cancer Res Treat 72:117-30. 2002
    ..The conjugate demonstrated potential as an anti-cancer agent...
  24. pmc EGFR associated expression profiles vary with breast tumor subtype
    Katherine A Hoadley
    Curriculum in Genetics and Molecular Biology, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA
    BMC Genomics 8:258. 2007
    ..An EGFR-associated gene expression signature was identified in the basal-like SUM102 cell line and was used to classify a diverse set of sporadic breast tumors...
  25. pmc Relationship between expression of topoisomerase II isoforms and intrinsic sensitivity to topoisomerase II inhibitors in breast cancer cell lines
    S Houlbrook
    Molecular Oncology Laboratories, Imperial Cancer Research Fund, John Radcliffe Hospital, Oxford, UK
    Br J Cancer 72:1454-61. 1995
    ..No relationship was found between the level of mRNA for topoisomerase II alpha or beta, and either sensitivity of breast cancer cell lines to topoisomerase II inhibitors or the level of topoisomerase II protein expression...
  26. ncbi Sensitization of human tumor cells to CPT-11 via adenoviral-mediated delivery of a rabbit liver carboxylesterase
    M Wierdl
    Department of Molecular Pharmacology, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, USA
    Cancer Res 61:5078-82. 2001
    ..These data suggest that the described reagents may be suitable for use in vivo in a viral-directed enzyme prodrug therapy approach using CPT-11...
  27. pmc Appraisal of the MTT assay as a rapid test of chemosensitivity in acute myeloid leukaemia
    J M Sargent
    Department of Haematology, Pembury Hospital, Kent, UK
    Br J Cancer 60:206-10. 1989
    ..The test can be repeated throughout the course of the disease to help identify any change in tumour sensitivity. This technique appears to give useful information to assist in the management of acute myeloid leukaemia...
  28. ncbi The use of an in vitro adenosine triphosphate-based chemotherapy response assay to predict chemotherapeutic response in breast cancer
    Hyun Ah Kim
    Department of Surgery, College of Medicine, Ewha Womans University and Ewha Medical Research Institute, 911 1 MokDong, Yangcheon Ku, Seoul, Republic of Korea
    Breast 17:19-26. 2008
    ..Our results show that ATP-CRA has high specificity and positive predictive value for predicting response to chemotherapy...
  29. ncbi Differential sensitivity of human colon cancer cell lines to the nucleoside analogs ARC and DRB
    Uppoor G Bhat
    Department of Medicine, University of Illinois at Chicago, Chicago, IL 60612, USA
    Int J Cancer 122:1426-9. 2008
    ..Overall, ARC could represent an attractive candidate for anti-cancer drug development that targets multiple survival pathways in colon cancer cells...
  30. ncbi Aurilides B and C, cancer cell toxins from a Papua New Guinea collection of the marine cyanobacterium Lyngbya majuscula
    Bingnan Han
    College of Pharmacy, Oregon State University, Corvallis, OR 97331, USA
    J Nat Prod 69:572-5. 2006
    ....
  31. ncbi Adenosine triphosphate-based chemotherapy response assay (ATP-CRA)-guided platinum-based 2-drug chemotherapy for unresectable nonsmall-cell lung cancer
    Yong Wha Moon
    Department of Internal Medicine, Yonsei Cancer Center, Yonsei University College of Medicine, Seoul, and Department of Division of Hemato Oncology, National Health Insurance Corp, Ilsan Hospital, Kyonggi Do, Korea
    Cancer 109:1829-35. 2007
    ..The study investigated correlations between adenosine triphosphate / chemotherapy response assay (ATP-CRA) and clinical outcomes after ATP-CRA-guided platinum-based chemotherapy for unresectable nonsmall-cell lung cancer (NSCLC)...
  32. pmc Metabolomic profiling of drug responses in acute myeloid leukaemia cell lines
    Stefano Tiziani
    CR UK Institute for Cancer Studies, University of Birmingham, Henry Wellcome Building for Biomolecular NMR Spectroscopy HWB NMR, Birmingham, United Kingdom
    PLoS ONE 4:e4251. 2009
    ..This opens new perspectives to use metabolic profiling as a tool to study the rational redeployment of drugs in new disease settings...
  33. ncbi The anti-malarial artesunate is also active against cancer
    T Efferth
    Virtual Campus Rhineland Palatinate, P O Box 4380, D 55033 Mainz, Germany
    Int J Oncol 18:767-73. 2001
    ..None of the other DNA repair or DNA check-point deficient isogenic strains were different from the wild-type. These results and the known low toxicity of ART are clues that ART may be a promising novel candidate for cancer chemotherapy...
  34. ncbi Micro-array analysis of resistance for gemcitabine results in increased expression of ribonucleotide reductase subunits
    K Smid
    Department of Medical Oncology, VU University Medical Center, Amsterdam, The Netherlands
    Nucleosides Nucleotides Nucleic Acids 25:1001-7. 2006
    ..Culture in the absence of gemcitabine reduced resistance as well as RRM1 RNA expression, demonstrating a direct relationship of RRM1 RNA expression with acquired resistance to gemcitabine...
  35. ncbi Redefining the target: chemotherapeutics as antiangiogenics
    K D Miller
    Division of Hematology and Oncology, Indiana University School of Medicine, Indianapolis, IN, USA
    J Clin Oncol 19:1195-206. 2001
    ..Finally, we describe potential mechanisms of resistance to antiangiogenic chemotherapies-some of which may apply to the pure antiangiogenics currently in development...
  36. ncbi Impact of intracellular chloride concentration on cisplatin accumulation in sensitive and resistant GLC4 cells
    Milena Salerno
    Laboratoire de Biophysique Moléculaire Cellulaire et Tissulaire, UMR CNRS 7033, UFR SMBH, Universite Paris 13, Bobigny, France
    J Biol Inorg Chem 14:123-32. 2009
    ..Our findings indicate that increase of intracellular chloride concentration may be a major determinant of CDDP resistance...
  37. ncbi Activity of PXD101, a histone deacetylase inhibitor, in preclinical ovarian cancer studies
    Xiaozhong Qian
    CuraGen Corporation, 322 East Main Street, Branford, CT 06405, USA
    Mol Cancer Ther 5:2086-95. 2006
    ..Taken together, these results support the clinical evaluation of PXD101 used alone or in combination therapy for the treatment of ovarian cancer...
