dideoxynucleosides

Summary

Summary: Nucleosides that have two hydroxy groups removed from the sugar moiety. The majority of these compounds have broad-spectrum antiretroviral activity due to their action as antimetabolites. The nucleosides are phosphorylated intracellularly to their 5'-triphosphates and act as chain-terminating inhibitors of viral reverse transcription.

Top Publications

  1. ncbi Imaging proliferation in vivo with [F-18]FLT and positron emission tomography
    A F Shields
    Karmanos Cancer Institute, Department of Medicine, Wayne State University, Detroit Medical Center, MI 48301, USA
    Nat Med 4:1334-6. 1998
  2. ncbi Simplification of antiretroviral therapy with tenofovir-emtricitabine or abacavir-Lamivudine: a randomized, 96-week trial
    Allison Martin
    National Centre in HIV Epidemiology and Clinical Research UNSW, 5St Vincent s Centre for Applied Medical Research, Sydney, Australia
    Clin Infect Dis 49:1591-601. 2009
  3. ncbi 18F-fluoro-L-thymidine and 11C-methylmethionine as markers of increased transport and proliferation in brain tumors
    Andreas H Jacobs
    Laboratory for Gene Therapy and Molecular Imaging, Max Planck Institute for Neurological Research, Cologne, Germany
    J Nucl Med 46:1948-58. 2005
  4. ncbi Validation of FLT uptake as a measure of thymidine kinase-1 activity in A549 carcinoma cells
    Janet S Rasey
    Department of Radiation Oncology, University of Washington School of Medicine, Seattle, Washington 98195, USA
    J Nucl Med 43:1210-7. 2002
  5. ncbi Imaging proliferation in brain tumors with 18F-FLT PET: comparison with 18F-FDG
    Wei Chen
    Department of Molecular and Medical Pharmacology, David Geffen School of Medicine, University of California Los Angeles, Los Angeles, CA, USA
    J Nucl Med 46:945-52. 2005
  6. ncbi Comparison of changes in bone density and turnover with abacavir-lamivudine versus tenofovir-emtricitabine in HIV-infected adults: 48-week results from the ASSERT study
    Hans Jurgen Stellbrink
    Infektions Medizinisches Centrum Hamburg Study Center, Hamburg, Germany
    Clin Infect Dis 51:963-72. 2010
  7. pmc Bone mineral density and fractures in antiretroviral-naive persons randomized to receive abacavir-lamivudine or tenofovir disoproxil fumarate-emtricitabine along with efavirenz or atazanavir-ritonavir: Aids Clinical Trials Group A5224s, a substudy of ACTG
    Grace A McComsey
    Departments of Pediatrics and Medicine, Rainbow Babies and Children s Hospital, Case Western Reserve University, Cleveland, OH 44106, USA
    J Infect Dis 203:1791-801. 2011
  8. ncbi Glioma proliferation as assessed by 3'-fluoro-3'-deoxy-L-thymidine positron emission tomography in patients with newly diagnosed high-grade glioma
    Roland Ullrich
    Max Planck Institute for Neurological Research with Klaus Joachim Zülch Laboratories, Cologne, Germany
    Clin Cancer Res 14:2049-55. 2008
  9. ncbi Randomized comparison of renal effects, efficacy, and safety with once-daily abacavir/lamivudine versus tenofovir/emtricitabine, administered with efavirenz, in antiretroviral-naive, HIV-1-infected adults: 48-week results from the ASSERT study
    Frank A Post
    King s College London, London, United Kingdom
    J Acquir Immune Defic Syndr 55:49-57. 2010
  10. ncbi Impact of individual antiretroviral drugs on the risk of myocardial infarction in human immunodeficiency virus-infected patients: a case-control study nested within the French Hospital Database on HIV ANRS cohort CO4
    Sylvie Lang
    INSERM Unité 943, 56 Boulevard V Auriol, Paris Cedex 13, France
    Arch Intern Med 170:1228-38. 2010

Research Grants

  1. NUCLEOSIDES WITH DUAL ANTI-HIV AND HBV ACTIVITY
    RAYMOND SCHINAZI; Fiscal Year: 2009
  2. PHARMACOLOGY OF DIDEOXYNUCLEOSIDES IN SMALL INTESTINAL
    JESSIE AU; Fiscal Year: 1991
  3. NEW STRATEGIES FOR GLYCOCONJUGATE SYNTHESIS FROM ALKYNES
    Frank McDonald; Fiscal Year: 1999
  4. NEW PHENYL NUCLEOSIDES AS ANTI-HIV AGENTS
    Shashikant Phadtare; Fiscal Year: 2003
  5. MULTIFUNCTIONAL PHOSPHONOFORMATE PRODRUGS AGAINST HIV 1
    Andre Rosowsky; Fiscal Year: 1993
  6. FETAL TOXICITY OF ZIDOVUDINE
    Jashvant Unadkat; Fiscal Year: 1993
  7. BIOCHEMICAL MODULATION OF ANTI-HIV DIDEOXYNUCLEOSIDES
    Arnold Fridland; Fiscal Year: 1993
  8. POTENTIATION OF ANTI-VIRAL NUCLEOSIDE ACTIVITY
    Thomas Chan; Fiscal Year: 1991
  9. Boronated L-nucleotides targeted against HIV
    Barbara Shaw; Fiscal Year: 2005
  10. CARRIERS FOR MEMBRANE TRANSPORT OF AIDS-TARGETED DRUGS
    Julius Rebek; Fiscal Year: 1992

Detail Information

Publications240 found, 100 shown here

  1. ncbi Imaging proliferation in vivo with [F-18]FLT and positron emission tomography
    A F Shields
    Karmanos Cancer Institute, Department of Medicine, Wayne State University, Detroit Medical Center, MI 48301, USA
    Nat Med 4:1334-6. 1998
    ....
  2. ncbi Simplification of antiretroviral therapy with tenofovir-emtricitabine or abacavir-Lamivudine: a randomized, 96-week trial
    Allison Martin
    National Centre in HIV Epidemiology and Clinical Research UNSW, 5St Vincent s Centre for Applied Medical Research, Sydney, Australia
    Clin Infect Dis 49:1591-601. 2009
    ..Which fixed-dose-combination tablet is more effective and safe is uncertain...
  3. ncbi 18F-fluoro-L-thymidine and 11C-methylmethionine as markers of increased transport and proliferation in brain tumors
    Andreas H Jacobs
    Laboratory for Gene Therapy and Molecular Imaging, Max Planck Institute for Neurological Research, Cologne, Germany
    J Nucl Med 46:1948-58. 2005
    ..Additionally, the longer half-life might permit differentiation between transport and intracellular phosphorylation...
  4. ncbi Validation of FLT uptake as a measure of thymidine kinase-1 activity in A549 carcinoma cells
    Janet S Rasey
    Department of Radiation Oncology, University of Washington School of Medicine, Seattle, Washington 98195, USA
    J Nucl Med 43:1210-7. 2002
    ..We tested the accuracy with which FLT uptake predicted the activity of cytosolic thymidine kinase-1 (TK(1)), an enzyme that is upregulated before and during DNA synthesis...
  5. ncbi Imaging proliferation in brain tumors with 18F-FLT PET: comparison with 18F-FDG
    Wei Chen
    Department of Molecular and Medical Pharmacology, David Geffen School of Medicine, University of California Los Angeles, Los Angeles, CA, USA
    J Nucl Med 46:945-52. 2005
    ..We characterized (18)F-FLT PET of brain gliomas and compared (18)F-FLT with (18)F-FDG PET in side-by-side studies of the same patients...
  6. ncbi Comparison of changes in bone density and turnover with abacavir-lamivudine versus tenofovir-emtricitabine in HIV-infected adults: 48-week results from the ASSERT study
    Hans Jurgen Stellbrink
    Infektions Medizinisches Centrum Hamburg Study Center, Hamburg, Germany
    Clin Infect Dis 51:963-72. 2010
    ..Abacavir-lamivudine and tenofovir DF-emtricitabine fixed-dose combinations are commonly used as first-line antiretroviral therapies. However, few studies have comprehensively compared their relative safety profiles...
  7. pmc Bone mineral density and fractures in antiretroviral-naive persons randomized to receive abacavir-lamivudine or tenofovir disoproxil fumarate-emtricitabine along with efavirenz or atazanavir-ritonavir: Aids Clinical Trials Group A5224s, a substudy of ACTG
    Grace A McComsey
    Departments of Pediatrics and Medicine, Rainbow Babies and Children s Hospital, Case Western Reserve University, Cleveland, OH 44106, USA
    J Infect Dis 203:1791-801. 2011
    ..Long-term effects of abacavir (ABC)-lamivudine (3TC), compared with tenofovir (TDF)-emtricitabine (FTC) with efavirenz (EFV) or atazanavir plus ritonavir (ATV/r), on bone mineral density (BMD) have not been analyzed...
