pyrimidines

Summary

Summary: A family of 6-membered heterocyclic compounds occurring in nature in a wide variety of forms. They include several nucleic acid constituents (CYTOSINE; THYMINE; and URACIL) and form the basic structure of the barbiturates.

Top Publications

  1. ncbi Rosuvastatin to prevent vascular events in men and women with elevated C-reactive protein
    Paul M Ridker
    Center for Cardiovascular Disease Prevention, Brigham and Women s Hospital, Harvard Medical School, Boston, MA 02215, USA
    N Engl J Med 359:2195-207. 2008
  2. ncbi Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors
    George D Demetri
    Dana-Farber Cancer Institute and Harvard Cancer Center, Boston, MA 02115, USA
    N Engl J Med 347:472-80. 2002
  3. ncbi An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer
    Teresa A Soucy
    Discovery, Millennium Pharmaceuticals, Inc, 40 Landsdowne Street, Cambridge, Massachusetts 02139, USA
    Nature 458:732-6. 2009
  4. ncbi Effect of very high-intensity statin therapy on regression of coronary atherosclerosis: the ASTEROID trial
    Steven E Nissen
    Department of Cardiovascular Medicine, Cleveland Clinic Lerner School of Medicine, Cleveland, Ohio 44195, USA
    JAMA 295:1556-65. 2006
  5. ncbi Somatic activation of KIT in distinct subtypes of melanoma
    John A Curtin
    Comprehensive Cancer Center, University of California, San Francisco, San Francisco, CA 94143-0808, USA
    J Clin Oncol 24:4340-6. 2006
  6. ncbi Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia
    Neil P Shah
    Department of Medicine, Jonsson Comprehensive Cancer Center, David Geffen School of Medicine, University of California, Los Angeles, CA 90095, USA
    Cancer Cell 2:117-25. 2002
  7. ncbi Adjuvant imatinib mesylate after resection of localised, primary gastrointestinal stromal tumour: a randomised, double-blind, placebo-controlled trial
    Ronald P Dematteo
    Memorial Sloan Kettering Cancer Center, New York, NY, USA
    Lancet 373:1097-104. 2009
  8. ncbi Primitive, quiescent, Philadelphia-positive stem cells from patients with chronic myeloid leukemia are insensitive to STI571 in vitro
    Susan M Graham
    Department of Medicine, Royal Infirmary, Glasgow, Scotland
    Blood 99:319-25. 2002
  9. ncbi Phase III randomized, intergroup trial assessing imatinib mesylate at two dose levels in patients with unresectable or metastatic gastrointestinal stromal tumors expressing the kit receptor tyrosine kinase: S0033
    Charles D Blanke
    Oregon Health and Science University Cancer Institute, 3181 SW Sam Jackson Park Rd, L 586, Portland, OR 97239, USA
    J Clin Oncol 26:626-32. 2008
  10. ncbi Long-term results from a randomized phase II trial of standard- versus higher-dose imatinib mesylate for patients with unresectable or metastatic gastrointestinal stromal tumors expressing KIT
    Charles D Blanke
    Oregon Health and Science University Cancer Center and Portland Veterans Affairs Hospital, Portland, OR, USA
    J Clin Oncol 26:620-5. 2008

Research Grants

  1. LIPOPHILIC ANTIFOLATES AND AIDS OPPORTUNISTIC INFECTIONS
    Andre Rosowsky; Fiscal Year: 2000
  2. LIPOPHILIC ANTIFOLATES AND AIDS OPPORTUNISTIC INFECTIONS
    Andre Rosowsky; Fiscal Year: 2004
  3. SELENIUM AND LUNG CANCER RISK
    Henry Thompson; Fiscal Year: 2003
  4. Structural Biology of Purine and Pyrimidine Biosynthesis and Metabolism
    Steven E Ealick; Fiscal Year: 2010
  5. Structural Biology of Purine and Pyrimidine Biosynthesis and Metabolism
    Steven Ealick; Fiscal Year: 2009
  6. SELENIUM AND LUNG CANCER RISK
    Henry Thompson; Fiscal Year: 2002
  7. Hybridization of Oligonucleotide Probes with Duplex DNA
    Maxim Frank Kamenetskii; Fiscal Year: 2005
  8. SIMULATION OF PROTON AND HYDRIDE TRANSFER IN ENZYMES
    Sharon Hammes Schiffer; Fiscal Year: 2010
  9. FUNCTION OF THE S CEREVISIAE PHRI GENE AND PHOTOLYASE
    GWENDOLYN SANCAR; Fiscal Year: 1992
  10. STRUCTURE AND REGULATION OF E. COLI DNA PHOTOLYASE
    Aziz Sancar; Fiscal Year: 1990

Detail Information

Publications296 found, 100 shown here

  1. ncbi Rosuvastatin to prevent vascular events in men and women with elevated C-reactive protein
    Paul M Ridker
    Center for Cardiovascular Disease Prevention, Brigham and Women s Hospital, Harvard Medical School, Boston, MA 02215, USA
    N Engl J Med 359:2195-207. 2008
    ....
  2. ncbi Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors
    George D Demetri
    Dana-Farber Cancer Institute and Harvard Cancer Center, Boston, MA 02115, USA
    N Engl J Med 347:472-80. 2002
    ..Inhibition of the KIT signal-transduction pathway is a promising treatment for advanced gastrointestinal stromal tumors, which resist conventional chemotherapy...
  3. ncbi An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer
    Teresa A Soucy
    Discovery, Millennium Pharmaceuticals, Inc, 40 Landsdowne Street, Cambridge, Massachusetts 02139, USA
    Nature 458:732-6. 2009
    ..MLN4924 suppressed the growth of human tumour xenografts in mice at compound exposures that were well tolerated. Our data suggest that NAE inhibitors may hold promise for the treatment of cancer...
  4. ncbi Effect of very high-intensity statin therapy on regression of coronary atherosclerosis: the ASTEROID trial
    Steven E Nissen
    Department of Cardiovascular Medicine, Cleveland Clinic Lerner School of Medicine, Cleveland, Ohio 44195, USA
    JAMA 295:1556-65. 2006
    ....
  5. ncbi Somatic activation of KIT in distinct subtypes of melanoma
    John A Curtin
    Comprehensive Cancer Center, University of California, San Francisco, San Francisco, CA 94143-0808, USA
    J Clin Oncol 24:4340-6. 2006
    ..Because the majority of the KIT mutations we found in melanoma also occur in imatinib-responsive cancers of other types, imatinib may offer an immediate therapeutic benefit for a significant proportion of the global melanoma burden...