  38. ncbi BPR0L075, a novel synthetic indole compound with antimitotic activity in human cancer cells, exerts effective antitumoral activity in vivo
    Ching Chuan Kuo
    Division of Cancer Research, National Health Research Institutes, Taipei, Taiwan, ROC
    Cancer Res 64:4621-8. 2004
    ..v. doses of 50 mg/kg in nude mice. These findings indicate BPR0L075 is a promising anticancer compound with antimitotic activity that has potential for management of various malignancies, particularly for patients with drug resistance...
  39. ncbi A prospective randomized controlled trial of tumour chemosensitivity assay directed chemotherapy versus physician's choice in patients with recurrent platinum-resistant ovarian cancer
    Ian A Cree
    Translational Oncology Research Centre, Queen Alexandra Hospital, Portsmouth, UK
    Anticancer Drugs 18:1093-101. 2007
    ..The ATP-based tumour chemosensitivity assay remains an investigational method in this condition...
  40. pmc Resistance gene expression determines the in vitro chemosensitivity of non-small cell lung cancer (NSCLC)
    Sharon Glaysher
    Translational Oncology Research Centre, Queen Alexandra Hospital, Portsmouth PO6 3LY, UK
    BMC Cancer 9:300. 2009
    ..This study has tested the hypothesis that the molecular basis of the observed in vitro chemosensitivity of NSCLC lies within the known resistance mechanisms inherent to these patients' tumors...
  41. ncbi An integrated database of chemosensitivity to 55 anticancer drugs and gene expression profiles of 39 human cancer cell lines
    Shingo Dan
    Division of Molecular Pharmacology, Cancer Chemotherapy Center, Japanese Foundation for Cancer Research, Toshima ku, Tokyo 170 8455
    Cancer Res 62:1139-47. 2002
    ..Therefore, the integrated database approach of gene expression and chemosensitivity profiles may be useful in the development of systems to predict drug efficacies of cancer cells by examining the expression levels of particular genes...
  42. pmc Identification of a small molecule with synthetic lethality for K-ras and protein kinase C iota
    Wei Guo
    Department of Thoracic and Cardiovascular Surgery, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    Cancer Res 68:7403-8. 2008
    ..Our results indicate that oncrasin-1 or its active analogues could be a novel class of anticancer agents, which effectively kill K-Ras mutant cancer cells...
  43. ncbi Structure-based design of spiro-oxindoles as potent, specific small-molecule inhibitors of the MDM2-p53 interaction
    Ke Ding
    Department of Internal Medicine, Comprehensive Cancer Center, Life Sciences Institute, University of Michigan, 1500 E Medical Center Drive, Ann Arbor, 48109, USA
    J Med Chem 49:3432-5. 2006
    ..MI-63 has excellent specificity over cancer cells with deleted p53 and shows a minimal toxicity to normal cells...
  44. ncbi Targeting the loss of the von Hippel-Lindau tumor suppressor gene in renal cell carcinoma cells
    Patrick D Sutphin
    Program in Cancer Biology, Department of Radiation Oncology, Stanford University, Stanford, California 94305, USA
    Cancer Res 67:5896-905. 2007
    ....
  45. ncbi Clinical evaluation of chemosensitivity testing for patients with unresectable non-small cell lung cancer (NSCLC) using collagen gel droplet embedded culture drug sensitivity test (CD-DST)
    Masafumi Kawamura
    Division of General Thoracic Surgery, Department of Surgery, School of Medicine, Keio University, 35 Shinanomachi, Shinjuku, Tokyo, 160 8582, Japan
    Cancer Chemother Pharmacol 59:507-13. 2007
    ..In the present study, we prospectively evaluated the clinical feasibility and efficacy of collagen gel droplet embedded culture drug sensitivity test (CD-DST) in unresectable non-small cell lung cancer (NSCLC) without previous treatment...
  46. ncbi Culicinin D, an antitumor peptaibol produced by the fungus Culicinomyces clavisporus, strain LL-12I252
    Haiyin He
    Wyeth Research, Pearl River, New York 10965, USA
    J Nat Prod 69:736-41. 2006
    ..Studies on the 3D structure of 4 using NOE data and computer modeling revealed a dominant conformation of the right-handed helix...
  47. ncbi Enhancement of Apo2L/TRAIL-mediated cytotoxicity in esophageal cancer cells by cisplatin
    Wilson S Tsai
    Section of Thoracic Oncology, Surgery Branch, Center for Cancer Research, National Cancer Institute, NIH, Room 4 4W 3940, 10 Center Drive, Bethesda, MD 20892 1502, USA
    Mol Cancer Ther 5:2977-90. 2006
    ....
  48. ncbi A novel natural compound, a cycloanthranilylproline derivative (Fuligocandin B), sensitizes leukemia cells to apoptosis induced by tumor necrosis factor related apoptosis-inducing ligand (TRAIL) through 15-deoxy-Delta 12, 14 prostaglandin J2 production
    Hiroo Hasegawa
    Department of Laboratory Medicine, Nagasaki University Graduate School of Biomedical Sciences, Nagasaki, Japan
    Blood 110:1664-74. 2007
    ..These results indicate that 15d-PGJ(2) sensitizes TRAIL-resistant cells to TRAIL in a PPAR gamma-independent manner and that the use of 15d-PGJ(2) or its inducers, such as FCB, is a new strategy for cancer therapy...
  49. ncbi The sesquiterpene lactone parthenolide induces selective apoptosis of B-chronic lymphocytic leukemia cells in vitro
    A J Steele
    Department of Hematology, Royal Free and University College Medical School, London, UK
    Leukemia 20:1073-9. 2006
    ..This is the first report showing the relative selectivity of PTL towards CLL cells. The data here warrant further investigation of this class of natural product as potential therapeutic agents for CLL...
  50. ncbi Anticancer medicines in development: assessment of bioactivity profiles within the National Cancer Institute anticancer screening data
    David G Covell
    National Cancer Institute Frederick, Developmental Therapeutics Program, Screening Technologies Branch, Laboratory of Computational Technologies, Frederick, MD 21702, USA
    Mol Cancer Ther 6:2261-70. 2007
    ..These results are extended to applications of two-dimensional structural features to further refine compound selections based on tumor panel sensitivity obtained from tumor screening results...
  51. ncbi Dihydroxystyrene metabolites from an association of the sponges Poecillastra wondoensis and Jaspis sp
    Yong Ha Chang
    College of Pharmacy, Seoul National University, Gwanak Gu, Seoul, Korea
    J Nat Prod 71:779-83. 2008
    ..Several compounds exhibited weak to moderate inhibitory effects against isocitrate lyase and sortase A enzymes derived from microorganisms...