  8. ncbi Glioma proliferation as assessed by 3'-fluoro-3'-deoxy-L-thymidine positron emission tomography in patients with newly diagnosed high-grade glioma
    Roland Ullrich
    Max Planck Institute for Neurological Research with Klaus Joachim Zülch Laboratories, Cologne, Germany
    Clin Cancer Res 14:2049-55. 2008
    ....
  9. ncbi Randomized comparison of renal effects, efficacy, and safety with once-daily abacavir/lamivudine versus tenofovir/emtricitabine, administered with efavirenz, in antiretroviral-naive, HIV-1-infected adults: 48-week results from the ASSERT study
    Frank A Post
    King s College London, London, United Kingdom
    J Acquir Immune Defic Syndr 55:49-57. 2010
    ..Abacavir/lamivudine and tenofovir/emtricitabine fixed-dose combinations are commonly used first-line antiretroviral therapies, yet few studies have comprehensively compared their safety profiles...
  10. ncbi Impact of individual antiretroviral drugs on the risk of myocardial infarction in human immunodeficiency virus-infected patients: a case-control study nested within the French Hospital Database on HIV ANRS cohort CO4
    Sylvie Lang
    INSERM Unité 943, 56 Boulevard V Auriol, Paris Cedex 13, France
    Arch Intern Med 170:1228-38. 2010
    ..The role of exposure to specific antiretroviral drugs on risk of myocardial infarction in human immunodeficiency virus (HIV)-infected patients is debated in the literature...
  11. ncbi Correlation of 18F-FLT and 18F-FDG uptake on PET with Ki-67 immunohistochemistry in non-small cell lung cancer
    Yuka Yamamoto
    Department of Radiology, Faculty of Medicine, Kagawa University, 1750 1 Ikenobe, Miki cho, Kita gun, Kagawa 761 0793, Japan
    Eur J Nucl Med Mol Imaging 34:1610-6. 2007
    ..We prospectively evaluated whether FLT uptake reflects proliferative activity as indicated by the Ki-67 index in non-small cell lung cancer (NSCLC), in comparison with 2-deoxy-2-(18)F-fluoro-D-glucose (FDG)...
  12. ncbi Randomized, double-blind, placebo-matched, multicenter trial of abacavir/lamivudine or tenofovir/emtricitabine with lopinavir/ritonavir for initial HIV treatment
    Kimberly Y Smith
    Rush University Medical Center, Chicago, Illinois 60612, USA
    AIDS 23:1547-56. 2009
    ..This is the first completed, randomized clinical trial to directly compare the efficacy, safety, and tolerability of these agents, each in combination with lopinavir/ritonavir in antiretroviral-naive patients...
  13. ncbi 3-deoxy-3-[(18)F]fluorothymidine-positron emission tomography for noninvasive assessment of proliferation in pulmonary nodules
    Andreas K Buck
    Department of Nuclear Medicine, Universit of Ulm, Germany
    Cancer Res 62:3331-4. 2002
    ..0001; r = 0.87). FLT uptake was specific for malignant lesions and may be used for differential diagnosis of SPNs, assessment of proliferation, and estimation of prognosis...
  14. pmc Abacavir-lamivudine versus tenofovir-emtricitabine for initial HIV-1 therapy
    Paul E Sax
    Division of Infectious Diseases and the Department of Medicine, Brigham and Women s Hospital and Harvard Medical School, Boston, MA 02115, USA
    N Engl J Med 361:2230-40. 2009
    ....
  15. ncbi In vivo validation of 3'deoxy-3'-[(18)F]fluorothymidine ([(18)F]FLT) as a proliferation imaging tracer in humans: correlation of [(18)F]FLT uptake by positron emission tomography with Ki-67 immunohistochemistry and flow cytometry in human lung tumors
    Hubert Vesselle
    Department of Radiology, Division of Nuclear Medicine, University of Washington, Seattle, Washington 98195, USA
    Clin Cancer Res 8:3315-23. 2002
    ....
  16. ncbi [(18)F]FLT: an imaging biomarker of tumour proliferation for assessment of tumour response to treatment
    DMITRY SOLOVIEV
    Cancer Research UK, Cambridge Research Institute, Cambridge CB2 0RE, UK
    Eur J Cancer 48:416-24. 2012
    ..Nevertheless FLT-PET could potentially be used as a negative predictor of tumour response to chemotherapy, and hence evaluation of this IB is granted in multi-centre clinical trials...
  17. ncbi 3'-deoxy-3'-[18F]fluorothymidine as a new marker for monitoring tumor response to antiproliferative therapy in vivo with positron emission tomography
    Henryk Barthel
    Cancer Research United Kingdom PET Oncology Group, Department of Cancer Medicine, Faculty of Medicine, Imperial College of Science, Technology and Medicine, Hammersmith Hospital Campus, London W12 0NN, United Kingdom
    Cancer Res 63:3791-8. 2003
    ..The decrease in [(18)F]FLT uptake after 5-FU was more pronounced than that of [(18)F]FDG. [(18)F]FLT is, therefore, a promising marker for monitoring antiproliferative drug activity in oncology that warrants additional testing...
  18. ncbi PET imaging with 18F-FLT and thymidine analogs: promise and pitfalls
    Anthony F Shields
    Karmanos Cancer Institute, Wayne State University School of Medicine, Detroit, Michigan, USA
    J Nucl Med 44:1432-4. 2003
  19. ncbi Early changes in [18F]FLT uptake after chemotherapy: an experimental study
    Helmut Dittmann
    Department of Nuclear Medicine, Eberhard Karls University, Roentgenweg 13, 72076 Tubingen, Germany
    Eur J Nucl Med Mol Imaging 29:1462-9. 2002
    ..By contrast, CDDP results in an early decline in FLT but not in FDG uptake. This drug-specific modulation of FLT uptake has to be taken into account in positron emission tomography studies using FLT for treatment monitoring...
  20. ncbi Abacavir-lamivudine-zidovudine vs indinavir-lamivudine-zidovudine in antiretroviral-naive HIV-infected adults: A randomized equivalence trial
    S Staszewski
    Klinikum der Johann Wolfgang Goethe Universitat, Zentrum der Inneren Medizin, Infektionsambulanz, Haus 68, Theodor Stern Kai 7, D 60596 Frankfurt, Germany
    JAMA 285:1155-63. 2001
    ..However, the role of abacavir in a triple nucleoside combination regimen has not been evaluated against a standard protease inhibitor-containing regimen for initial antiretroviral treatment...
  21. ncbi Increased platelet reactivity in HIV-1-infected patients receiving abacavir-containing antiretroviral therapy
    Claudette S Satchell
    HIV Molecular Research Group, School of Medicine and Medical Sciences, University College Dublin, Ireland
    J Infect Dis 204:1202-10. 2011
    ..Given the role of platelet aggregation in thrombus formation in MI and the reversible nature of the abacavir association, we hypothesized that patients treated with abacavir would have increased platelet reactivity...
  22. ncbi 3'-[18F]fluoro-3'-deoxythymidine ([18F]-FLT) as positron emission tomography tracer for imaging proliferation in a murine B-Cell lymphoma model and in the human disease
    Martin Wagner
    Department of Nuclear Medicine, University of Ulm, 89081 Ulm, Germany
    Cancer Res 63:2681-7. 2003
    ..These results suggest that [(18)F]-FLT represents a novel tracer for PET that enables imaging of proliferation in human lymphoma in vivo...
  23. pmc Early identification of antigen-specific immune responses in vivo by [18F]-labeled 3'-fluoro-3'-deoxy-thymidine ([18F]FLT) PET imaging
    Erik H J G Aarntzen
    Department of Tumor Immunology, Radboud University Nijmegen Medical Centre, 6500 HB, Nijmegen, The Netherlands
    Proc Natl Acad Sci U S A 108:18396-9. 2011
    ..This technique allows for early discrimination of responding from nonresponding patients in anti-cancer vaccination and aid physicians in individualized decisionmaking...
  24. ncbi Detection and grading of soft tissue sarcomas of the extremities with (18)F-3'-fluoro-3'-deoxy-L-thymidine
    David C P Cobben
    Department of Surgical Oncology, Groningen University Hospital, Groningen, The Netherlands
    Clin Cancer Res 10:1685-90. 2004
    ..The aim of the study was to investigate the feasibility of (18)F-3'-fluoro-3'-deoxy-L-thymidine positron emission tomography (FLT-PET) for the detection and grading of soft tissue sarcoma (STS)...