  6. ncbi Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia
    Neil P Shah
    Department of Medicine, Jonsson Comprehensive Cancer Center, David Geffen School of Medicine, University of California, Los Angeles, CA 90095, USA
    Cancer Cell 2:117-25. 2002
    ..Multiple independent mutant clones were detected in a subset of relapsed cases. Our data support a clonal selection model of preexisting BCR-ABL mutations that confer imatinib resistance...
  7. ncbi Adjuvant imatinib mesylate after resection of localised, primary gastrointestinal stromal tumour: a randomised, double-blind, placebo-controlled trial
    Ronald P Dematteo
    Memorial Sloan Kettering Cancer Center, New York, NY, USA
    Lancet 373:1097-104. 2009
    ..We postulated that adjuvant treatment with imatinib would improve recurrence-free survival compared with placebo after resection of localised, primary gastrointestinal stromal tumour...
  8. ncbi Primitive, quiescent, Philadelphia-positive stem cells from patients with chronic myeloid leukemia are insensitive to STI571 in vitro
    Susan M Graham
    Department of Medicine, Royal Infirmary, Glasgow, Scotland
    Blood 99:319-25. 2002
    ..Despite dramatic short-term responses in vivo, such in vitro insensitivity to STI571, in combination with its demonstrated antiproliferative activity, could translate into disease relapse after prolonged therapy...
  9. ncbi Phase III randomized, intergroup trial assessing imatinib mesylate at two dose levels in patients with unresectable or metastatic gastrointestinal stromal tumors expressing the kit receptor tyrosine kinase: S0033
    Charles D Blanke
    Oregon Health and Science University Cancer Institute, 3181 SW Sam Jackson Park Rd, L 586, Portland, OR 97239, USA
    J Clin Oncol 26:626-32. 2008
    ....
  10. ncbi Long-term results from a randomized phase II trial of standard- versus higher-dose imatinib mesylate for patients with unresectable or metastatic gastrointestinal stromal tumors expressing KIT
    Charles D Blanke
    Oregon Health and Science University Cancer Center and Portland Veterans Affairs Hospital, Portland, OR, USA
    J Clin Oncol 26:620-5. 2008
    ..We conducted a long-term analysis of patients treated on the trial, including patients followed during an extension phase, to evaluate survival, patterns of failure, and potential prognostic factors, including tumor mutational status...
  11. ncbi Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors
    Marcus Bantscheff
    Cellzome AG, Meyerhofstrasse 1, D 69117 Heidelberg, Germany
    Nat Biotechnol 25:1035-44. 2007
    ..The data suggest that our approach is a valuable tool for drug discovery...
  12. ncbi Six-year follow-up of patients receiving imatinib for the first-line treatment of chronic myeloid leukemia
    A Hochhaus
    Universitatsmedizin Mannheim, Heidelberg University, Mannheim, Germany
    Leukemia 23:1054-61. 2009
    ..The estimated overall survival was 88% -- or 95% when only CML-related deaths were considered. This 6-year update of IRIS underscores the efficacy and safety of imatinib as first-line therapy for patients with CML...
  13. ncbi Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl
    Ellen Weisberg
    Dana-Farber Cancer Institute, Boston, Massachusetts 02115, USA
    Cancer Cell 7:129-41. 2005
    ..AMN107 is a promising new inhibitor for the therapy of CML and Ph+ ALL...
  14. ncbi Substrate-assisted inhibition of ubiquitin-like protein-activating enzymes: the NEDD8 E1 inhibitor MLN4924 forms a NEDD8-AMP mimetic in situ
    James E Brownell
    Discovery, Millennium Pharmaceuticals, Inc, 40 Landsdowne Street, Cambridge, MA 02139, USA
    Mol Cell 37:102-11. 2010
    ..These findings reveal insights into the mechanism of E1s and suggest a general strategy for selective inhibition of UBL conjugation pathways...
  15. ncbi Dasatinib versus imatinib in newly diagnosed chronic-phase chronic myeloid leukemia
    Hagop Kantarjian
    Department of Leukemia, University of Texas M D Anderson Cancer Center, 1515 Holcombe Blvd, Houston, TX 77030, USA
    N Engl J Med 362:2260-70. 2010
    ..We assessed the efficacy and safety of dasatinib, as compared with imatinib, for the first-line treatment of chronic-phase CML...
  16. ncbi Phase II proof-of-concept study of pazopanib monotherapy in treatment-naive patients with stage I/II resectable non-small-cell lung cancer
    Nasser Altorki
    Weill Medical College, Cornell University, 525 East 68th St, New York, NY 10021, USA
    J Clin Oncol 28:3131-7. 2010
    ..This proof-of-concept study examined safety and efficacy of short-term, preoperative pazopanib monotherapy in patients with operable stage I/II NSCLC...
  17. ncbi Drugging the PI3 kinome: from chemical tools to drugs in the clinic
    Paul Workman
    Cancer Research UK Centre for Cancer Therapeutics, Section of Cancer Therapeutics, The Institute of Cancer Research, Haddow Laboratories, Sutton, Surrey, United Kingdom
    Cancer Res 70:2146-57. 2010
    ..The challenges and outlook for drugging the PI3 kinome are discussed in the more general context of the role of structural biology and chemical biology in innovative drug discovery...
  18. ncbi Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors
    Jianming Zhang
    Dana Farber Cancer Institute, Harvard Medical School, Department of Cancer Biology, Seeley G Mudd Building 628, Boston, Massachusetts 02115, USA
    Nature 463:501-6. 2010
    ....
  19. ncbi A Phase II, open-label study evaluating pazopanib in patients with recurrent ovarian cancer
    Michael Friedlander
    Prince of Wales Hospital, Randwick, Sydney, Australia
    Gynecol Oncol 119:32-7. 2010
    ..This phase II, open-label study evaluated oral pazopanib monotherapy in patients with low-volume recurrent ovarian cancer...
  20. ncbi The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy
    Lee A Honigberg
    Pharmacyclics, Sunnyvale, CA 94085 4521, USA
    Proc Natl Acad Sci U S A 107:13075-80. 2010
    ..These findings support Btk inhibition as a therapeutic approach for the treatment of human diseases associated with activation of the BCR pathway...
  21. ncbi Diagnosis of gastrointestinal stromal tumors: A consensus approach
    Christopher D M Fletcher
    Department of Pathology, Brigham and Women's Hospital and Harvard Medical School, Boston MA 02115, USA
    Hum Pathol 33:459-65. 2002
    ....