  52. pmc Guggulsterone inhibits tumor cell proliferation, induces S-phase arrest, and promotes apoptosis through activation of c-Jun N-terminal kinase, suppression of Akt pathway, and downregulation of antiapoptotic gene products
    Shishir Shishodia
    Cytokine Research Laboratory, Department of Experimental Therapeutics, Unit 143, The University of Texas M D Anderson Cancer Center, 1515 Holcombe Boulevard, Houston, TX 77030, United States
    Biochem Pharmacol 74:118-30. 2007
    ..Overall, our results indicate that guggulsterone can inhibit cell proliferation and induce apoptosis through the activation of JNK, suppression of Akt, and downregulation of antiapoptotic protein expression...
  53. ncbi The nucleoside analog sangivamycin induces apoptotic cell death in breast carcinoma MCF7/adriamycin-resistant cells via protein kinase Cdelta and JNK activation
    Sung A Lee
    Department of Radiation Medicine, Georgetown University Medical Center, Washington, DC 20057 1482, USA
    J Biol Chem 282:15271-83. 2007
    ..Taken together, our data suggest that sangivamycin induces mitochondria-mediated apoptotic cell death of MCF7/ADR cells via activation of JNK in a protein kinase Cdelta-dependent manner...
  54. ncbi Cytotoxic withanolides from Tubocapsicum anomalum
    Pei Wen Hsieh
    Graduate Institute of Natural Products, School of Pharmcy, Kaohsiung Medical University, Kaohsiung 807, Taiwan, Republic of China
    J Nat Prod 70:747-53. 2007
    ..The structure of 1 and 3 were further confirmed by X-ray crystallographic analysis. Compounds 1, 4-6, 8-10, and 13 showed significant cytotoxic activity against Hep G2, Hep 3B, A-549, MDA-MB-231, MCF-7, and MRC-5 cell lines...
  55. ncbi Pharmacogenomic strategies provide a rational approach to the treatment of cisplatin-resistant patients with advanced cancer
    David S Hsu
    Division of Medical Oncology, Department of Medicine, Duke University, Durham, NC 27710, USA
    J Clin Oncol 25:4350-7. 2007
    ..We utilized a genomic strategy to develop signatures predictive of chemotherapeutic response to both cisplatin and pemetrexed to provide a rational approach to effective individualized medicine...
  56. ncbi (1)H and (13)C NMR signal assignments of paecilin A and B, two new chromone derivatives from mangrove endophytic fungus Paecilomyces sp. (tree 1-7)
    Zhiyong Guo
    School of Chemistry and Chemical Engineering, SunYat Sen Zhongshan University, Guangzhou 510275, PR China
    Magn Reson Chem 45:777-80. 2007
    ..In our cytotoxicity assays, secalonic D (3) showed cytotoxicity toward KB cells with IC(50) < 1 microg ml(-1) and inhibiting human topoisomerase I with IC(50) at 0.16 micromol ml(-1). 1, 2, and 4 showed no activity to KB cells...
  57. ncbi Cytotoxic activity of the third-generation bisphosphonate zoledronic acid in acute myeloid leukemia
    Michael Fiegl
    Department of Internal Medicine III, University Hospital Grosshadern, Ludwig Maximilians University, Marchioninistr 15, 81377 Munich, Germany
    Leuk Res 31:531-9. 2007
    ..Both agents, however, exerted an additive cytotoxicity as revealed by isobologram-analysis and combination index. These data warrant further investigation of ZOL in the treatment of AML...
  58. pmc Gene expression patterns within cell lines are predictive of chemosensitivity
    Brian Z Ring
    Applied Genomics Inc, Burlingame, CA, 94010, USA
    BMC Genomics 9:74. 2008
    ..A strong correlation between the pattern of expression of a biomarker and sensitivity to a compound could suggest a clinically interesting biological relationship between the two...
  59. ncbi In vitro drug sensitivity predicts response and survival after individualized sensitivity-directed chemotherapy in metastatic melanoma: a multicenter phase II trial of the Dermatologic Cooperative Oncology Group
    Selma Ugurel
    Skin Cancer Unit, German Cancer Research Center Heidelberg and Department of Dermatology, University Hospital of Mannheim, Mannheim, Germany
    Clin Cancer Res 12:5454-63. 2006
    ..This multicenter phase II trial was aimed to investigate the efficacy of a sensitivity-directed, first-line chemotherapy in metastasized melanoma patients, and to prove an association between in vitro sensitivity and therapy outcome...
  60. ncbi Kahalalide derivatives from the Indian sacoglossan mollusk Elysia grandifolia
    Mohamed Ashour
    Institut fur Pharmazeutische Biologie und Biotechnologie, Heinrich Heine Universitat Dusseldorf, Universitatsstrasse 1, Geb 26 23, 40225 Dusseldorf, Germany
    J Nat Prod 69:1547-53. 2006
    ..The new derivative kahalalide R was found to exert comparable or even higher cytotoxicity than the potential drug candidate kahalalide F toward the MCF7 human mammary carcinoma cell line...
  61. ncbi Ex vivo assessment of chemotherapy-induced apoptosis and associated molecular changes in patient tumor samples
    Farzaneh Pirnia
    Institute of Medical Oncology, University of Bern, Inselspital, Bern, Switzerland
    Anticancer Res 26:1765-72. 2006
    ..One of the few possible approaches is serial biopsies in patients. However, this type of research is severely limited by methodological and ethical constraints...
  62. ncbi Structure-activity relationships for cytotoxic ruthenium(II) arene complexes containing N,N-, N,O-, and O,O-chelating ligands
    Abraha Habtemariam
    School of Chemistry, University of Edinburgh, West Mains Road, Edinburgh EH9 3JJ, UK, and University of Edinburgh Centre for Cancer Research, Western General Hospital, Crewe Road South, Edinburgh EH4 2XR, UK
    J Med Chem 49:6858-68. 2006
    ..Complexes were not cross-resistant with cisplatin, and cross-resistance to Adriamycin was circumvented by replacing XY=en with 1,2-phenylenediamine. Some complexes were also active against colon, pancreatic, and lung cancer cells...
  63. ncbi In vitro chemosensitivity test to predict chemosensitivity for paclitaxel, using human gastric carcinoma tissues
    Yasuhiro Kodera
    Department of Surgery II, Nagoya University Graduate School of Medicine, 65 Tsurumai Cho, Showa Ku, Nagoya 466 8550, Japan
    Int J Clin Oncol 11:449-53. 2006
    ..Therapy guided by chemotherapy sensitivity and resistance assays may lead to rational treatment decisions. Paclitaxel, one of several new drugs for gastric carcinoma, has not been extensively evaluated by in vitro chemosensitivity tests...