  25. ncbi Radiosynthesis of 3'-deoxy-3'-[(18)F]fluorothymidine: [(18)F]FLT for imaging of cellular proliferation in vivo
    J R Grierson
    Research Imaging Laboratory, University of Washington Medical Center, Seattle, Washington 98195, USA
    Nucl Med Biol 27:143-56. 2000
    ..18)F]FLT has been designed as a new positron emission tomography imaging agent for visualizing cellular proliferation in vivo based on the metabolism of thymidine...
  26. ncbi FLT: measuring tumor cell proliferation in vivo with positron emission tomography and 3'-deoxy-3'-[18F]fluorothymidine
    Alexander Salskov
    Division of Nuclear Medicine, Department of Radiology, University of Washington, Seattle, WA 98195, USA
    Semin Nucl Med 37:429-39. 2007
    ....
  27. ncbi Kinetics of 3'-deoxy-3'-18F-fluorothymidine during treatment monitoring of recurrent high-grade glioma
    Christiaan Schiepers
    Department of Molecular and Medical Pharmacology, David Geffen School of Medicine, University of California, Los Angeles, California 90095 6942, USA
    J Nucl Med 51:720-7. 2010
    ..3'-Deoxy-3'-(18)F-fluorothymidine ((18)F-FLT) is used as a biomarker of cell proliferation. We investigated the kinetics of (18)F-FLT during treatment of malignant glioma with bevacizumab and irinotecan...
  28. ncbi [18F]-3'Deoxy-3'-fluorothymidine positron emission tomography and breast cancer response to docetaxel
    Kaiyumars B Contractor
    Departments of Surgery and Cancer, Neuroscience, and Nuclear Medicine, Imperial College London and Imperial College Healthcare NHS Trust, Hammersmith and Charing Cross Hospitals, London, United Kingdom
    Clin Cancer Res 17:7664-72. 2011
    ..To establish biomarkers indicating clinical response to taxanes, we determined whether early changes in [(18)F]-3'deoxy-3'-fluorothymidine positron emission tomography (FLT-PET) can predict benefit from docetaxel therapy in breast cancer...
  29. ncbi [(18)F]FLT-PET imaging does not always "light up" proliferating tumor cells
    Cathy C Zhang
    Oncology Research Unit, La Jolla Laboratories, Pfizer Global Research and Development, San Diego, California 92121, USA
    Clin Cancer Res 18:1303-12. 2012
    ..The aim of this article was to validate the use of [(18)F]FLT-PET imaging for measuring xenograft proliferation and subsequent monitoring of targeted therapy...
  30. pmc Early detection of response to experimental chemotherapeutic Top216 with [18F]FLT and [18F]FDG PET in human ovary cancer xenografts in mice
    Mette Munk Jensen
    Cluster for Molecular Imaging, Faculty of Health Sciences, University of Copenhagen, Copenhagen, Denmark
    PLoS ONE 5:e12965. 2010
    ..To do so, we studied early anti-proliferative effects of the experimental chemotherapy Top216 non-invasively by PET...
  31. ncbi Kinetic analysis of 3'-deoxy-3'-18F-fluorothymidine in patients with gliomas
    Mark Muzi
    Department of Radiology, University of Washington, Seattle, Washington 98195 6004, USA
    J Nucl Med 47:1612-21. 2006
    ..Uptake may result from retention in the biosynthetic pathway or leakage via the disrupted blood-tumor barrier. Visual analysis or static measures of 18F-FLT uptake are problematic as transport and retention cannot be distinguished...
  32. ncbi Altered tissue 3'-deoxy-3'-[18F]fluorothymidine pharmacokinetics in human breast cancer following capecitabine treatment detected by positron emission tomography
    Laura M Kenny
    Department of Oncology, Imperial College London, London, United Kingdom
    Clin Cancer Res 15:6649-57. 2009
    ..In this study, we assessed for the first time the altered pharmacokinetics of FLT in patients following administration of capecitabine, a drug whose mode of action has been reported to include TS inhibition...
  33. ncbi In vivo biological activity of the histone deacetylase inhibitor LAQ824 is detectable with 3'-deoxy-3'-[18F]fluorothymidine positron emission tomography
    Julius Leyton
    Molecular Therapy and Cancer Cell Biology, Imperial College London, Faculty of Medicine, Hammersmith Hospital, Du Cane Road, London W12 0NN, United Kingdom
    Cancer Res 66:7621-9. 2006
    ..Drug-induced changes in tumor [18F]FLT uptake were due, at least in part, to reductions in TK1 transcription and translation...
  34. ncbi Kinetic analysis of 3'-deoxy-3'-fluorothymidine PET studies: validation studies in patients with lung cancer
    Mark Muzi
    Department of Radiology, University of Washington, Seattle, Washington 98195 6465, USA
    J Nucl Med 46:274-82. 2005
    ..Compartmental modeling results were compared with simple model-independent methods of estimating FLT uptake...
  35. ncbi Use of 3'-deoxy-3'-[18F]fluorothymidine PET to monitor early responses to radiation therapy in murine SCCVII tumors
    You Jung Yang
    Department of Nuclear Medicine, University of Ulsan College of Medicine, Asan Medical Center, 388 1 Pungnap 2Dong Songpa Gu, Seoul 138 736, South Korea
    Eur J Nucl Med Mol Imaging 33:412-9. 2006
    ..3'-Deoxy-3'-[(18)F]fluorothymidine (FLT) is a promising new radiopharmaceutical for imaging cell proliferation. We evaluated whether FLT PET can be used to monitor early responses to radiation treatment...
  36. ncbi Monitoring antiproliferative responses to kinase inhibitor therapy in mice with 3'-deoxy-3'-18F-fluorothymidine PET
    Christian Waldherr
    Department of Molecular and Medical Pharmacology, Ahmanson Biological Imaging Center, David Geffen School of Medicine, University of California at Los Angeles, 10833 Le Conte Ave, Los Angeles, CA 90095, USA
    J Nucl Med 46:114-20. 2005
    ..The aim of this study was to evaluate, whether PET with (18)F-FDG and 3'-deoxy-3'-(18)F-fluorothymidine ((18)F-FLT) may be used to monitor noninvasively the antiproliferative effects of tyrosine kinase inhibitors...
  37. ncbi A simplification trial switching from nucleoside reverse transcriptase inhibitors to once-daily fixed-dose abacavir/lamivudine or tenofovir/emtricitabine in HIV-1-infected patients with virological suppression
    Esteban Martinez
    Hospital Clinic Institut d Investigaciones Biomediques August Pi i Sunyer, University of Barcelona, 08036 Barcelona, Spain
    J Acquir Immune Defic Syndr 51:290-7. 2009
    ..We compared 48-week efficacy and safety of these combinations as substitutes of nucleosides in patients with virological suppression...
  38. ncbi [18F]FLT-PET in oncology: current status and opportunities
    Lukas B Been
    PET Center, Groningen University Hospital, Groningen, RB, The Netherlands
    Eur J Nucl Med Mol Imaging 31:1659-72. 2004
    ..The opportunities provided by, and the limitations of, [18F]FLT as a proliferation tracer are addressed in this review, and directions are given for further research, taking into account the strong and weak points of the new tracer...
  39. ncbi Imaging proliferation in lung tumors with PET: 18F-FLT versus 18F-FDG
    Andreas K Buck
    Department of Nuclear Medicine, University of Ulm, Ulm, Germany
    J Nucl Med 44:1426-31. 2003
    ..In this prospective study, we examined whether (18)F-FLT better determines proliferative activity in newly diagnosed lung nodules than does (18)F-FDG...
  40. pmc Imaging biomarkers predict response to anti-HER2 (ErbB2) therapy in preclinical models of breast cancer
    Chirayu Shah
    Vanderbilt University Institute of Imaging Science, Department of Radiology and Radiological Sciences, Vanderbilt University Medical Center, Nashville, Tennessee 37232, USA
    Clin Cancer Res 15:4712-21. 2009
    ..The correlation between tumor regression and molecular imaging of apoptosis, glucose metabolism, and cellular proliferation was evaluated longitudinally in responding and nonresponding tumor-bearing cohorts...
  41. pmc 3'-deoxy-3'-[18F]fluorothymidine positron emission tomography is a sensitive method for imaging the response of BRAF-dependent tumors to MEK inhibition
    David B Solit
    Department of Medicine, Memorial Sloan Kettering Cancer Center, New York, New York 10021, USA
    Cancer Res 67:11463-9. 2007
    ..The data suggest that [(18)F]FLT PET can effectively image induction of G(1) arrest by MEK inhibitors in mutant BRAF tumors and may be a useful noninvasive method for assessing the early biological response to this class of drugs...