  22. ncbi Identification of candidate molecular markers predicting sensitivity in solid tumors to dasatinib: rationale for patient selection
    Fei Huang
    Departments of Clinical Discovery and Oncology Discovery, Bristol Myers Squibb Co, Princeton, NJ 08543, USA
    Cancer Res 67:2226-38. 2007
    ..Our results implicate that dasatinib may represent a valuable treatment option in this difficult-to-treat population. To test this hypothesis, clinical studies are now under way to determine the activity of dasatinib in these patients...
  23. ncbi Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia
    B J Druker
    Division of Hematology and Medical Oncology, Oregon Health Sciences University, Portland 97201, USA
    N Engl J Med 344:1031-7. 2001
    ..Since tyrosine kinase activity is essential to the transforming function of BCR-ABL, an inhibitor of the kinase could be an effective treatment for CML...
  24. ncbi Nilotinib versus imatinib for newly diagnosed chronic myeloid leukemia
    Giuseppe Saglio
    University of Turin, San Luigi Gonzaga Hospital, Orbassano, Turin, Italy
    N Engl J Med 362:2251-9. 2010
    ..We evaluated the efficacy and safety of nilotinib, as compared with imatinib, in patients with newly diagnosed Philadelphia chromosome-positive chronic myeloid leukemia (CML) in the chronic phase...
  25. ncbi Reversal of experimental pulmonary hypertension by PDGF inhibition
    Ralph Theo Schermuly
    Department of Internal Medicine, Justus Liebig University Giessen, Giessen, Germany
    J Clin Invest 115:2811-21. 2005
    ..This regimen offers a unique novel approach for antire-modeling therapy in progressed pulmonary hypertension...
  26. ncbi Comparison of the efficacy and safety of rosuvastatin versus atorvastatin, simvastatin, and pravastatin across doses (STELLAR* Trial)
    Peter H Jones
    Baylor College of Medicine, 6565 Fannin Avenue, A 601, Houston, TX 77030, USA
    Am J Cardiol 92:152-60. 2003
    ..0 mmol/L was achieved by 79% to 92% in rosuvastatin groups compared with 52% to 81% in atorvastatin groups. Drug tolerability was similar across treatments...
  27. ncbi Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases
    Florence I Raynaud
    Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Haddow and McElwain Laboratories, Sutton, Surrey, United Kingdom
    Cancer Res 67:5840-50. 2007
    ....
  28. ncbi The safety and efficacy of a JAK inhibitor in patients with active rheumatoid arthritis: Results of a double-blind, placebo-controlled phase IIa trial of three dosage levels of CP-690,550 versus placebo
    Joel M Kremer
    Albany Medical College, Albany, New York, USA
    Arthritis Rheum 60:1895-905. 2009
    ....
  29. ncbi Pazopanib, a multikinase angiogenesis inhibitor, in patients with relapsed or refractory advanced soft tissue sarcoma: a phase II study from the European organisation for research and treatment of cancer-soft tissue and bone sarcoma group (EORTC study 620
    Stefan Sleijfer
    Dept of Medical Oncology, Erasmus University Medical Center, Daniel den Hoed Cancer Center, Groene Hilledijk 301, 3075 EA Rotterdam, The Netherlands
    J Clin Oncol 27:3126-32. 2009
    ..7%). CONCLUSION Pazopanib is well tolerated in patients with relapsed, advanced STS and demonstrates interesting activity that warrants additional study in patients with leiomyosarcomas, synovial sarcomas, and other STS types...
  30. ncbi Role of AMP-activated protein kinase in mechanism of metformin action
    G Zhou
    Department of Molecular Endocrinology, Merck Research Laboratories, Rahway, New Jersey 07065, USA
    J Clin Invest 108:1167-74. 2001
    ..Activation of AMPK provides a unified explanation for the pleiotropic beneficial effects of this drug; these results also suggest that alternative means of modulating AMPK should be useful for the treatment of metabolic disorders...
  31. ncbi Dasatinib: a potent SRC inhibitor in clinical development for the treatment of solid tumors
    John Araujo
    Genitourinary Center, M D Anderson Cancer Centre, Houston, TX 77030, USA
    Cancer Treat Rev 36:492-500. 2010
    ..Future clinical trials will further assess the clinical value of SRC inhibition with dasatinib...
  32. ncbi Persistence of malignant hematopoietic progenitors in chronic myelogenous leukemia patients in complete cytogenetic remission following imatinib mesylate treatment
    Ravi Bhatia
    Division of Hematology and Bone Marrow Transplantation, City of Hope National Medical Center, Duarte, CA 91010, USA
    Blood 101:4701-7. 2003
    ..Patients in CCR with imatinib mesylate treatment need to be followed carefully to assess for risk of relapse...
  33. ncbi Critical role for Gab2 in transformation by BCR/ABL
    Martin Sattler
    Dana Farber Cancer Institute, Department of Adult Oncology, Harvard Medical School, 44 Binney Street, Boston, Massachusetts 02115, USA
    Cancer Cell 1:479-92. 2002
    ..Our results identify Gab2 and its associated proteins as key determinants of the lineage and severity of BCR/ABL transformation...
  34. ncbi Rosuvastatin for primary prevention in patients with European systematic coronary risk evaluation risk ≥ 5% or Framingham risk >20%: post hoc analyses of the JUPITER trial requested by European health authorities
    Wolfgang Koenig
    Department of Internal Medicine II Cardiology, University of Ulm Medical Center, Albert Einstein Allee 23, Ulm, Germany
    Eur Heart J 32:75-83. 2011
    ..However, as these are post hoc analyses, data describing these subgroups have not previously been available to the clinical community...
  35. ncbi Correlation of computed tomography and positron emission tomography in patients with metastatic gastrointestinal stromal tumor treated at a single institution with imatinib mesylate: proposal of new computed tomography response criteria
    Haesun Choi
    Division of Diagnostic Imaging and Department of Sarcoma Medical Oncology, The University of Texas M D Anderson Cancer Center, Houston, TX 77030, USA
    J Clin Oncol 25:1753-9. 2007
    ....
  36. ncbi Pharmacokinetic-pharmacodynamic correlation from mouse to human with pazopanib, a multikinase angiogenesis inhibitor with potent antitumor and antiangiogenic activity
    Rakesh Kumar
    Oncology Biology, GlaxoSmithKline, 1250 South Collegeville Road, UP1450, Collegeville, PA 19426, USA
    Mol Cancer Ther 6:2012-21. 2007
    ..Furthermore, the steady-state concentration of pazopanib determined from preclinical activity showed a strong correlation with the pharmacodynamic effects and antitumor activity in the phase I clinical trial...