  64. ncbi Determination of the mechanism of gemcitabine modulation of cisplatin drug resistance in panel of human endometrial cancer cell lines
    Judith A Smith
    Division of Pharmacy, The University of Texas MD Anderson Cancer Center, Houston, TX 77230 1439, USA
    Gynecol Oncol 103:518-22. 2006
    ..To evaluate the mechanism that gemcitabine modulates cisplatin drug resistance in endometrial cancer cell lines...
  65. ncbi Chemistry of renieramycins. Part 8: synthesis and cytotoxicity evaluation of renieramycin M-jorunnamycin A analogues
    Kornvika Charupant
    Department of Pharmacognosy and Pharmaceutical Botany, Center for Bioactive Natural Products from Marine Organisms and Endophytic Fungi BNPME, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Pathumwan, Bangkok, Thailand
    Bioorg Med Chem 17:4548-58. 2009
    ..2'-Pyridinecarboxylic acid ester derivative (9c) exhibited a threefold increase in cytotoxicity relative to 1m...
  66. pmc MS-1020 is a novel small molecule that selectively inhibits JAK3 activity
    Byung Hak Kim
    Pediatrics Hematology Oncology, New York Medical College, Valhalla, NY, USA
    Br J Haematol 148:132-43. 2010
    ..These results suggest that MS-1020 may have therapeutic potential in the treatment of cancers harbouring aberrant JAK3 signalling...
  67. ncbi RhoA silencing reverts the resistance to doxorubicin in human colon cancer cells
    Sophie Doublier
    Department of Genetics, Biology and Biochemistry, University of Torino, Torino, Italy
    Mol Cancer Res 6:1607-20. 2008
    ..Therefore, we suggest that inactivating RhoA has potential clinical applications and might in the future become part of a gene therapy protocol...
  68. ncbi Cytotoxic bromotyrosine derivatives from a two-sponge association of Jaspis sp. and Poecillastra sp
    Pramod B Shinde
    College of Pharmacy, Pusan National University, Geumjung ku, Busan 609 735, Republic of Korea
    Bioorg Med Chem Lett 18:6414-8. 2008
    ..Compounds 1-4, 6, 10, and 12 were evaluated for cytotoxicity against a small panel of five human solid tumor cell lines and their activity was compared in relevance to their structure...
  69. ncbi American Society of Clinical Oncology Technology Assessment: chemotherapy sensitivity and resistance assays
    Deborah Schrag
    American Society of Clinical Oncology, Cancer Policy and Clinical Affairs, Alexandria, VA 22314, USA
    J Clin Oncol 22:3631-8. 2004
    ..To develop a technology assessment of chemotherapy sensitivity and resistance assays in order to define the role of these tests in routine oncology practice...
  70. ncbi Menadione reduction by pharmacological doses of ascorbate induces an oxidative stress that kills breast cancer cells
    Raphael Beck
    Universite Catholique de Louvain, Louvain Drug Research Institute, Toxicology and Cancer Biology Research Group, PMNT Unit, Belgium
    Int J Toxicol 28:33-42. 2009
    ..Since ascorbate is taken up by cancer cells and, due to their antioxidant enzyme deficiency, oxidative stress should affect cancer cells to a greater extent than normal cells. This differential sensitivity may have clinical applications...
  71. pmc Detailed NMR, including 1,1-ADEQUATE, and anticancer studies of compounds from the echinoderm Colobometra perspinosa
    Anthony D Wright
    Australian Institute of Marine Science, PMB No 3, Townsville MC, Townsville 4810, Australia
    Mar Drugs 7:565-75. 2009
    ..The NMR data for 4 and 5 are reported here for the first time, as is their occurrence from the marine environment. The in vitro anticancer activity of the original extract was found to be associated with 1, 3 and 5...
  72. ncbi Cytotoxic activity and cellular processing in human ovarian carcinoma cell lines of a new platinum(II) compound containing a fluorescent substituted propylene diamine ligand
    Patricia Marqués-Gallego
    Leiden Institute of Chemistry, Gorlaeus Laboratories, Leiden University, PO Box 9502, 2300 RA Leiden, The Netherlands
    Biochem Pharmacol 78:365-73. 2009
    ..Additionally, the reaction of cis-[Pt(bapda)Cl2] with 9-ethylguanine appears to be very slow, as studied by 1H and 195Pt NMR spectroscopy...
  73. ncbi Antitumoral and antiangiogenic efficacy of bisphosphonates in vitro and in a murine RENCA model
    Jens Soltau
    Cancer Hospital Sanafontis, Freiburg, Federal Republic of Germany
    Anticancer Res 28:933-41. 2008
    ..In this study the antiangiogenic potency of zoledronic acid and clodronate were evaluated...
  74. ncbi Bcl-2 overexpression enhances in vitro sensitivity against docetaxel in non-small cell lung cancer
    Yoshimasa Inoue
    Department of Surgery, Teikyo University School of Medicine, 2 11 1, Kaga, Itabashi ku, Tokyo, 173 8605, Japan
    Oncol Rep 13:259-64. 2005
    ..On the other hand, positive P-gp expression may be an indicator of enhanced in vitro resistance to CDDP in pulmonary adenocarcinomas...
  75. ncbi Apoptosis and tumor remission in liver tumor xenografts by 4-phenylbutyrate
    Irina Svechnikova
    Department of Clinical Neuroscience, Experimental Alcohol and Drug Addiction Research Section, Karolinska Hospital, CMM, L8 01, S 171 76 Stockholm, Sweden
    Int J Oncol 22:579-88. 2003
    ..Reduction in expression of alpha-fetoprotein was found both in Hep3B cells and xenografts, suggesting also a differentiation effect by PB...
  76. pmc Inhibiting JNK dephosphorylation and induction of apoptosis by novel anticancer agent NSC-741909 in cancer cells
    Xiaoli Wei
    Department of Thoracic and Cardiovascular Surgery, University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    J Biol Chem 284:16948-55. 2009
    ..Thus, NSC-741909-mediated inhibition of JNK dephosphorylation results in sustained JNK activation, which leads to apoptosis in cancer cells...
  77. pmc Enhanced antitumor activity of combinations of free and HPMA copolymer-bound drugs
    J Hongrapipat
    Department of Pharmaceutics and Pharmaceutical Chemistry, University of Utah, Salt Lake City, UT 84112, USA
    Int J Pharm 351:259-70. 2008
    ..95, respectively. However, all other combinations were synergistic up to fa<0.9 and were additive at higher fa values. The observations that most combinations produced synergistic effects will be important for clinical translation...