  42. ncbi Evaluation of 3'-deoxy-3'-18F-fluorothymidine for monitoring tumor response to radiotherapy and photodynamic therapy in mice
    Masahiro Sugiyama
    Department of Radiology, Hamamatsu University School of Medicine, Hamamatsu, Japan
    J Nucl Med 45:1754-8. 2004
    ..3'-Deoxy-3'-18F-fluorothymidine (18F-FLT) has been suggested as a new PET tracer for imaging tumor proliferation. We investigated the use of 18F-FLT to monitor the response of tumors to radiotherapy and photodynamic therapy (PDT) in mice...
  43. pmc Early changes in inflammatory and pro-thrombotic biomarkers in patients initiating antiretroviral therapy with abacavir or tenofovir
    Sergio Padilla
    Infectious Diseases Unit, Hospital General Universitario de Elche, Department of Clinical Medicine, University Miguel Hernandez, Elche, Alicante, Spain
    BMC Infect Dis 11:40. 2011
    ..We evaluated longitudinal changes in pro-atherosclerotic biomarkers in patients initiating abacavir or tenofovir...
  44. ncbi Monitoring tumor cell proliferation by targeting DNA synthetic processes with thymidine and thymidine analogs
    Jeffrey L Schwartz
    Department of Radiation Oncology, University of Washington School of Medicine, Seattle, Washington 98195 6069, USA
    J Nucl Med 44:2027-32. 2003
    ..The goal of this study was to test this hypothesis and determine how well these tracers track changes in proliferation of tumor cells...
  45. ncbi Quantification of cellular proliferation in tumor and normal tissues of patients with breast cancer by [18F]fluorothymidine-positron emission tomography imaging: evaluation of analytical methods
    Laura M Kenny
    Molecular Therapy and PET Oncology Research Group, Hammersmith Hospital, London, UK
    Cancer Res 65:10104-12. 2005
    ..We conclude that [18F]FLT-positron emission tomography is a promising clinical tool for imaging cellular proliferation in breast cancer, and is most predictive when analyzed by graphical and spectral methods...
  46. ncbi Visualisation of neuroblastoma growth in a Scid mouse model using [18F]FDG and [18F]FLT-PET
    Nina Krieger-Hinck
    Department of Anatomy II Experimental Morphology, University Medical Center Hamburg Eppendorf, 20246 Hamburg, Germany
    Anticancer Res 26:3467-72. 2006
    ..Thus, the [18F]FDG and [18F]FLT uptake by human neuroblastomas grown in Scid mice are compared in this study...
  47. ncbi The uptake of 3'-deoxy-3'-[18F]fluorothymidine into L5178Y tumours in vivo is dependent on thymidine kinase 1 protein levels
    Henryk Barthel
    Molecular Therapy and PET Oncology Research Group, Faculty of Medicine, Imperial College London, Hammersmith Hospital Campus, Du Cane Road, London, W12 0NN, UK
    Eur J Nucl Med Mol Imaging 32:257-63. 2005
    ..The aim of this study was to investigate the role of thymidine kinase 1 (TK1) protein in 3'-deoxy-3'-[18F]fluorothymidine ([18F]FLT) positron emission tomography (PET) studies...
  48. ncbi Evaluation of thoracic tumors with 18F-fluorothymidine and 18F-fluorodeoxyglucose-positron emission tomography
    Cecelia S Yap
    Department of Molecular and Medical Pharmacology, Ahmanson Biological Imaging Center Nuclear Medicine, UCLA School of Medicine, AR 144 CHS, Los Angeles, CA 90095 6948, USA
    Chest 129:393-401. 2006
    ....
  49. pmc Abacavir increases platelet reactivity via competitive inhibition of soluble guanylyl cyclase
    Paul D Baum
    Division of Experimental Medicine, Department of Medicine bVeterans Affairs Medical Center, University of California San Francisco, San Francisco, California 94143 1234, USA
    AIDS 25:2243-8. 2011
    ..To provide a molecular mechanism that explains the association of the antiretroviral guanosine analogue, abacavir, with an increased risk of myocardial infarction...
  50. ncbi HLA-B*5701 screening for hypersensitivity to abacavir
    Simon Mallal
    Royal Perth Hospital and Murdoch University, Perth, Australia
    N Engl J Med 358:568-79. 2008
    ..This study was designed to establish the effectiveness of prospective HLA-B*5701 screening to prevent the hypersensitivity reaction to abacavir...
  51. ncbi Evaluation of 2-deoxy-2-[18F]fluoro-D-glucose- and 3'-deoxy-3'-[18F]fluorothymidine-positron emission tomography as biomarkers of therapy response in platinum-resistant ovarian cancer
    Meg Perumal
    Comprehensive Cancer Imaging Centre, Department of Cancer and Surgery, Faculty of Medicine, Imperial College London, Hammersmith Hospital, 240 MRC Cyclotron Building, Du Cane Road, London, W12 0NN, UK
    Mol Imaging Biol 14:753-61. 2012
    ..We evaluated whether 2-deoxy-2-[(18)F]fluoro-D-glucose ([(18)F]FDG) and 3'-deoxy-3'-[(18)F]fluorothymidine ([(18)F]FLT) positron emission tomography (PET) could be used as imaging biomarkers of platinum resensitization in ovarian cancer...
  52. ncbi Pharmacogenetic information derived from analysis of HLA alleles
    Hiroyuki Gatanaga
    AIDS Clinical Center, International Medical Center of Japan, 1 21 1 Toyama, Shinjuku ku, Tokyo 162 8655, Japan
    Pharmacogenomics 9:207-14. 2008
    ..HLA typing can stratify risk of hypersensitivity to certain drugs and allow personalized treatment, although the patients should be monitored closely even if they are negative for HLA alleles associated with hypersensitivity...
  53. ncbi Early prediction of nonprogression in advanced non-small-cell lung cancer treated with erlotinib by using [(18)F]fluorodeoxyglucose and [(18)F]fluorothymidine positron emission tomography
    Thomas Zander
    Department I of Internal Medicine, Center for Integrated Oncology Köln Bonn, University Hospital of Cologne, 50924 Cologne, Germany
    J Clin Oncol 29:1701-8. 2011
    ....
  54. pmc Imaging colon cancer response following treatment with AZD1152: a preclinical analysis of [18F]fluoro-2-deoxyglucose and 3'-deoxy-3'-[18F]fluorothymidine imaging
    Maxim A Moroz
    Department of Neurology, Memorial Sloan Kettering Cancer Center, New York, New York 10065, USA
    Clin Cancer Res 17:1099-110. 2011
    ....
  55. ncbi Abacavir and didanosine induce the interaction between human leukocytes and endothelial cells through Mac-1 upregulation
    Carmen de Pablo
    Departamento de Farmacología and CIBERehd, Universidad de Valencia, Spain
    AIDS 24:1259-66. 2010
    ..The objective of this study was to analyze the effects of clinically relevant doses of abacavir and didanosine on human leukocyte-endothelium interactions and to compare them with those of other NRTIs...
  56. pmc Evaluation of cardiovascular biomarkers in HIV-infected patients switching to abacavir or tenofovir based therapy
    Thomas A Rasmussen
    Department of Infectious Diseases, Aarhus University Hospital, Skejby, Denmark
    BMC Infect Dis 11:267. 2011
    ..Our objective was to evaluate and compare the effect of abacavir on levels of biomarkers associated with cardiovascular risk...
  57. ncbi Abacavir hypersensitivity reaction
    Ross G Hewitt
    Departments of Medicine and Pharmacy Practice, State University of New York, Buffalo, NY, 14215, USA
    Clin Infect Dis 34:1137-42. 2002
    ..Clinical management involves supportive measures and discontinuation of abacavir therapy. Rechallenge with abacavir in a hypersensitive patient should be avoided because it might precipitate a life-threatening reaction...
  58. pmc 3'-Azido-2',3'-dideoxynucleoside 5'-triphosphates inhibit telomerase activity in vitro, and the corresponding nucleosides cause telomere shortening in human HL60 cells
    Xiaohong Liu
    Biotechnology Research Center, Teikyo University of Science and Technology, Uenohara, Yamanashi, Japan
    Nucleic Acids Res 35:7140-9. 2007
    ..Southern hybridization analysis of genomic DNA prepared from cells cultured in the presence of AZddG and AZddAA revealed reproducible telomere shortening...