  37. ncbi The CML stem cell: evolution of the progenitor
    Scott A Stuart
    Division of Hematology Oncology, Department of Medicine, University of California at San Diego, School of Medicine, La Jolla, CA 92093, USA
    Cell Cycle 8:1338-43. 2009
    ..Characterization of these cells and evaluation of their sensitivity to imatinib is critical to our understanding and treatment of CML blast crisis...
  38. ncbi Correlation of kinase genotype and clinical outcome in the North American Intergroup Phase III Trial of imatinib mesylate for treatment of advanced gastrointestinal stromal tumor: CALGB 150105 Study by Cancer and Leukemia Group B and Southwest Oncology Gr
    Michael C Heinrich
    Division of Hematology Oncology, Department of Medicine and Cell and Developmental Biology, Portland Veterans Affairs Medical Center and Oregon Health and Science University Cancer Institute, Portland, OR 97239, USA
    J Clin Oncol 26:5360-7. 2008
    ..In previous studies, GIST genotype correlated with treatment outcome and optimal imatinib dosing...
  39. ncbi Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor
    M C Heinrich
    Division of Hematology and Medical Oncology, Department of Medicine, Oregon Health Sciences University, and Portland Veterans Affairs Medical Center, USA
    Blood 96:925-32. 2000
    ..This compound may be useful in treating cancers associated with increased c-kit kinase activity...
  40. ncbi Prospective multicentric randomized phase III study of imatinib in patients with advanced gastrointestinal stromal tumors comparing interruption versus continuation of treatment beyond 1 year: the French Sarcoma Group
    Jean Yves Blay
    Unité INSERM U590 Centre Léon Bérard and Université Claude Bernard Lyon I and Hopital Edouard Herriot, Lyon, France
    J Clin Oncol 25:1107-13. 2007
    ..Imatinib is the standard treatment of advanced GI stromal tumors (GISTs). It is not known whether imatinib may be stopped in patients in whom disease is controlled...
  41. ncbi Efficacy and safety of ABT-335 (fenofibric acid) in combination with rosuvastatin in patients with mixed dyslipidemia: a phase 3 study
    Peter H Jones
    Baylor College of Medicine, Houston, TX 77030, USA
    Atherosclerosis 204:208-15. 2009
    ..To evaluate a new formulation of fenofibric acid (ABT-335) co-administered with 2 doses of rosuvastatin in patients with mixed dyslipidemia...
  42. ncbi Safety and tolerability of oral paliperidone extended-release tablets in elderly patients with schizophrenia: a double-blind, placebo-controlled study with six-month open-label extension
    Andreas Tzimos
    Psychiatric Hospital of Thessaloniki, Thessaloniki, Greece
    Am J Geriatr Psychiatry 16:31-43. 2008
    ..The study was not powered to show statistical differences...
  43. ncbi PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib
    Christopher L Corless
    Department of Pathology, Division of Hematology and Oncology, Oregon Health and Science University Cancer Institute, Portland, OR 97201, USA
    J Clin Oncol 23:5357-64. 2005
    ..Little is known of the other types of PDGFRA mutations that occur in GISTs...
  44. ncbi Effective killing of Gleevec-resistant CML cells with T315I mutation by a natural compound PEITC through redox-mediated mechanism
    H Zhang
    Department of Molecular Pathology, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA
    Leukemia 22:1191-9. 2008
    ..Our results suggest that PEITC is a promising compound capable of killing Gleevec-resistant CML cells through a ROS-mediated mechanism and warrants further investigations...
  45. ncbi Phase I trial of pazopanib in patients with advanced cancer
    Herbert I Hurwitz
    Duke University Medical Center, Durham, North Carolina, USA
    Clin Cancer Res 15:4220-7. 2009
    ....
  46. ncbi Reduction in C-reactive protein and LDL cholesterol and cardiovascular event rates after initiation of rosuvastatin: a prospective study of the JUPITER trial
    Paul M Ridker
    Center for Cardiovascular Disease Prevention, Brigham and Women s Hospital, Harvard Medical School, Boston, MA, USA
    Lancet 373:1175-82. 2009
    ..8 mmol/L (<70 mg/dL). However, the benefit of lowering both LDL cholesterol and hsCRP after the start of statin therapy is controversial. We prospectively tested this hypothesis...
  47. ncbi Dasatinib inhibits migration and invasion in diverse human sarcoma cell lines and induces apoptosis in bone sarcoma cells dependent on SRC kinase for survival
    Audrey C Shor
    Gonzmart Laboratory, Sarcoma Program, H Lee Moffitt Cancer Center and Research Institute, Tampa, Florida, USA
    Cancer Res 67:2800-8. 2007
    ..Therefore, dasatinib may provide therapeutic benefit by preventing the growth and metastasis of sarcomas in patients...
  48. ncbi Solution conformations and dynamics of ABL kinase-inhibitor complexes determined by NMR substantiate the different binding modes of imatinib/nilotinib and dasatinib
    Navratna Vajpai
    Novartis Institutes for BioMedical Research, Basel, Switzerland
    J Biol Chem 283:18292-302. 2008
    ..Nanosecond as well as microsecond dynamics can be detected for certain residues in the activation loop in the inactive and active conformation complexes...
  49. ncbi Rosuvastatin for primary prevention in older persons with elevated C-reactive protein and low to average low-density lipoprotein cholesterol levels: exploratory analysis of a randomized trial
    Robert J Glynn
    Division of Preventive Medicine, Brigham and Women s Hospital, Harvard Medical School, Boston, Massachusetts 02215, USA
    Ann Intern Med 152:488-96, W174. 2010
    ..Randomized data on statins for primary prevention in older persons are limited, and the relative hazard of cardiovascular disease associated with an elevated cholesterol level weakens with advancing age...
  50. ncbi Voriconazole versus amphotericin B for primary therapy of invasive aspergillosis
    Raoul Herbrecht
    Département d Hématologie et d Oncologie, Hopital de Hautepierre, Strasbourg, France
    N Engl J Med 347:408-15. 2002
    ..Voriconazole is a broad-spectrum triazole that is active against aspergillus species. We conducted a randomized trial to compare voriconazole with amphotericin B for primary therapy of invasive aspergillosis...
  51. ncbi The specificities of protein kinase inhibitors: an update
    Jenny Bain
    Division of Signal Transduction Therapy, School of Life Sciences, MSI/WTB Complex, University of Dundee, Dow Street, Dundee DD1 5EH, Scotland, UK
    Biochem J 371:199-204. 2003
    ..33 microM) and p38-regulated/activated kinase (PRAK; IC(50)=1.0 microM)...
  52. ncbi Activation of the PI3K/mTOR pathway by BCR-ABL contributes to increased production of reactive oxygen species
    Jeong H Kim
    Department of Medical Oncology, Dana-Farber Cancer Institute, 44 Binney St, Boston, MA 02115, USA
    Blood 105:1717-23. 2005
    ..Finally, these results hint at novel targets for drug development that may aid traditional therapy...