  78. ncbi Antineoplastic agents. 499. Synthesis of hystatin 2 and related 1H-benzo[de][1,6]-naphthyridinium salts from aaptamine
    George R Pettit
    Cancer Research Institute and Department of Chemistry and Biochemistry, Arizona State University, Box 872404, Tempe, Arizona 85287 2404, USA
    J Med Chem 47:1775-82. 2004
    ..Naphthyridinium chloride 8a was selected for further development, and results of an initial cell cycle analysis and a cDNA microarray study showed effects consistent with inhibition of the S-phase of cell growth...
  79. pmc Phellinus linteus sensitises apoptosis induced by doxorubicin in prostate cancer
    L Collins
    Department of Pathology, K522, Boston University School of Medicine, 80 East Concord Street, Boston, MA 02118, USA
    Br J Cancer 95:282-8. 2006
    ..Our study also suggests that PL has therapeutic potential to augment the magnitude of apoptosis induced by antiprostate cancer drugs...
  80. ncbi Use of isogenic human cancer cells for high-throughput screening and drug discovery
    C J Torrance
    The Howard Hughes Medical Institute, 1650 Orleans Street, Baltimore, MD 21231, USA
    Nat Biotechnol 19:940-5. 2001
    ..The present data demonstrate a broadly applicable approach for mining therapeutic agents targeted to the specific genetic alterations responsible for cancer development...
  81. ncbi Interference by anti-cancer chemotherapeutic agents in the MTT-tumor chemosensitivity assay
    Engin Ulukaya
    University of Uludag, School of Medicine, Department of Biochemistry, Bursa, Turkey
    Chemotherapy 50:43-50. 2004
    ..The MTT assay is one of the methods used to predict the drug response in malignancies. However, it may suffer from interference by the anticancer drugs with the MTT assay...
  82. ncbi A novel combretastatin A-4 derivative, AC-7700, shows marked antitumor activity against advanced solid tumors and orthotopically transplanted tumors
    Y Nihei
    Pharmaceutical Research Laboratories, Ajinomoto Co, Inc, Kawasaki
    Jpn J Cancer Res 90:1016-25. 1999
    ..These results suggest that AC-7700 is a novel antivascular agent that may have potent activity against advanced-stage cancer in the clinical setting...
  83. ncbi A bioactive secosterol with an unusual A- and B-ring oxygenation pattern isolated from an Indonesian soft coral Lobophytum sp
    L A Morris
    Department of Chemistry, University of Aberdeen, Scotland, U K
    J Nat Prod 61:538-41. 1998
    ..The structures of 1 was solved by 2D NMR methods and by chemical shift analogy to the known secogorgosterol 2. Compound 1 was found to have activity against human ovarian tumor and human leukemia cell lines...
  84. ncbi Ex vivo programmed cell death and the prediction of response to chemotherapy
    Robert A Nagourney
    Rational Therapeutics, 750 East 29th Street, Long Beach, CA 90806, USA
    Curr Treat Options Oncol 7:103-10. 2006
    ..This article briefly reviews the history of whole-cell experimental models of in vitro chemosensitivity testing then focuses on cell-death measures as the most robust predictors of clinical outcome in human cancer...
  85. ncbi Effect of culture conditions on the chemosensitivity of ovarian cancer cell lines
    Augusta Fernando
    Translational Oncology Research Centre, Queen Alexandra Hospital, Portsmouth, UK
    Anticancer Drugs 17:913-9. 2006
    ..Such a panel could be used to screen and develop anticancer drugs...
  86. ncbi Chemosensitivity and resistance assays: a systematic review?
    Robert Nagourney
    J Clin Oncol 23:3640-1; author reply 3646-8. 2005
  87. ncbi Erlotinib hydrochloride
    Jonathan Dowell
    Nat Rev Drug Discov 4:13-4. 2005
  88. ncbi Doxorubicin-PAMAM dendrimer complex attached to liposomes: cytotoxic studies against human cancer cell lines
    Aristarchos Papagiannaros
    Department of Pharmaceutical Technology, School of Pharmacy, National and Kapodistrian University of Athens, Panepistimiopolis, 15771 Zografou Athens, Greece
    Int J Pharm 302:29-38. 2005
    ..Liposomal formulations composed of lipids and of a drug-dendrimer complex could be characterized as modulatory liposomal controlled release system (MLCRS), and could provide benefits to the delivery of drugs and modulate their release...
  89. ncbi Chemotherapy sensitivity and resistance assays: a systematic review
    David J Samson
    Blue Cross and Blue Shield Association Technology Evaluation Center, Washington, DC 20005, USA
    J Clin Oncol 22:3618-30. 2004
    ..This systematic review evaluates evidence comparing therapy guided by chemotherapy sensitivity and resistance assays with empiric chemotherapy, emphasizing survival outcomes...
  90. ncbi Progress in the development and acquisition of anticancer agents from marine sources
    M L Amador
    The Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, Baltimore, MD 21231, USA
    Ann Oncol 14:1607-15. 2003
  91. ncbi Didmolamide A and B, two new cyclic hexapeptides from the marine ascidian Didemnum molle
    Amira Rudi
    School of Chemistry, Tel Aviv University, Ramat Aviv 69978, Israel
    J Nat Prod 66:575-7. 2003
    ..The structure of the two peptides was elucidated by interpretation of MS, COSY, HMQC, and HMBC data. The absolute configuration of all amino acids was determined to be l using Marfey's method for HPLC...
  92. ncbi Heterogeneity of chemosensitivity of metastatic cutaneous melanoma
    I A Cree
    Department of Pathology, Institute of Ophthalmology, University College London, UK
    Anticancer Drugs 10:437-44. 1999
    ..This provides the rationale for future randomized controlled trials of ATP-TCA-directed chemotherapy versus physician's choice to determine whether assay-directed chemotherapy can improve patient response and survival...
  93. ncbi Antitumor Agents. 211. Fluorinated 2-phenyl-4-quinolone derivatives as antimitotic antitumor agents
    Y Xia
    Division of Medicinal Chemistry and Natural Products, School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599-7360, USA
    J Med Chem 44:3932-6. 2001
    ..46 microM) and of radiolabeled colchicine binding to tubulin, with activities comparable to those of the potent antimitotic natural products colchicine, podophyllotoxin, and combretastatin A-4...