  59. ncbi [18F]3'-deoxy-3'-fluorothymidine PET for the diagnosis and grading of brain tumors
    Seung Jin Choi
    Department of Nuclear Medicine, Asan Medical Center, University of Ulsan College of Medicine, 388 1 Poongnap dong, Songpa Gu, Seoul, 138 736, Korea
    Eur J Nucl Med Mol Imaging 32:653-9. 2005
    ..The aim of this study was to evaluate the feasibility of using [(18)F] 3'-deoxy-3'-fluorothymidine (FLT) positron emission tomography (PET) for the diagnosis and grading of brain tumors...
  60. ncbi Correlation of 18F-FLT uptake with equilibrative nucleoside transporter-1 and thymidine kinase-1 expressions in gastrointestinal cancer
    Reiko Kameyama
    Department of Radiology, Faculty of Medicine, Kagawa University, Kagawa, Japan
    Nucl Med Commun 32:460-5. 2011
    ....
  61. ncbi Abacavir use and cardiovascular disease events: a meta-analysis of published and unpublished data
    Mario Cruciani
    Centre of Community Medicine and HIV Outpatient Clinic, Verona, Italy
    AIDS 25:1993-2004. 2011
    ..However, no excess risk of myocardial infarction (MI) with ABC therapy has been observed in individual randomized clinical trials (RCTs) and in the aggregated clinical trials database maintained by the manufacturer of ABC...
  62. ncbi 11C-methionine (MET) and 18F-fluorothymidine (FLT) PET in patients with newly diagnosed glioma
    Tetsuhiro Hatakeyama
    Department of Neurological Surgery, Kagawa University School of Medicine, 1750 1 Miki cho, Kita gun, Kagawa, 761 0793, Japan
    Eur J Nucl Med Mol Imaging 35:2009-17. 2008
    ....
  63. ncbi Noninvasive imaging of cell proliferation following mitogenic extracellular kinase inhibition by PD0325901
    Julius Leyton
    Molecular Therapy Group, Faculty of Medicine, Imperial College London, Hammersmith Hospital, Du Cane Road, London W12 ONN, United Kingdom
    Mol Cancer Ther 7:3112-21. 2008
    ..6; P > or = 0.003). In summary, [18F]FLT-PET is a sensitive imaging biomarker for detecting the antiproliferative effect of MEK1/2 inhibition by PD0325901...
  64. ncbi Evaluation of D-18F-FMT, 18F-FDG, L-11C-MET, and 18F-FLT for monitoring the response of tumors to radiotherapy in mice
    Chieko Murayama
    Department of Clinical Pharmacology, Tokai University School of Medicine, Isehara, Kanagawa, Japan
    J Nucl Med 50:290-5. 2009
    ....
  65. ncbi Abacavir use and risk of acute myocardial infarction and cerebrovascular events in the highly active antiretroviral therapy era
    Roger J Bedimo
    VA North Texas Health Care System, University of Texas Southwestern Medical Center, Dallas, Texas 75216, USA
    Clin Infect Dis 53:84-91. 2011
    ..Some studies have suggested that exposure to antiretroviral therapy (ART) with abacavir is associated with an increased risk of acute myocardial infarction (AMI)...
  66. ncbi Diverging substrate specificity of pure human thymidine kinases 1 and 2 against antiviral dideoxynucleosides
    B Munch-Petersen
    Department of Biochemistry I, Karolinska Institute, Stockholm, Sweden
    J Biol Chem 266:9032-8. 1991
    ..The much lower tolerance for modifications of the deoxyribose moiety of TK2 as compared to TK1 is important for the design of new antiviral nucleoside analogues intended for use in cells with different expression of TK1 and TK2...
  67. ncbi PET with [18F]fluorothymidine for imaging of primary breast cancer: a pilot study
    Brigitte Smyczek-Gargya
    Breast Clinic, Department of Gynecology and Obstetrics, University of Tubingen, 72076 Tubingen, Germany
    Eur J Nucl Med Mol Imaging 31:720-4. 2004
    ..03). FLT-PET is suitable for the diagnosis of primary breast cancer and locoregional metastases. High image contrast may facilitate the detection of small foci, especially in the mediastinum...
  68. pmc No risk of myocardial infarction associated with initial antiretroviral treatment containing abacavir: short and long-term results from ACTG A5001/ALLRT
    Heather J Ribaudo
    Center for Biostatistics in AIDS Research, Department of Biostatistics, Harvard School of Public Health, Boston, Massachusetts 02115, USA
    Clin Infect Dis 52:929-40. 2011
    ....
  69. ncbi Repeatability of metabolically active volume measurements with 18F-FDG and 18F-FLT PET in non-small cell lung cancer
    Virginie Frings
    Department of Nuclear Medicine and PET Research, VU University Medical Centre, Amsterdam, The Netherlands
    J Nucl Med 51:1870-7. 2010
    ....
  70. pmc Inflammatory biomarkers and abacavir use in the Women's Interagency HIV Study and the Multicenter AIDS Cohort Study
    Frank J Palella
    Division of Infectious Diseases, Northwestern University Feinberg School of Medicine, Chicago, Illinois 60611, USA
    AIDS 24:1657-65. 2010
    ..To assess associations between abacavir (ABC) use and systemic inflammation...
  71. ncbi Kinetic modeling of 3'-deoxy-3'-18F-fluorothymidine for quantitative cell proliferation imaging in subcutaneous tumor models in mice
    Su Jin Kim
    Department of Nuclear Medicine, College of Medicine, Seoul National University, Seoul, Korea
    J Nucl Med 49:2057-66. 2008
    ..The aim of this study was to establish a kinetic modeling analysis method for quantitative (18)F-FLT PET studies in subcutaneous tumor models in mice...
  72. ncbi Monitoring of therapy in androgen-dependent prostate tumor model by measuring tumor proliferation
    Nobuyuki Oyama
    Mallinckrodt Institute of Radiology, Washington University School of Medicine, Saint Louis, Missouri 63110, USA
    J Nucl Med 45:519-25. 2004
    ..This study was undertaken to determine whether (18)F-FLT is useful in the detection of prostate cancer as well as monitoring therapeutic effects in a human tumor model...
  73. ncbi Kinetic modeling of 3'-deoxy-3'-fluorothymidine in somatic tumors: mathematical studies
    Mark Muzi
    Department of Radiology, University of Washington, Seattle, Washington 98195 6465, USA
    J Nucl Med 46:371-80. 2005
    ..The model reflects the retention of FLT-monophosphate (FLTMP), which is generated by the phosphorylation of FLT by thymidine kinase 1 (TK1), the initial step in the exogenous pathway...
  74. ncbi (18)F-FDG and (18)F-FLT uptake early after cyclophosphamide and mTOR inhibition in an experimental lymphoma model
    Lieselot Brepoels
    Department of Nuclear Medicine, University Hospital Gasthuisberg Leuven, Leuven, Belgium
    J Nucl Med 50:1102-9. 2009
    ..A second objective of this study was to investigate whether (18)F-FDG and (18)F-FLT responses were comparable early after mammalian target of rapamycin (mTOR) inhibition, as an example of proliferation-targeting therapies...
  75. ncbi Early detection of chemoradioresponse in esophageal carcinoma by 3'-deoxy-3'-3H-fluorothymidine using preclinical tumor models
    Smith Apisarnthanarax
    Department of Radiation Oncology, The University of Texas M D Anderson Cancer Center, Houston, 77030, USA
    Clin Cancer Res 12:4590-7. 2006
    ..We assessed the ability of 3'-deoxy-3'-(18)F-fluorothymidine positron emission tomography (FLT-PET) to detect early changes in tumor proliferation after chemoradiotherapy in experimental models of esophageal carcinoma...
  76. ncbi Comparison of methodologies for the in vivo assessment of 18FLT utilisation in colorectal cancer
    D Visvikis
    Institute of Nuclear Medicine, Royal Free and University College Medical School, Middlesex Hospital, London, UK
    Eur J Nucl Med Mol Imaging 31:169-78. 2004
    ..The good correlation found between the SUVs (at 60 min) and Ki values supports the use of semi-quantitative indices to assess the proliferation rate of colorectal cancer lesions in vivo with 18FLT...
  77. ncbi Abacavir does not affect circulating levels of inflammatory or coagulopathic biomarkers in suppressed HIV: a randomized clinical trial
    Allison Martin
    National Centre in HIV Epidemiology and Clinical Research, University of New South Wales, Australia
    AIDS 24:2657-63. 2010
    ..7, P = 0.048) in ABC/3TC recipients compared with TDF/FTC in the STEAL study. The impact of ABC/3TC treatment on a range of CVD and inflammatory biomarkers was explored...