  53. ncbi The small-molecule VEGF receptor inhibitor pazopanib (GW786034B) targets both tumor and endothelial cells in multiple myeloma
    Klaus Podar
    Department of Medical Oncology, Dana Farber Cancer Institute, Harvard Medical School, Boston, MA 02115, USA
    Proc Natl Acad Sci U S A 103:19478-83. 2006
    ....
  54. ncbi Phase II, open-label study of pazopanib or lapatinib monotherapy compared with pazopanib plus lapatinib combination therapy in patients with advanced and recurrent cervical cancer
    Bradley J Monk
    University of California Irvine Medical Center, Orange, CA 92868, USA
    J Clin Oncol 28:3562-9. 2010
    ..In cervical cancer, EGFR and HER2/neu overexpression and high microvascular density correlate with survival...
  55. ncbi Poor adherence is the main reason for loss of CCyR and imatinib failure for chronic myeloid leukemia patients on long-term therapy
    Amr R Ibrahim
    Department of Haematology, Imperial College London, Hammersmith Hospital, Du Cane Road, London, United Kingdom
    Blood 117:3733-6. 2011
    ..In summary, we have shown that poor adherence is the principal factor contributing to the loss of cytogenetic responses and treatment failure in patients on long-term therapy...
  56. ncbi Inhibition of NEDD8-activating enzyme: a novel approach for the treatment of acute myeloid leukemia
    Ronan T Swords
    Institute for Drug Development, Cancer Therapy and Research Center at The University of Texas Health Science Center at San Antonio, San Antonio, TX 78245, USA
    Blood 115:3796-800. 2010
    ..Our findings indicate that MLN4924 is a highly promising novel agent that has advanced into clinical trials for the treatment of AML...
  57. ncbi Combined blockade of Src kinase and epidermal growth factor receptor with gemcitabine overcomes STAT3-mediated resistance of inhibition of pancreatic tumor growth
    Nagathihalli S Nagaraj
    Department of Surgery, Vanderbilt University School of Medicine, Nashville, Tennessee, USA
    Clin Cancer Res 17:483-93. 2011
    ..The purpose of this study was to translate the current understanding of complementary activated tyrosine kinase signaling pathways by targeting Src kinase and epidermal growth factor receptor (EGFR)...
  58. ncbi Primary and secondary kinase genotypes correlate with the biological and clinical activity of sunitinib in imatinib-resistant gastrointestinal stromal tumor
    Michael C Heinrich
    Division of Hematology Oncology, Department of Medicine and Cell and Developmental Biology, Portland Veterans Affairs Medical Center and Oregon Health and Science University Cancer Institute, Portland, OR 97239, USA
    J Clin Oncol 26:5352-9. 2008
    ..We evaluated the impact of primary and secondary kinase genotype on sunitinib activity...
  59. ncbi Philadelphia chromosome-positive acute lymphoblastic leukemia: current treatment and future perspectives
    Hun J Lee
    Leukemia Section, Department of Medicine, Roswell Park Cancer Institute, Buffalo, New York 14263, USA
    Cancer 117:1583-94. 2011
    ..For this article, the authors reviewed past, current, and future treatment approaches for adult and elderly patients with Ph-positive ALL with a focus on TKIs and combined chemotherapeutic regimens...
  60. ncbi Efficacy and safety of sunitinib in patients with advanced gastrointestinal stromal tumour after failure of imatinib: a randomised controlled trial
    George D Demetri
    Ludwig Center at Dana Farber Cancer Institute and Harvard Medical School, Boston, MA 02115, USA
    Lancet 368:1329-38. 2006
    ....
  61. ncbi Bone marrow mesenchymal stromal cells non-selectively protect chronic myeloid leukemia cells from imatinib-induced apoptosis via the CXCR4/CXCL12 axis
    Fabrizio Vianello
    Department of Haematology, Kennedy Institute of Rheumatology, Imperial College, London, UK
    Haematologica 95:1081-9. 2010
    ..Mesenchymal stromal cells in the bone marrow may favor the persistence and progression of leukemia by preserving the proliferation and self-renewal capacities of the malignant progenitor cells...
  62. ncbi Hypereosinophilic syndrome and clonal eosinophilia: point-of-care diagnostic algorithm and treatment update
    Ayalew Tefferi
    Division of Hematology, Mayo Clinic, Rochester, MN 55905, USA
    Mayo Clin Proc 85:158-64. 2010
    ..In the current review, we provide a simplified algorithm for distinguishing the various causes of clonal and idiopathic eosinophilia and discuss current therapy, including new drugs (imatinib mesylate, alemtuzumab, and mepolizumab)...
  63. ncbi Tyrosine kinase inhibitors reverse type 1 diabetes in nonobese diabetic mice
    Cedric Louvet
    Diabetes Center and the Department of Medicine, University of California, San Francisco, CA 94143, USA
    Proc Natl Acad Sci U S A 105:18895-900. 2008
    ..Thus, long-term efficacy and tolerance is likely to depend on inhibiting a combination of tyrosine kinases supporting the use of selective kinase inhibitors as a new, potentially very attractive approach for the treatment of T1D...
  64. ncbi Drug-resistant aurora A mutants for cellular target validation of the small molecule kinase inhibitors MLN8054 and MLN8237
    Dominic A Sloane
    Yorkshire Cancer Research Institute for Cancer Studies, University of Sheffield, UK
    ACS Chem Biol 5:563-76. 2010
    ....
  65. ncbi Riociguat for chronic thromboembolic pulmonary hypertension and pulmonary arterial hypertension: a phase II study
    H A Ghofrani
    Dept of Internal Medicine, Medical Clinic II V, University Hospital Giessen and Marburg GmbH, Klinikstrasse 36, 35392 Giessen, Germany
    Eur Respir J 36:792-9. 2010
    ..These preliminary data show that riociguat has a favourable safety profile and improves exercise capacity, symptoms and pulmonary haemodynamics in CTEPH and PAH. Randomised controlled trials are underway...
  66. ncbi Reduction of CCR5 with low-dose rapamycin enhances the antiviral activity of vicriviroc against both sensitive and drug-resistant HIV-1
    Alonso Heredia
    Institute of Human Virology, University of Maryland School of Medicine, Baltimore, MD 21201, USA
    Proc Natl Acad Sci U S A 105:20476-81. 2008
    ....