  94. ncbi Chemistry of renieramycins. Part 5. Structure elucidation of renieramycin-type derivatives O, Q, R, and S from thai marine sponge Xestospongia species pretreated with potassium cyanide
    Surattana Amnuoypol
    Bioactive Marine Natural Products Chemistry Research Unit BMNCU, Department of Pharmacognosy, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Pathumwan, Bangkok 10330, Thailand
    J Nat Prod 67:1023-8. 2004
    ..Their structures were elucidated by comparison of spectral data with those of recently reported renieramycins M (1m) and N (1n). The results of transformation and cytotoxicity measurements are also described...
  95. ncbi Array-based structure and gene expression relationship study of antitumor sulfonamides including N-[2-[(4-hydroxyphenyl)amino]-3-pyridinyl]-4-methoxybenzenesulfonamide and N-(3-chloro-7-indolyl)-1,4-benzenedisulfonamide
    Takashi Owa
    Eisai Co, Ltd, 5 1 3 Tokodai, Tsukuba, Ibaraki 300 2635, Japan
    J Med Chem 45:4913-22. 2002
    ..These results provide an example of the utility of structure and gene expression relationship studies in medicinal genomics...
  96. ncbi Gold dithiocarbamate derivatives as potential antineoplastic agents: design, spectroscopic properties, and in vitro antitumor activity
    Luca Ronconi
    Department of Chemical Sciences, University of Padua, Via Marzolo 1, 35131 Padua, Italy
    Inorg Chem 44:1867-81. 2005
    ....
  97. ncbi Development of cobalt(3,4-diarylsalen) complexes as tumor therapeutics
    Ronald Gust
    Institute of Pharmacy, Free University of Berlin, Konigin Luise Strasse 2 4, D 14195 Berlin, Germany
    J Med Chem 47:5837-46. 2004
    ..Therefore, a mode of action based on a cobalt-catalyzed oxidative damage of the DNA is not very likely...
  98. ncbi Haterumaimides F-I, four new cytotoxic diterpene alkaloids from an ascidian Lissoclinum species
    M J Uddin
    Department of Chemistry, Biology and Marine Science, University of the Ryukyus, Nishihara-cho, Okinawa 903-0213, Japan
    J Nat Prod 64:1169-73. 2001
    ..Haterumaimides F-I (1-4) inhibited the first cleavage of fertilized sea urchin eggs and exhibited potent to weak cytotoxicities against P388 cells...
  99. ncbi Taurolidine: cytotoxic and mechanistic evaluation of a novel antineoplastic agent
    P Calabresi
    Department of Medicine, Division of Clinical Pharmacology, Brown University and Rhode Island Hospital, Providence, Rhode Island 02903, USA
    Cancer Res 61:6816-21. 2001
    ..Administration of this regimen to nude mice bearing i.p. human ovarian tumor xenografts significantly inhibited both tumor formation and growth. These findings are discussed in light of their clinical implications...
  100. ncbi Synthesis and antitumor activity of some curcumin analogs
    Khairia M Youssef
    Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia
    Arch Pharm (Weinheim) 338:181-9. 2005
    ..This may be attributed to an increased positive inductive effect and/or increased lipophilicity of the new compounds, a fact which is proven by the superior activities of compounds 17 and 18...
  101. pmc Selective cancer cell killing by alpha-tocopheryl succinate
    J Neuzil
    Institute for Prevention of Cardiovascular Diseases, Ludwig Maximilians University, Pettenkoferstrasse 9, Munich, 80336, Germany
    Br J Cancer 84:87-9. 2001
    ..e. primary and non-transformed cells. These findings strongly suggest a potential of this micronutrient in the therapy and/or prevention of cancer without significant side-effects...

Research Grants72

  1. Novel Single, Dual and Multitargeted Inhibitors of RTKs
    Aleem Gangjee; Fiscal Year: 2007
    ..abstract_text> ..
  2. Molecular Target Focused Discovery of Anticancer Drugs
    George R Pettit; Fiscal Year: 2010
    ....
  3. Molecular Target Focused Discovery of Anticancer Drugs
    GEORGE PETTIT; Fiscal Year: 2007
    ..In summary, the proposed research will be sharply aimed at the discovery and very rapid development of new anticancer drugs for the NCI programs direct at improving human cancer treatments. ..
  4. Novel, P. jirovecii Specific Antipneumocystis Agents
    Aleem Gangjee; Fiscal Year: 2009
    ..These agents could be used alone or in combination to treat PCP thus providing novel agents against a new target. ..
  5. Third Generation Antiopportunistic Agents
    Aleem Gangjee; Fiscal Year: 2003
    ..Screening against tuberculosis (NIAID) and tumor cells in culture (NCI) is also proposed. ..
  6. Single Agents with Designed Combination Chemotherapy Potential
    Aleem Gangjee; Fiscal Year: 2010
    ..abstract_text> ..
  7. NOVEL NONINDUCIBLE THYMIDYLATE SYNTHASE INHIBITORS
    Aleem Gangjee; Fiscal Year: 2004
    ....
  8. STRUCTURE BASED ANALOGS AS ANTIOPPORTUNISTIC AGENTS
    Aleem Gangjee; Fiscal Year: 2001
    ..The analogues synthesized will also be submitted for screening against tuberculosis (NIAID) parasitic diseases (WHO) and tumor cells in culture (NCI). ..
  9. Alpha Folate Receptor Mediated GARFTase Inhibitors as Selective Antitumor Agents
    Aleem Gangjee; Fiscal Year: 2010
    ....
  10. Antitumor Antimitotics That Reverse Tumor Resistance
    Aleem Gangjee; Fiscal Year: 2010
    ..The study will also further define the mechanism of action of the novel series and could afford agents for clinical use. ..
  11. DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORS
    Arun K Ghosh; Fiscal Year: 2010
    ..This research integrates organic synthesis, protein-ligand x-ray crystallography, molecular modeling and in-depth virus and cell-biological studies to design the next generation of HIV-1 protease inhibitors. ..
  12. PRE-CLINICAL COMBINATION CHEMO- AND RADIOANTIBODY THERAP
    Rhona Stein; Fiscal Year: 2005
    ..2) Therapy-induced changes in marker expression post therapy can be identified clinically in small samples of circulating tumor cells. ..
  13. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2005
    ..abstract_text> ..
  14. Doxorubicin-Immunoconjugate Therapy of Non-Hodgkin's Lymphoma
    Rhona Stein; Fiscal Year: 2008
    ..abstract_text> ..