  78. ncbi 18F-FLT PET as a surrogate marker of drug efficacy during mTOR inhibition by everolimus in a preclinical cisplatin-resistant ovarian tumor model
    Nicolas Aide
    Bioticla Team, EA1772, IFR 146 ICORE, GRECAN, François Baclesse Cancer Centre and Caen University, Caen, France
    J Nucl Med 51:1559-64. 2010
    ....
  79. pmc Use of nucleoside reverse transcriptase inhibitors and risk of myocardial infarction in HIV-infected patients enrolled in the D:A:D study: a multi-cohort collaboration
    Caroline A Sabin
    Lancet 371:1417-26. 2008
    ..Our aim was to explore whether exposure to such drugs was associated with an excess risk of myocardial infarction in a large, prospective observational cohort of HIV-infected patients...
  80. pmc The antiretroviral nucleoside analogue Abacavir reduces cell growth and promotes differentiation of human medulloblastoma cells
    Alessandra Rossi
    Sbarro Institute for Cancer Research and Molecular Medicine, Center for Biotechnology, College of Science and Technology, Temple University, Philadelphia PA
    Int J Cancer 125:235-43. 2009
    ..Thus, using Abacavir, alone or in combination with current therapies, might be an effective therapeutic strategy for the treatment of medulloblastoma...
  81. ncbi Imaging of cell proliferation: status and prospects
    James R Bading
    Department of Radioimmunotherapy, City of Hope, Duarte, California, USA
    J Nucl Med 49:64S-80S. 2008
    ..Further work is needed to determine the optimal tracer(s) and timing of imaging after treatment...
  82. ncbi Comparison of 18F-FLT PET and 18F-FDG PET in esophageal cancer
    Henderik L van Westreenen
    Department of Surgical Oncology, University Medical Center, Groningen, The Netherlands
    J Nucl Med 46:400-4. 2005
    ..Furthermore, the correlation between 18F-FLT and 18F-FDG uptake and proliferation of the tumor was investigated...
  83. ncbi TRIZAL study: switching from successful HAART to Trizivir (abacavir-lamivudine-zidovudine combination tablet): 48 weeks efficacy, safety and adherence results
    C Katlama
    Hopital Pitie Salpetriere, Paris, France
    HIV Med 4:79-86. 2003
    ..To assess the antiviral efficacy, safety, and adherence in subjects who switched to Trizivir following long-term HIV-1 RNA suppression...
  84. ncbi Abacavir-based therapy does not affect biological mechanisms associated with cardiovascular dysfunction
    Esteban Martinez
    Infectious Diseases Unit, Hospital Clinic Institut d Investigacions Biomediques August Pi i Sunyer, University of Barcelona, C Villarroel 170, 08036 Barcelona, Spain
    AIDS 24:F1-9. 2010
    ..To assess the effects of initiating abacavir-containing therapy on plasma lipids and cardiovascular biomarkers...
  85. ncbi A randomized trial of simplified maintenance therapy with abacavir, lamivudine, and zidovudine in human immunodeficiency virus infection
    Milos Opravil
    Division of Infectious Diseases, University Hospital, CH 8091 Zurich, Switzerland
    J Infect Dis 185:1251-60. 2002
    ....
  86. ncbi Evaluation of primary brain tumors with FLT-PET: usefulness and limitations
    Tsuneo Saga
    Department of Diagnostic Imaging and Nuclear Medicine, Graduate School of Medicine, Kyoto University, Kyoto, Japan
    Clin Nucl Med 31:774-80. 2006
    ..The purpose of this report was to investigate the potential of positron emission tomography using F-18 fluorodeoxythymidine (FLT-PET) in evaluating primary brain tumors...
  87. pmc The K65R mutation in human immunodeficiency virus type 1 reverse transcriptase exhibits bidirectional phenotypic antagonism with thymidine analog mutations
    Urvi M Parikh
    Division of Infectious Diseases, Department of Medicine, University of Pittsburgh School of Medicine, Pittsburgh, PA 15261, USA
    J Virol 80:4971-7. 2006
    ....
  88. pmc Analysis and reproducibility of 3'-Deoxy-3'-[18F]fluorothymidine positron emission tomography imaging in patients with non-small cell lung cancer
    Anthony F Shields
    Department of Internal Medicine, Wayne State University, Detroit, Michigan 48201 2013, USA
    Clin Cancer Res 14:4463-8. 2008
    ..This study assessed the methods to measure FLT retention in patients with non-small cell lung cancer (NSCLC) to measure the reproducibility of this approach...
  89. pmc Synthesis and evaluation of 3'-azido-2',3'-dideoxypurine nucleosides as inhibitors of human immunodeficiency virus
    Hong Wang Zhang
    Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Veterans Affairs Medical Center, Atlanta, GA 30033, USA
    Bioorg Med Chem Lett 20:60-4. 2010
    ..Among the synthesized compounds, several show potent and selective anti-HIV activity in primary lymphocytes...
  90. ncbi Early nucleoside reverse transcriptase inhibitors for the treatment of HIV: a brief history of stavudine (D4T) and its comparison with other dideoxynucleosides
    John C Martin
    Gilead Sciences, Inc, 333 Lakeside Drive, Foster City, CA 94404, United States
    Antiviral Res 85:34-8. 2010
    ..It has only recently been supplanted by better-tolerated treatments. This article forms part of a special issue of Antiviral Research marking the 25th anniversary of antiretroviral drug discovery and development, vol. 85, issue 1, 2010...
  91. ncbi [18F]FLT PET for diagnosis and staging of thoracic tumours
    Helmut Dittmann
    Department of Nuclear Medicine, Eberhard Karls University Tubingen, Tubingen, Germany
    Eur J Nucl Med Mol Imaging 30:1407-12. 2003
    ..In the liver and the bone marrow, high physiological FLT uptake hampers detection of metastases. On the other hand, FLT may be favourable for imaging of brain metastases owing to the low physiological uptake...
  92. ncbi Potential impact of [18F]3'-deoxy-3'-fluorothymidine versus [18F]fluoro-2-deoxy-D-glucose in positron emission tomography for colorectal cancer
    D L Francis
    Institute of Nuclear Medicine, Royal Free and University College Medical School, Middlesex Hospital, Mortimer Street, W1T 3AA, London, UK
    Eur J Nucl Med Mol Imaging 30:988-94. 2003
    ..We have demonstrated that (18)FDG and (18)FLT image two distinct processes. The prognostic implications of the uptake of (18)FLT need to be assessed in terms of response to chemoradiotherapy and survival...
  93. ncbi Two-dimensional LC-MS/MS determination of antiretroviral drugs in rat serum and urine
    R Nageswara Rao
    Analytical Chemistry Division, Discovery Laboratory, Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500 007, India
    J Pharm Biomed Anal 50:994-9. 2009
    ..7 ng ml(-1). The calibration graphs were linear in the range of 4-50 ng ml(-1)for abacavir, nevirapine and indinavir. The method was successfully applied to study the pharmacokinetics of antiretroviral in rats...
  94. ncbi Detection of colorectal cancer using ¹⁸F-FLT PET: comparison with ¹⁸F-FDG PET
    Yuka Yamamoto
    Department of Radiology, Kagawa University, Kagawa, Japan
    Nucl Med Commun 30:841-5. 2009
    ....
  95. ncbi 18F-FLT and 18F-FDG PET to measure response to radiotherapy combined with celecoxib in two colorectal xenograft models
    Annelies Debucquoy
    Lab of Experimental Radiotherapy, Department of Radiation Oncology and Experimental Therapy, University Hospitals Gasthuisberg, Herestraat 49, 3000 Leuven, Belgium
    Int J Radiat Biol 85:763-71. 2009
    ..To determine the dependence of celecoxib on the tumour micro-environment in vitro and in vivo and to compare the use of (18)F-Fluorodeoxyglucose ((18)F-FDG) and (18)F- 3'-deoxy-3-fluorothymidine ((18)F-FLT) to measure tumour response...
  96. ncbi Molecular basis of antagonism between K70E and K65R tenofovir-associated mutations in HIV-1 reverse transcriptase
    R M Kagan
    Department of Infectious Diseases, Quest Diagnostics Nichols Institute, San Juan Capistrano, CA 92675, United States
    Antiviral Res 75:210-8. 2007
    ..The net effect of the atomic-level changes in the double mutant may be to destabilize the pyrophosphate leaving group of the ligand, more severely affecting the catalytic rate of the polymerization reaction than the R65 single mutation...
  97. ncbi The role of 18F-FLT in cancer imaging: does it really reflect proliferation?