  67. ncbi First acute haemodynamic study of soluble guanylate cyclase stimulator riociguat in pulmonary hypertension
    F Grimminger
    Dept of Internal Medicine, University Hospital Giessen and Marburg, Giessen, Germany
    Eur Respir J 33:785-92. 2009
    ..The drug was well-tolerated and superior to nitric oxide in efficacy and duration. Riociguat, therefore, has potential as a novel therapy for pulmonary hypertension and warrants further investigation...
  68. ncbi Treatment with imatinib prevents fibrosis in different preclinical models of systemic sclerosis and induces regression of established fibrosis
    Alfiya Akhmetshina
    Department of Internal Medicine III, University of Erlangen Nuremberg, Erlangen, Germany
    Arthritis Rheum 60:219-24. 2009
    ....
  69. ncbi Elevations of creatine kinase in patients treated with imatinib mesylate (Gleevec)
    Jessica K Gordon
    Department of Rheumatology, Hospital for Special Surgeryy, New York, NY 10021, USA
    Leuk Res 34:827-9. 2010
    ..We found a high prevalence of CK abnormalities in this group and believe that CKs should be monitored during therapy with imatinib...
  70. ncbi In silico analysis of kinase expression identifies WEE1 as a gatekeeper against mitotic catastrophe in glioblastoma
    Shahryar E Mir
    Neuro oncology Research Group, Departments of Neurosurgery and Pediatric Oncology Hematology, VU University Medical Center, 1081 HV, Amsterdam, The Netherlands
    Cancer Cell 18:244-57. 2010
    ..Our results suggest that inhibition of WEE1 kinase holds potential as a therapeutic approach in treatment of glioblastoma...
  71. ncbi Delayed achievement of cytogenetic and molecular response is associated with increased risk of progression among patients with chronic myeloid leukemia in early chronic phase receiving high-dose or standard-dose imatinib therapy
    Alfonso Quintas-Cardama
    Departments of Leukemia, University of Texas M D Anderson Cancer Center, Houston, 77030, USA
    Blood 113:6315-21. 2009
    ..This risk is discernible as early as 3 months into imatinib therapy by molecular analysis and may provide the rationale to institute therapies that render higher rates of early response...
  72. ncbi Nilotinib exerts equipotent antiproliferative effects to imatinib and does not induce apoptosis in CD34+ CML cells
    Heather G Jørgensen
    Section of Experimental Haematology, Division of Cancer Sciences and Molecular Pathology, University of Glasgow, 10 Alexandra Parade, Glasgow, UK
    Blood 109:4016-9. 2007
    ..These results confirmed that, like IM, the predominant effect of nilotinib is antiproliferative rather than proapoptotic...
  73. ncbi Intracellular tyrosine kinases as novel targets for anti-fibrotic therapy in systemic sclerosis
    J H W Distler
    Department of Internal Medicine 3, University of Erlangen Nuremberg, Germany
    Rheumatology (Oxford) 47:v10-1. 2008
    ..Based on the promising pre-clinical data, imatinib is currently evaluated in clinical trials for the treatment of fibrosis in SSc and trials with other tyrosine kinase inhibitors are in preparation...
  74. ncbi Structural basis for the recognition of the FapydG lesion (2,6-diamino-4-hydroxy-5-formamidopyrimidine) by formamidopyrimidine-DNA glycosylase
    Franck Coste
    Centre de Biophysique Moleculaire, UPR4301, CNRS, rue Charles Sadron, 45071 Orleans Cedex 02, France
    J Biol Chem 279:44074-83. 2004
    ..The significant differences between the Fpg recognition modes of 8-oxodG and FapydG provide new insights into the Fpg substrate specificity...
  75. ncbi Gastrointestinal stromal tumors: the incidence, prevalence, clinical course, and prognostication in the preimatinib mesylate era--a population-based study in western Sweden
    Bengt Nilsson
    Department of Surgery, The Lundberg Laboratory for Cancer Research, , , Sweden
    Cancer 103:821-9. 2005
    ..Prognostication in patients with GIST can be refined using a proposed risk score based solely on tumor size and proliferative index...
  76. ncbi The pharmacology and safety of paliperidone extended-release in the treatment of schizophrenia
    Edoardo Spina
    Universiy of Messina, Department of Clinical and Experimental Medicine and Pharmacology, Section of Pharmacology, Policlinico Universitario, Via Consolare Valeria, 98125 Messina, Italy
    Expert Opin Drug Saf 6:651-62. 2007
    ..Safety data from elderly patients appear to be promising. Due to negligible hepatic biotransformation, paliperidone ER is unlikely to be involved in clinically significant metabolic drug-drug interactions...
  77. ncbi Conformational disturbance in Abl kinase upon mutation and deregulation
    Roxana E Iacob
    The Barnett Institute and Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA 02115, USA
    Proc Natl Acad Sci U S A 106:1386-91. 2009
    ..Similar analyses could be performed on any protein to provide mechanistic details about conformational changes and protein function...
  78. ncbi Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK
    Anna V Galkin
    Kinase Lead Discovery, Department of Pharmacology, Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA
    Proc Natl Acad Sci U S A 104:270-5. 2007
    ..NVP-TAE684 also induced down-regulation of CD30 expression, suggesting that CD30 may be used as a biomarker of therapeutic NPM-ALK kinase activity inhibition...
  79. ncbi Risperidone and paliperidone inhibit p-glycoprotein activity in vitro
    Hao Jie Zhu
    Laboratory of Drug Disposition and Pharmacogenetics, Department of Pharmaceutical Sciences, Medical University of South Carolina, Charleston, SC, USA
    Neuropsychopharmacology 32:757-64. 2007
    ..In particular, RSP may interact with its own active metabolite PALI by promoting its brain concentration through inhibiting P-gp-mediated efflux of PALI across endothelial cells of the BBB...
  80. ncbi Oncogenic association of the Cbp/PAG adaptor protein with the Lyn tyrosine kinase in human B-NHL rafts
    Sebastien Tauzin
    Department of Pathology and Immunology, Faculty of Medicine, University of Geneva, Geneva, Switzerland
    Blood 111:2310-20. 2008
    ..The Lyn-Cbp/PAG signalosome appears to control proliferation and survival in most B-NHLs and constitutes a therapeutic target in B-NHL cells that exhibit oncogenic "addiction" to the Lyn kinase...
  81. ncbi Imatinib treatment for idiopathic pulmonary fibrosis: Randomized placebo-controlled trial results
    Craig E Daniels
    Mayo Clinic, Rochester, Minnesota, USA
    Am J Respir Crit Care Med 181:604-10. 2010
    ..Idiopathic pulmonary fibrosis (IPF) is a progressive lung disease with no known efficacious therapy. Imatinib is a tyrosine kinase inhibitor with potential efficacy to treat fibrotic lung disease...