  15. SYNTHETIC STUDIES RELATED TO CANCER RESEARCH/TREATMENT
    Paul Wender; Fiscal Year: 2005
    ..Overall, this research program is expected to be of significant value in chemistry, biology, and medicine. ..
  16. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2008
    ..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
  17. Anti-Angiogenesis/Drugs in Tumors--Bench /Bedside & Back
    Rakesh Jain; Fiscal Year: 2005
    ..Attendance at this conference will provide an excellent opportunity for young investigators working on cancer to educate and familiarize themselves with the field of angiogenesis and the complexities of the system. ..
  18. NMR systems : 2 Bruker Avance 500 Consoles
    AMOS SMITH; Fiscal Year: 2006
    ..The areas of public health research include, among others, cancer, infectious diseases, neurodegenerative diseases such as Alzheimer's disease, and heart and cardiovascular disease. [unreadable] [unreadable] [unreadable]..
  19. SYNTHESIS OF SPONGISTATIN ANTITUMOR AGENTS
    AMOS SMITH; Fiscal Year: 2007
    ..abstract_text> ..
  20. Rexinoid Synergy in Prostate Cancer Apoptosis
    Marcia Dawson; Fiscal Year: 2009
    ..We anticipate that our results will provide a more effective and less systemically toxic means of enhancing the efficacy of chemotherapeutic agents currently used to treat prostate cancer. ..
  21. Design and Synthesis of HIV-1 Protease Inhibitors
    AMOS SMITH; Fiscal Year: 2004
    ....
  22. SYNTHESIS OF CHLOROPEPTINS, GP120 CD4 BINDING INHIBITORS
    AMOS SMITH; Fiscal Year: 2001
    ..abstract_text> ..
  23. Conference on Angiogenesis in Cancer and Other Diseases
    Rakesh Jain; Fiscal Year: 2002
    ..The meeting's synthesis of available information will be particularly thought-provoking for students and post- doctoral fellows. ..
  24. Role of BMDCs in Solid Tumor Growth and Relapse
    Rakesh K Jain; Fiscal Year: 2010
    ..Furthermore, our results will offer strategies for the inhibition of tumor relapse after radiotherapy by targeting molecular pathways that are critical for both angiogenesis and myeloid BMDC recruitment. ..
  25. SYNTHESIS OF ANTICANCER AGENTS
    K C Nicolaou; Fiscal Year: 2010
    ..abstract_text> ..
  26. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2004
    ..The proposed work is expected to have significant impact in the area of cancer chemotherapy and should provide enabling technologies and tools for biology and medicine. ..
  27. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2002
    ..3] sigmatropic rearrangement and a radical based ring closure to form the bicyclic skeleton. ..
  28. Integrative Biology of Tumor Metastasis
    Rakesh Jain; Fiscal Year: 2009
    ..Finally, we have the resources and the clinical collaborators in place to initiate a clinical trial based on our findings, as attested by our ongoing trial using a VEGF-specific antibody. ..
  29. DEVELOPMENT OF LIGAND ASSISTED ASYMMETRIC SYNTHESES
    Arun Ghosh; Fiscal Year: 2001
    ..Besides the broad range of scope and generality, this line of research will provide excellent opportunities to teach and train graduate and undergraduate students in the laboratory. ..
  30. Inhibition of Alzheimer's Beta-Amyloid Fibril Formation
    Duy Hua; Fiscal Year: 2009
    ..However, soluble oligomeric Abeta showed high neuronal toxicity. Inhibition of the formation of these toxic soluble Abeta oligomers would provide therapeutics for AD. ..
  31. ACYLTRANSFERASE INHIBITORS AS ANTI RAS AGENTS
    Charles Smith; Fiscal Year: 2009
    ..abstract_text> ..
  32. The Role of Urokinase Receptor in Prostate Cancer Progression
    Inder Sehgal; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  33. Roles of Nkx3.1 in prostate development and cancer
    Cory Abate Shen; Fiscal Year: 2007
    ..1 protein expression. These mice will provide a valuable model for exploring the reversibility of prostate carcinogenesis in vivo. ..
  34. Bevacizumab and radiation therapy for sarcomas
    Sam Yoon; Fiscal Year: 2007
    ..This study explores a novel combination of the anti-angiogenic agent bevacizumab and radiation therapy for the treatment of STS. [unreadable] [unreadable] [unreadable]..
  35. Chemoprevention of Prostate Cancer by Curcumin
    Sharmila Shankar; Fiscal Year: 2008
    ..We expect the proposed studies to yield data in support of our hypothesis and to serve as a critical step in developing new approaches to prostate cancer prevention. [unreadable] [unreadable] [unreadable]..
  36. Dual-color tumor-host imaging models
    Meng Yang; Fiscal Year: 2007
    ..These models have significant commercial potential for discovery and development of stroma-targeted and anti-angiogenesis drugs. [unreadable] [unreadable] [unreadable]..
  37. Analysis of Apigenin in Inhibiting Ovarian Tumorigenesis
    Bing Hua Jiang; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  38. A novel sulindac derivative for colon cancer chemoprevention
    Gary Piazza; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  39. Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.
    BARRY TROST; Fiscal Year: 2009
    ..These new synthetic methods apply to many structural types beyond those illustrated and constitutes a significant to gain access to complex molecular targets more easily. ..
  40. Roles for MSX1 in vertebrate embryogenesis
    Cory Abate Shen; Fiscal Year: 2007
    ..Taken together, our focused analyses of Msx homeoproteins will provide general paradigms for addressing the functional specificities of other homeoproteins in vivo. ..
  41. Chemoprevention of Esophageal Squamous Cell Carcinoma
    Gary Stoner; Fiscal Year: 2004
    ..abstract_text> ..
  42. DRUG DISCOVERY CORE FACILITY
    Charles Smith; Fiscal Year: 2005
    ..Establishment of this DDCF will provide an important bridge between basic and applied research, and so will enhance the research environment and advance cancer research. ..
  43. Cell-based Assay on Microtransponders
    Wlodek Mandecki; Fiscal Year: 2004
    ..The benefits of the program involve the advancement of cell-based assay technology, acceleration of drug discovery programs in research laboratories and pharmaceutical industry, and cost savings. ..
  44. Clofarabine: Cytarabine Activation for Leukemia Response
    Stefan Faderl; Fiscal Year: 2004
    ..abstract_text> ..
  45. NON-PROTEIN AMINO ACIDS AND TAXOID ANTITUMOR AGENTS
    Iwao Ojima; Fiscal Year: 2002
    ..Drug resistance in cancer chemotherapy is a serious problem. In order to solve this problem, the PI will continue his successful approach to the development of MDR reversal agents based on the strategic modification of baccatins. ..