    Antonia Dimitrakopoulou-Strauss
    Eur J Nucl Med Mol Imaging 35:523-6. 2008
  98. ncbi Detection of gastric cancer using 18F-FLT PET: comparison with 18F-FDG PET
    Reiko Kameyama
    Department of Radiology, Faculty of Medicine, Kagawa University, 1750 1 Ikenobe, Miki cho, Kita gun, Kagawa 761 0793, Japan
    Eur J Nucl Med Mol Imaging 36:382-8. 2009
    ....
  99. ncbi New telluride-mediated elimination for novel synthesis of 2',3'-didehydro-2',3'-dideoxynucleosides
    Jia Sheng
    Department of Chemistry, Georgia State University, Atlanta, GA 30303, USA
    J Org Chem 73:3725-9. 2008
    Several 2',3'-dideoxynucleosides (ddNs) and 2',3'-didehydro-2',3'-dideoxynucleosides (d4Ns) are FDA-approved anti-HIV drugs...
  100. ncbi Determination of abacavir, amprenavir, didanosine, efavirenz, nevirapine, and stavudine concentration in human plasma by MALDI-TOF/TOF
    Stefania Notari
    Istituto Nazionale per le Malattie Infettive IRCCS Lazzaro Spallanzani, Via Portuense 292, I 00149 Roma, Italy
    J Chromatogr B Analyt Technol Biomed Life Sci 863:249-57. 2008
    ..00 x 10(-2)-1.00 pmol/microL. The limit of quantification value was 1.00 x 10(-2)pmol/microL for abacavir, amprenavir, didanosine, efavirenz, nevirapine, and stavudine...

Research Grants62

  1. NUCLEOSIDES WITH DUAL ANTI-HIV AND HBV ACTIVITY
    RAYMOND SCHINAZI; Fiscal Year: 2009
    ..immunodeficiency virus (HIV), led to the discovery that certain 2',3'- didehydro-2',3'-dideoxynucleosides (d4N) and their 2'-fluoro analogs are effective antiviral agents...
  2. PHARMACOLOGY OF DIDEOXYNUCLEOSIDES IN SMALL INTESTINAL
    JESSIE AU; Fiscal Year: 1991
    2',3'-Dideoxynucleosides (ddNS) have antiviral and cytostatic activities. ddNS are structural analogs and can be competitive inhibition or feedback regulation affect the metabolism and utilization of normal endogenous substrates...
  3. NEW STRATEGIES FOR GLYCOCONJUGATE SYNTHESIS FROM ALKYNES
    Frank McDonald; Fiscal Year: 1999
    ..enol ethers (glycals) and specific application of this chemistry to anti- AIDS nucleosides such as dideoxynucleosides, the antineoplastic compound puromycin, and antifungal compounds such as polyoxin and amipurimycin...
  4. NEW PHENYL NUCLEOSIDES AS ANTI-HIV AGENTS
    Shashikant Phadtare; Fiscal Year: 2003
    ..Although these nucleoside analogues, dideoxynucleosides and their carbocyclic analogs, offer great promise for the inhibition of viral replication, several ..
  5. MULTIFUNCTIONAL PHOSPHONOFORMATE PRODRUGS AGAINST HIV 1
    Andre Rosowsky; Fiscal Year: 1993
    ..both projects, can be divided into two broad areas based on our currently ongoing work: (1) antiretroviral dideoxynucleosides (ddN's) in which the heterocycle or the sugar is modified; and (2) -novel lipophilic esters of the ..
  6. FETAL TOXICITY OF ZIDOVUDINE
    Jashvant Unadkat; Fiscal Year: 1993
    ..In addition, the execution of the proposed studies will result in the development of an animal model to test the fetal toxicity of future anti-HIV drugs, in particular the newer dideoxynucleosides.
  7. BIOCHEMICAL MODULATION OF ANTI-HIV DIDEOXYNUCLEOSIDES
    Arnold Fridland; Fiscal Year: 1993
    ..These studies may reveal whether the active dinucleotide derivative of tiazofurin or selenazofurin may act as inhibitor of DNA repair synthesis in cells...
  8. POTENTIATION OF ANTI-VIRAL NUCLEOSIDE ACTIVITY
    Thomas Chan; Fiscal Year: 1991
    ..for activity against the HIV, and the ones that have been found effective in vitro are all members of the dideoxynucleosides. It has recently come to the attention of researchers that the intracellular anabolism of these nucleosides ..
  9. Boronated L-nucleotides targeted against HIV
    Barbara Shaw; Fiscal Year: 2005
    ..alpha-P-borano) analogs of potent viral replication inhibitors, including D- and L-enantiomers of 2',3'-dideoxynucleosides (2',3'-ddN), 2',3'-dideoxy- 2',3'-didehydrothymidine (d4T), 2'-deoxy-3'-thiacytidine triphosphate (3TC), and ..
  10. CARRIERS FOR MEMBRANE TRANSPORT OF AIDS-TARGETED DRUGS
    Julius Rebek; Fiscal Year: 1992
    ..2',3'-Dideoxynucleosides like 3'-azido-2',3'- dideoxythimidine (AZT) are efficient substrate inhibitors of HIV reverse transcriptase, ..
  11. NUCLEOTIDE METABOLISM IN LYMPHOCYTES AND MACROPHAGES
    Dennis Carson; Fiscal Year: 1991
    ..in deoxynuclootide pool kinetics can affect the metabolism, toxicity, and potential anti-HIV activity of dideoxynucleosides. The results of these studies should provide a rational basis for the further pharmacologic evaluation of ..
  12. Labeled Thymidine -- Development as A PET Imaging Agent
    Anthony Shields; Fiscal Year: 2008
    ..Our ultimate goal is to demonstrate that this approach is useful in evaluating both experimental and routine clinical treatment. ..
  13. PET IMAGING OF DRUG KINETICS AND PATHWAYS
    Anthony Shields; Fiscal Year: 2002
    ..Our proposed study of [F-18]FAU with PET will provide information on the biodistribution of this new therapeutic agent and may provide a way to image tumor TS activity and proliferation. ..
  14. COLUMBIA-ADARC-CORNELL AIDS CLINICAL TRIALS UNIT
    Scott Hammer; Fiscal Year: 2006
    ..Thus, the Columbia-ADARC ACTU will be an active participant in the Group's mission to improve the health of HIV infected individuals and set standards for treatment of HIV disease. ..
  15. Uridine Supplementation for HIV lipoatrophy
    Grace McComsey; Fiscal Year: 2007
    ..On-study subjects will continue to be followed per study protocol for a total of 12 months. The last 6 months of the grant will be dedicated to processing of samples and analysis of all data. [unreadable] [unreadable]..
  16. Imaging Thymidine Uptake During Treatment for Head and Neck Cancer
    Yusuf Menda; Fiscal Year: 2008
    ..The studies proposed here will refine and characterize a non-invasive imaging test that may allow treatment responses to be determined shortly after treatment has begun. [unreadable] [unreadable] [unreadable]..
  17. Mitochondrial Function and HIV Lipoatrophy
    Cecilia Shikuma; Fiscal Year: 2005
    ..Obtained ATP levels will be correlated with level of adipocyte apoptosis as well as with adipocyte mtDNA copies/cell by real-time PCR and SC adipose tissue expression of select oxidative phosphorylation (OXPHOS) genes. ..
  18. Metabolic Consequences of Thymidine Sparing Regimens
    Grace A McComsey; Fiscal Year: 2010
    ..at the top of each printed page and each continuation page. RESEARCH GRANT TABLE OF CONTENTS Page Numbers Face Page 1 Description, ..
  19. Early Prediction of Pathological Response of Chemoradiotherapy with FLT PET
    KS CLIFFORD CHAO; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  20. FLT PET to Plan the Best Therapy for Lung Cancer
    Hubert Vesselle; Fiscal Year: 2008
    ..At the conclusion of this study, the insight gained in the response of stage III NSCLCs will allow clinicians to plan the best therapy for these patients. [unreadable] [unreadable]..
  21. HIV-1 adaptation to HLA-restricted immune responses
    Simon Mallal; Fiscal Year: 2008
    ..The results will be used to determine how well the immune responses induced by a given vaccine would recognise diverse, variably HLA-adapted HIV-1 strains at those epitopes most critical for the prevalent HLA types of the study cohort. ..
  22. HAWAII ACTU - ADULT THERAPEUTIC CLINICAL TRIALS PROGRAM
    Cecilia Shikuma; Fiscal Year: 2008
    ..abstract_text> ..
  23. Role of macrophages in HIV Lipoatrophy
    Cecilia M Shikuma; Fiscal Year: 2010
    ..We are particularly well suited to undertake these studies as our research team combines clinical research expertise in HIV lipoatrophy with specific laboratory competency in adipose tissue-, mitochondrial- and M/MO-related research. ..