  82. ncbi Crystal structure of the T315I Abl mutant in complex with the aurora kinases inhibitor PHA-739358
    Michele Modugno
    Nerviano Medical Sciences Srl Oncology, Milan, Italy
    Cancer Res 67:7987-90. 2007
    ....
  83. ncbi Allosteric inhibitors of Bcr-abl-dependent cell proliferation
    Francisco J Adrian
    Biological Chemistry Department, Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, California 92121, USA
    Nat Chem Biol 2:95-102. 2006
    ..We propose that this new class of compounds inhibits Bcr-abl kinase activity through an allosteric non-ATP competitive mechanism...
  84. ncbi Imatinib mesylate in the treatment of refractory idiopathic pulmonary arterial hypertension
    Karen C Patterson
    Ann Intern Med 145:152-3. 2006
  85. ncbi Efficacy and tolerability of oral paliperidone extended-release tablets in the treatment of acute schizophrenia: pooled data from three 6-week, placebo-controlled studies
    Herbert Y Meltzer
    Department of Psychiatry, Vanderbilt Medical Center, Nashville, TN, USA
    J Clin Psychiatry 69:817-29. 2008
    ..To evaluate the efficacy and safety of an extended-release (ER) formulation of paliperidone in patients with an acute episode of schizophrenia, in the dosage range of 3 to 15 mg daily...
  86. ncbi Imatinib mesylate blocks a non-Smad TGF-beta pathway and reduces renal fibrogenesis in vivo
    Shinong Wang
    Los Angeles Biomedical Research Institute at Harbor-UCLA Medical Center, California, USA
    FASEB J 19:1-11. 2005
    ..Inhibition of c-abl activity with imatinib mesylate ameliorates experimental renal fibrosis in rats...
  87. ncbi Comparison of imatinib mesylate, dasatinib (BMS-354825), and nilotinib (AMN107) in an N-ethyl-N-nitrosourea (ENU)-based mutagenesis screen: high efficacy of drug combinations
    Heather A Bradeen
    Oregon Health and Science University Cancer Institute, L592, 3181 SW Sam Jackson Park Rd, Portland, OR 97239, USA
    Blood 108:2332-8. 2006
    ..However, sequencing uniformly revealed T315I, consistent with the need for a T315I inhibitor, to completely block resistance...
  88. ncbi Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2
    Morris E Feldman
    Howard Hughes Medical Institute and Department of Cellular and Molecular Pharmacology, University of California San Francisco, San Francisco, USA
    PLoS Biol 7:e38. 2009
    ..These potent new pharmacological agents complement rapamycin in the study of mTOR and its role in normal physiology and human disease...
  89. ncbi Choosing the best treatment strategy for chronic myeloid leukemia patients resistant to imatinib: weighing the efficacy and safety of individual drugs with BCR-ABL mutations and patient history
    E Jabbour
    Department of Leukemia, The University of Texas MD Anderson Cancer Center, 1515 Holcombe Blvd, Unit 423, Houston, TX 77030, USA
    Leukemia 24:6-12. 2010
    ..Here, we propose a treatment algorithm for imatinib-resistant patients based on BCR-ABL mutation status and patient history...
  90. ncbi Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRalpha, Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants
    Ellen Weisberg
    Department of Medical Oncology Hematologic Neoplasia, Dana Farber Cancer Institute, Boston, MA
    Blood 115:4206-16. 2010
    ..The distinctive ability of HG-7-85-01 to simultaneously inhibit both wild-type and mutant forms of several kinases of clinical relevance is an important step in the development of the next generation of tyrosine kinase inhibitors...
  91. ncbi Extended kinase profile and properties of the protein kinase inhibitor nilotinib
    Paul W Manley
    Novartis Institutes for BioMedical Research, Basel, Switzerland
    Biochim Biophys Acta 1804:445-53. 2010
    ..Although neither enzymatic nor cellular data are yet available to substantiate the drug as an inhibitor of ZAK phosphorylation, modeling predicts that it binds in an ATP-competitive fashion...
  92. ncbi Effects of rosuvastatin and atorvastatin on LDL and HDL particle concentrations in patients with metabolic syndrome: a randomized, double-blind, controlled study
    Robert S Rosenson
    University of Michigan, Ann Arbor, Michigan, USA
    Diabetes Care 32:1087-91. 2009
    ..Changes in lipoprotein particle concentration may predict the risk of coronary heart disease more accurately than lipoprotein cholesterol levels...
  93. ncbi Imatinib resistance associated with BCR-ABL upregulation is dependent on HIF-1alpha-induced metabolic reprograming
    F Zhao
    Department of Cancer Biology, Abramson Cancer Center, University of Pennsylvania School of Medicine, Philadelphia, PA 19104, USA
    Oncogene 29:2962-72. 2010
    ..Together, these results suggest that oxythiamine can enhance imatinib efficacy in patients who present an accelerated form of the disease...
  94. ncbi Effects of statin therapy according to plasma high-sensitivity C-reactive protein concentration in the Controlled Rosuvastatin Multinational Trial in Heart Failure (CORONA): a retrospective analysis
    John J V McMurray
    British Heart Foundation Glasgow Cardiovascular Research Centre, University of Glasgow, Glasgow, G12 8TA, UK
    Circulation 120:2188-96. 2009
    ..We examined whether the antiinflammatory action of statins may be of benefit in heart failure, a state characterized by inflammation in which low cholesterol is associated with worse outcomes...
  95. ncbi Substrate specificity of the Escherichia coli Fpg protein (formamidopyrimidine-DNA glycosylase): excision of purine lesions in DNA produced by ionizing radiation or photosensitization
    S Boiteux
    URA 158 CNRS, U 140 INSERM, Institut Gustave Roussy, Villejuif, France
    Biochemistry 31:106-10. 1992
    ..Thirteen products resulting from pyrimidines and purines were detected in gamma-irradiated DNA, whereas only the formation of 2,6-diamino-4-hydroxy-5-..
  96. ncbi Excision of the oxidatively formed 5-hydroxyhydantoin and 5-hydroxy-5-methylhydantoin pyrimidine lesions by Escherichia coli and Saccharomyces cerevisiae DNA N-glycosylases
    Didier Gasparutto
    Laboratoire des Lésions des Acides Nucléiques, Service de Chimie Inorganique et Biologique UMR E3 CEA UJF, INAC, DSM, CEA Grenoble, F 38054 Grenoble Cedex 9, France
    Biochim Biophys Acta 1790:16-24. 2009
    ..If not repaired, when present in cellular DNA, these base lesions may be processed by DNA polymerases that induce mutagenic and cell lethality processes...