  46. CMMI Human Subject Research Enhancement Program
    David Goldenberg; Fiscal Year: 2002
    ..3.) Provide travel expenses and educational materials for IRB members, investigators, and Regulatory Affairs Office personnel to attend meetings for educational enhancement. ..
  47. 9/10TH Conf./Cancer Therapy/Antibody/Immunoconjugates
    David Goldenberg; Fiscal Year: 2004
    ..The conference chairman, Dr. Goldenberg, has secured two outstanding scientists as co-chairmen, Drs. Ralph Reisfeld (Scripps) and Edward Sausville (NCI). ..
  48. Farnesyltransferase Inhibitor Therapy for Myelodysplasia
    Razelle Kurzrock; Fiscal Year: 2002
    ....
  49. Nucleolin--A Novel Target for Cancer Drug Discovery
    Paula Bates; Fiscal Year: 2002
    ....
  50. Conference on Photodynamic Therapy
    David Kessel; Fiscal Year: 2002
    ..The most recent PDT meeting, sponsored by the International Photodynamic Assn, has more than 600 participants. ..
  51. New Ligands for Radioimmunotherapy and MRI of Cancer
    Hyun Soon Chong; Fiscal Year: 2006
    ..The results of the proposed research will contribute to the development of better drugs for both MRI and RIT, which will greatly enhance clinical exploration of both modalities, and directly benefit cancer patients. ..
  52. SYNTHESIS OF ANNONACEOUS ACETOGENINS AND ANALOGUES
    James Marshall; Fiscal Year: 2001
    ..The synthetic approach will employ chiral allylic and allenic organometal reagents to introduce stereogenic centers with concurrent formation of carbon-carbon bonds. ..
  53. Biological Evaluation of CCI-779 in Brain Tumors
    Manuel Hidalgo; Fiscal Year: 2003
    ....
  54. ISOLATION OF THE NEUROBLASTOMA PREDISPOSITION GENE
    John Maris; Fiscal Year: 2006
    ..Ultimately, these experiments should lead to the identification of a common pathway to neuroblastoma tumorigenesis that will be an outstanding target for rationally designed therapeutics. ..
  55. Fluidic Sorter for Microtransponders
    Wlodek Mandecki; Fiscal Year: 2005
    ..An automatic sorter would enable combinatorial chemistry on microtransponders, accelerating drug discovery. The sorter, in a parallel application, will also reduce the cost of microtransponder kits for DNA and protein multiplex assay. ..
  56. Pharmacodynamic-guided Dose-finding Study of Rapamycin
    Manuel Hidalgo; Fiscal Year: 2005
    ..Overall this study will determine the biologically active dose of rapamycin in cancer patients that can then be explored in disease-oriented studies. ..
  57. Biosynthesis of Hypotensive Phosphonopeptide Natural Products
    Brian O Bachmann; Fiscal Year: 2010
    ..Metalloproteinase inhibitors have potential to treat a large number of human illnesses including hypertension, cancer and osteoarthritis, among others. ..
  58. RHOMOCYCSTEINASE FOR HOMOCYSTEINE ASSAY
    Yuying Tan; Fiscal Year: 2002
    ..The tHCY enzymatic kits for these applications will be ready for commercial launch at this point. PROPOSED COMMERCIAL APPLICATION: Not Available ..
  59. UNIQUE TISSUE AND TUMOR PROCESSING FACILITY
    Adi Gazdar; Fiscal Year: 2003
    ..A charge back fee system will recover some of the costs and will be used for future expansion of the Facility, which is anticipated to become self sustaining after five years. ..
  60. Inhibitors of 5alpha-reductase for acne therapy
    Lingna Li; Fiscal Year: 2002
    ..PROPOSED COMMERCIAL APPLICATIONS: Liposomal 4-MA will be developed as a topical selectively targeted therapeutic for acne for which they should be a very market. ..
  61. Therapeutic hair follicle-derived neurospheres
    Meng Yang; Fiscal Year: 2007
    ..Human hair- follicle bulge cells will be further characterized and developed for therapeutic potential for nerve regeneration in Phase III. [unreadable]..
  62. Discovery of novel fluorescent reporter genes
    Ming Zhao; Fiscal Year: 2004
    ..Reporters with spectral properties that can be used for whole-body imaging of tumors in the lung and their metastases will be candidates for further development for numerous applications of multi-color imaging. ..
  63. Targeted tumoricidal bacteria
    Ming Zhao; Fiscal Year: 2007
    ..Future human trials of the tumor-killing bacteria can be held after the Phase I and Phase II grant periods are completed. [unreadable] [unreadable] [unreadable]..
  64. Imageable tumor-targeting bacteria
    Ming Zhao; Fiscal Year: 2006
    ..unreadable] [unreadable] [unreadable]..
  65. Adenoviral GFP targeting of metastatic human tumors using multiple delivery route
    Hiroyuki Kishimoto; Fiscal Year: 2008
    ..Having obtained these results, we can move forward in the Phase II grant application with experiments to bring OBP-401 to the clinic for use in cancer surgery in human patients. [unreadable] [unreadable] [unreadable]..
  66. Orthotopic models of tumor angiogenesis and blood flow
    Meng Yang; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  67. Enzyme therapy for hyperhomocysteinemia
    Yuying Tan; Fiscal Year: 2005
    ..Phase II results will lead to an IND for MEGC-PEG-rMETase for end stage renal disease patients and other patients with intractable hyperhomocysteinemia and high cardiovascular disease mortality. ..
  68. Tumor suppressor adenomatous polyposis coli and breast carcinogenesis
    Satya Narayan; Fiscal Year: 2007
    ....
  69. INTERACTION OF APC AND P53 IN COLORECTAL CARCINOGENESIS
    Satya Narayan; Fiscal Year: 2001
    ..Therefore, novel therapeutic strategies may emerge with respect to potential new targets for chemotherapeutic intervention in colon cancer. ..
  70. TRIPTYCENE ANALOGS--NOVEL BIFUNCTIONAL ANTICANCER DRUGS
    Jean Pierre Perchellet; Fiscal Year: 2004
    ..abstract_text> ..
  71. Prediction and assessment of response to targated therapy in pancreatic cancer
    Soner Altiok; Fiscal Year: 2007
    ..We expect that this study will result in validation of the novel PD approaches and will also inform further assessment and refinement in future hypothesis testing studies. [unreadable] [unreadable] [unreadable]..