  24. Lung Cancer Prognosis: FLT PET and DNA Hypermethylation
    Hubert Vesselle; Fiscal Year: 2009
    ..This prognostic information will permit individualization and optimization of therapy for the 41,000 early stage NSCLC patients undergoing surgical resection each year in the United States. ..
  25. Role of Mitochondria in HIV Lipoatrophy
    Grace McComsey; Fiscal Year: 2009
    ..abstract_text> ..
  26. Toxoplasma Adenosine Kinase & Chemotherapy
    MAHMOUD EL KOUNI; Fiscal Year: 2007
    ..Determine the mechanism of selective toxicity of active compounds. These studies will utilize the complementary strengths of the investigators in a collaborative, integrated effort to achieve these goals. [unreadable] [unreadable]..
  27. THE BIOLOGY OF LUNG CANCER-- FDG AND FLUOROTHYMIDINE PET
    Hubert Vesselle; Fiscal Year: 2004
    ..By performing a biologic grading of resectable NSCLC with FDG PET, we will predict which patients will have a worse outcome. This information will allow individualized therapy. ..
  28. HYPOXIC IMAGING GUIDED INTENSITY MODULATED RADIOTHERAPY
    KS CLIFFORD CHAO; Fiscal Year: 2003
    ..They will test the hypothesis by performing multiple Cu-60 ATSM PET scans during the course of irradiation to understand the spatial evolution of hypoxic tumor. ..
  29. Enhancement of 5-Fluorouracil Chemotherapeutic Efficacy
    MAHMOUD EL KOUNI; Fiscal Year: 2002
    ..This will increase the use of FUra and enhance its commercial potential. Two patents have been awarded to protect the technology and were licensed to the Company. ..
  30. ADENOSINE KINASE TARGET FOR CHEMOTHERAPY IN TGONDII
    MAHMOUD EL KOUNI; Fiscal Year: 2001
    ..gondii; (3) evaluate active compounds as potential antitoxoplasmosis agents in vitro and in vivo. ..
  31. DNA Sequencing with Reversible dNTP and Cleavable Fluorescent ddNTPTerminators
    Jingyue Ju; Fiscal Year: 2009
    ..We anticipate that up to 100 bp of continuous sequences will be produced by this approach, which can be used to pursue a variety of biomedical research projects. ..
  32. MOLECULAR STAGING AND SCREENING OF LUNG CANCER
    Steven Ahrendt; Fiscal Year: 2002
    ..Completion of the proposed mentored training period will provide the candidate with an excellent foundation for pursuing his long-term goals in academic surgical oncology. ..
  33. AIDS CLINICAL TRIALS UNIT
    Pablo Tebas; Fiscal Year: 2007
    ..The investigators have credentials in basic and patient-oriented clinical research. ..
  34. DIMERIZATION INHIBITORS OF HIV-1 PROTEASE AND INTEGRASE
    Jean Chmielewski; Fiscal Year: 2003
    ..complex? Integrase Inhibition How general is the approach developed for dimerization inhibition of HIV protease, can it be applied to the inhibition of a structurally different protein such as HIV integrase? ..
  35. 3'-O-Modified Nucleotide Reversible Terminators for Pyrosequencing
    Jingyue Ju; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable] [unreadable]..
  36. Genomic Approaches to Neuronal Diversity and Plasticity
    Jingyue Ju; Fiscal Year: 2007
    ..RESEARCH GRANT TABLE OF CONTENTS Page Numbers Face Page .................................................................................................................................................. 1 Description, ..
  37. Positron Emission Tomography in Prostate Cancer
    Farrokh Dehdashti; Fiscal Year: 2008
    ..PET may also contribute significant prognostic information that may affect the decision to administer early adjuvant therapy to delay or prevent recurrence. [unreadable] [unreadable]..
  38. Universal Technology for Profiling the Dynamics of Normal & Oncogenic Signaling
    Karen Anderson; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable] [unreadable]..
  39. HIV-1 THERAPEUTICS AND DRUG RESISTANCE
    Daniel R Kuritzkes; Fiscal Year: 2010
    ..This research program provides a framework within which the applicant can mentor beginning clinical investigators in patient-oriented research focused on critical issues in HIV-1 medicine. ..
  40. Use of Radiation in Stage IV Non-Small Cell Lung Cancer
    James Hayman; Fiscal Year: 2003
    ..Lastly, we plan to examine whether the frequency and intensity of the administration of treatment with palliative radiation in this patient population has changed over time. ..
  41. Novel Drug Development for Prostatic Cancer
    Saeed Khan; Fiscal Year: 2006
    ..These studies will serve to identify the best candidate prodrug that will be subsequently tested in clinical trials as treatment for metastatic prostate cancer. ..
  42. Purine Analog Anti-Mycobacterial Drug Development
    William Parker; Fiscal Year: 2009
    ..tb activity;and (4) design and synthesis of purine and purine nucleoside analogs with selective activity against M. tb. ..
  43. MECHANISTIC STUDIES ON PEP UTILIZING ENZYMES
    Karen Anderson; Fiscal Year: 2003
    ..In addition as the investigator develops the quantitative aspects of the rapid mixing, pulsed-flow ESI-MS technique further, she will extend the studies of these enzymes to determine the full kinetic profile. ..
  44. HCV Treatment Cost-Effectiveness in 3 IDU Populations
    BRUCE SCHACKMAN; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable] [unreadable]..
  45. MOLECULAR EFFECTORS OF ENZYMATIC SYNTHESIS OF DNA
    MUKUND MODAK; Fiscal Year: 2003
    ..The molecular mechanism and functional anatomy of DNA polymerase clarified in this manner will lead to a better understanding of DNA replication, DNA repair and mutagenic effects of chemicals and carcinogenesis. ..
  46. Polymorphism of Multi-Drug-Resistance Protein-1
    RODNEY HO; Fiscal Year: 2005
    ....
  47. Drug susceptibility assay for non-subtypr B HIV-1
    Neil Parkin; Fiscal Year: 2006
    ....
  48. Understanding and Altering the Virologic Setpoint
    Martin Markowitz; Fiscal Year: 2006
    ..abstract_text> ..
  49. AFP-Based Immunotherapy for Hepatocellular Carcinoma
    Antoni Ribas; Fiscal Year: 2006
    ..In summary, I propose a clinically-oriented research program that translates this original work into novel, evidence-based immnunotherapy trials for hepatocellular carcinoma. ..
  50. Novel HIV-1 Microbicides
    Bharat Ramratnam; Fiscal Year: 2006
    ..The full realization of this potential will come from more extended experiments involving vaginal/rectal virus challenge in CCR5 siRNA treated macaques and appropriate controls. ..
  51. NOVEL APPROACHES TO TARGET LATENT RESERVOIRS OF HIV-1
    Bharat Ramratnam; Fiscal Year: 2004
    ..The goal of this proposal will be to design and implement novel immunologic and pharmacologic interventions and characterize their effect on viral burden during prolonged anti-retroviral therapy. ..
  52. A Molecular Approach For Opportunistic HIV-1 Infections
    Karen Anderson; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  53. Studies of DNA Pol I and Pol E2 of M. tuberculosis
    MUKUND MODAK; Fiscal Year: 2007
    ..unreadable] [unreadable]..
  54. Modulating Nucleotide Size in DNA for Detection by Nanopore
    Jingyue Ju; Fiscal Year: 2007
    ..The molecular tools developed here will facilitate achieving the long-term goal of single molecule sequencing by nanopores at single base resolution. [unreadable] [unreadable]..
  55. HIV-Related Proteinuria and Endothelial Dysfunction
    Samir Gupta; Fiscal Year: 2007
    ..Dub6) in the fields of HIV metabolic and renal complications, renal vascular and glomerular pathology, and clinical trials design and implementation. ..
  56. PET Evaluation of Hemorrhagic Shock and Resuscitation
    Vibhudutta Awasthi; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  57. HIV-1 resistance to nucleoside analogues
    Daniel Kuritzkes; Fiscal Year: 2004
    ..Better understanding of the virologic, genetic, and biochemical aspects of AZT/3TC dual resistance will help direct therapy and may lead to better therapeutic strategies in the future. ..
  58. DIOXOLANE NUCLEOSIDES AS ANTIVIRAL AGENTS
    Jinfa Du; Fiscal Year: 2003
    ..In Phase II, we will apply our best methodology for large-scale synthesis of D-FDOC as well as the most promising new dioxolane nucleoside for further development towards an IND application. ..
  59. An Integrated System for DNA Sequencing by Synthesis
    Jingyue Ju; Fiscal Year: 2009
    ..This new system for genome sequencing and resequencing will have wide applications in biology and biomedical research. ..