  97. ncbi Small-molecule inhibition of Wee1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents
    Hiroshi Hirai
    Department of Oncology, Banyu Tsukuba Research Institute, Merck Research Laboratories, Tsukuba, Japan
    Mol Cancer Ther 8:2992-3000. 2009
    ..Our data indicate that Wee1 inhibition provides a new approach for treatment of multiple human malignancies...
  98. ncbi Riociguat: an upcoming therapy in chronic thromboembolic pulmonary hypertension?
    N H Kim
    Division of Pulmonary and Critical Care Medicine, University of California, San Diego, La Jolla, CA 92037 1300, USA
    Eur Respir Rev 19:68-71. 2010
    ....
  99. ncbi Empirical relationship between intra-purine and intra-pyrimidine differences in conserved gene sequences
    Ashesh Nandy
    School of Environmental Studies, Jadavpur University, Kolkata, West Bengal, India
    PLoS ONE 4:e6829. 2009
    ..since the simple rule given by Chargaff almost a century ago that equates the total number of purines to the pyrimidines in a duplex DNA sequence...
  100. ncbi Effect of rosuvastatin on coronary atheroma in stable coronary artery disease: multicenter coronary atherosclerosis study measuring effects of rosuvastatin using intravascular ultrasound in Japanese subjects (COSMOS)
    Tadateru Takayama
    Division of Cardiology, Nihon University School of Medicine, Tokyo, Japan
    Circ J 73:2110-7. 2009
    ..The effect of rosuvastatin on plaque volume in patients with stable coronary artery disease (CAD), including those receiving prior lipid-lowering therapy, was examined in the present study...
  101. ncbi Second generation inhibitors of BCR-ABL for the treatment of imatinib-resistant chronic myeloid leukaemia
    Ellen Weisberg
    Dana Farber Cancer Institute, Mayer 540, 44 Binney Street, Boston, MA 02115, USA
    Nat Rev Cancer 7:345-56. 2007
    ..Here, we describe the mechanism of action of imatinib in CML, the structural basis of imatinib resistance, and the potential of second-generation BCR-ABL inhibitors to circumvent resistance...

Research Grants72

  1. LIPOPHILIC ANTIFOLATES AND AIDS OPPORTUNISTIC INFECTIONS
    Andre Rosowsky; Fiscal Year: 2000
    ..The 2,4-diamino compounds to be studied include: (a) pyridol[2,3-d]pyrimidines with H or Me at C5 and a small alkyl group or substituted Phe ring at C6; (b) pyrrolo[2,3-d]pyrimidines with a ..
  2. LIPOPHILIC ANTIFOLATES AND AIDS OPPORTUNISTIC INFECTIONS
    Andre Rosowsky; Fiscal Year: 2004
    ..way to achieve selectivity is with 2,4-diamino-5-[(2-methoxy- and 3,4-dimethoxy-5-(C3-9)alkoxy)-benzyl] pyrimidines containing an acidic carboxyl or tetrazole group at the end of the O-alkyl side chain...
  3. SELENIUM AND LUNG CANCER RISK
    Henry Thompson; Fiscal Year: 2003
    ..single cell gel electrophoresis assay that detects DNA strand breaks as well as oxidative damage to purines and pyrimidines. This project will contribute to understanding whether intermediate biomarkers for lung cancer can be altered ..
  4. Structural Biology of Purine and Pyrimidine Biosynthesis and Metabolism
    Steven E Ealick; Fiscal Year: 2010
    ..Catabolic pathways for the degradation of purines and pyrimidines have been previously described and structures are available for the key enzymes;however, recently a new pathway ..
  5. Structural Biology of Purine and Pyrimidine Biosynthesis and Metabolism
    Steven Ealick; Fiscal Year: 2009
    ..Catabolic pathways for the degradation of purines and pyrimidines have been previously described and structures are available for the key enzymes; however, recently a new ..
  6. SELENIUM AND LUNG CANCER RISK
    Henry Thompson; Fiscal Year: 2002
    ..from endobronchial biopsy and sputum using the COMET assay (in the presence and absence damage to purines and pyrimidines. Level of MDA and 8-EPG in sputum also will determined...
  7. Hybridization of Oligonucleotide Probes with Duplex DNA
    Maxim Frank Kamenetskii; Fiscal Year: 2005
    ..PNA openers with the extended triplex recognition will be used for mostly purine sites with few pyrimidines. A pseudocomplementary PNA modification, pcPNA, will be employed as an opener to substantially relieve the PD-..
  8. SIMULATION OF PROTON AND HYDRIDE TRANSFER IN ENZYMES
    Sharon Hammes Schiffer; Fiscal Year: 2010
    ..This enzyme maintains tetrahydrofolate levels required to support the biosynthesis of purines, pyrimidines, and amino acids...
  9. FUNCTION OF THE S CEREVISIAE PHRI GENE AND PHOTOLYASE
    GWENDOLYN SANCAR; Fiscal Year: 1992
    ..dimers in DNA and upon exposure to near UV or visible light cleave the cyclobutane ring and restore the pyrimidines to their original structure...
  10. STRUCTURE AND REGULATION OF E. COLI DNA PHOTOLYASE
    Aziz Sancar; Fiscal Year: 1990
    ..converts visible light (350-600 nm) energy into chemical energy to break the cyclobutane ring joining the two pyrimidines, thus restoring the integrity of the DNA. Photolyase of E...
  11. SIMULATION OF PROTON AND HYDRIDE TRANSFER IN ENZYMES
    Sharon Hammes Schiffer; Fiscal Year: 2009
    ..This enzyme maintains tetrahydrofolate levels required to support the biosynthesis of purines, pyrimidines, and amino acids...
  12. TRIPTYCENE ANALOGS--NOVEL BIFUNCTIONAL ANTICANCER DRUGS
    Jean Pierre Perchellet; Fiscal Year: 2004
    ..transport (effects on equilibrative and Na+-dependent transporters, bidirectional fluxes of purines and pyrimidines, competition with nucleoside transport probes), DNA (binding, intercalation, strand breakage and crosslinks, ..
  13. ROLE AND FUNCTION OF PYRIMIDINES IN CANCER THERAPY
    Giuseppe Pizzorno; Fiscal Year: 1999
    ....
  14. ROLE AND FUNCTIONS OF PYRIMIDINES IN CANCER THERAPY
    Giuseppe Pizzorno; Fiscal Year: 2004
    ..Specific alterations of UPase genetic information will be achieved by: a) targeted disruption of UPase gene to nullify the UPase allele, and conversely, b) UPase gene transfer to elevate the UPase expression and activity in tissues. ..