benzamides

Summary

Summary: BENZOIC ACID amides.

Top Publications

  1. ncbi Five-year follow-up of patients receiving imatinib for chronic myeloid leukemia
    Brian J Druker
    Oregon Health and Science University Cancer Institute, L592, 3181 SW Sam Jackson Park Rd, Portland, OR 97239, USA
    N Engl J Med 355:2408-17. 2006
  2. 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
  3. ncbi One vs three years of adjuvant imatinib for operable gastrointestinal stromal tumor: a randomized trial
    Heikki Joensuu
    Department of Oncology, Helsinki University Central Hospital, Haartmaninkatu 4, PO Box 180, FIN 00029 Helsinki, Finland
    JAMA 307:1265-72. 2012
  4. 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
  5. pmc BRAF mutation predicts sensitivity to MEK inhibition
    David B Solit
    Department of Medicine, Memorial Sloan Kettering Cancer Center, 1275 York Avenue, New York, New York 10021, USA
    Nature 439:358-62. 2006
  6. ncbi Discontinuation of imatinib in patients with chronic myeloid leukaemia who have maintained complete molecular remission for at least 2 years: the prospective, multicentre Stop Imatinib (STIM) trial
    Francois Xavier Mahon
    Laboratoire d Hématologie et Service des Maladies du Sang, Centre Hospitalier Universitaire de Bordeaux, Bordeaux, France
    Lancet Oncol 11:1029-35. 2010
  7. 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
  8. pmc 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
  9. ncbi Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL
    Hagop Kantarjian
    Department of Leukemia, University of Texas M D Anderson Cancer Center, Houston, TX 77230 1402, USA
    N Engl J Med 354:2542-51. 2006
  10. ncbi Protein kinases--the major drug targets of the twenty-first century?
    Philip Cohen
    Medical Research Council, Protein Phosphorylation Unit, School of Life Sciences, University of Dundee, Dundee DD1 5EH, Scotland, UK
    Nat Rev Drug Discov 1:309-15. 2002

Research Grants

Detail Information

Publications316 found, 100 shown here

  1. ncbi Five-year follow-up of patients receiving imatinib for chronic myeloid leukemia
    Brian J Druker
    Oregon Health and Science University Cancer Institute, L592, 3181 SW Sam Jackson Park Rd, Portland, OR 97239, USA
    N Engl J Med 355:2408-17. 2006
    ..Imatinib inhibits this kinase, and in a short-term study was superior to interferon alfa plus cytarabine for newly diagnosed CML in the chronic phase. For 5 years, we followed patients with CML who received imatinib as initial therapy...
  2. 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...
  3. ncbi One vs three years of adjuvant imatinib for operable gastrointestinal stromal tumor: a randomized trial
    Heikki Joensuu
    Department of Oncology, Helsinki University Central Hospital, Haartmaninkatu 4, PO Box 180, FIN 00029 Helsinki, Finland
    JAMA 307:1265-72. 2012
    ..Adjuvant imatinib administered for 12 months after surgery has improved recurrence-free survival (RFS) of patients with operable gastrointestinal stromal tumor (GIST) compared with placebo...
  4. 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...
  5. pmc BRAF mutation predicts sensitivity to MEK inhibition
    David B Solit
    Department of Medicine, Memorial Sloan Kettering Cancer Center, 1275 York Avenue, New York, New York 10021, USA
    Nature 439:358-62. 2006
    ..These data suggest an exquisite dependency on MEK activity in BRAF mutant tumours, and offer a rational therapeutic strategy for this genetically defined tumour subtype...
  6. ncbi Discontinuation of imatinib in patients with chronic myeloid leukaemia who have maintained complete molecular remission for at least 2 years: the prospective, multicentre Stop Imatinib (STIM) trial
    Francois Xavier Mahon
    Laboratoire d Hématologie et Service des Maladies du Sang, Centre Hospitalier Universitaire de Bordeaux, Bordeaux, France
    Lancet Oncol 11:1029-35. 2010
    ..We aimed to assess whether imatinib can be discontinued without occurrence of molecular relapse in patients in complete molecular remission (CMR) while on imatinib...
  7. 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...
  8. pmc 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...
  9. ncbi Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL
    Hagop Kantarjian
    Department of Leukemia, University of Texas M D Anderson Cancer Center, Houston, TX 77230 1402, USA
    N Engl J Med 354:2542-51. 2006
    ..Preclinical in vitro studies have shown that nilotinib (AMN107), a new BCR-ABL tyrosine kinase inhibitor, is more potent than imatinib against CML cells by a factor of 20 to 50...
  10. ncbi Protein kinases--the major drug targets of the twenty-first century?
    Philip Cohen
    Medical Research Council, Protein Phosphorylation Unit, School of Life Sciences, University of Dundee, Dundee DD1 5EH, Scotland, UK
    Nat Rev Drug Discov 1:309-15. 2002
    ..Protein kinases have now become the second most important group of drug targets, after G-protein-coupled receptors. Here, I give a personal view of some of the most important advances that have shaped this field...
  11. ncbi Roflumilast in symptomatic chronic obstructive pulmonary disease: two randomised clinical trials
    Peter M A Calverley
    School of Clinical Sciences, Liverpool, UK
    Lancet 374:685-94. 2009
    ..We therefore investigated whether roflumilast would reduce the frequency of exacerbations requiring corticosteroids in patients with COPD...
  12. pmc Human chronic myeloid leukemia stem cells are insensitive to imatinib despite inhibition of BCR-ABL activity
    Amie S Corbin
    Division of Hematology and Medical Oncology, Oregon Health and Science University Cancer Institute, Portland, Oregon, USA
    J Clin Invest 121:396-409. 2011
    ..Our findings suggest that primitive CML cells are not oncogene addicted and that therapies that biochemically target BCR-ABL will not eliminate CML stem cells...
  13. ncbi Chronic myeloid leukemia: an update of concepts and management recommendations of European LeukemiaNet
    Michele Baccarani
    Department of Hematology Oncology, L and A Seragnoli, University of Bologna, Bologna, Italy
    J Clin Oncol 27:6041-51. 2009
    ....
  14. ncbi Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification
    M E Gorre
    Department of Medicine, Molecular Biology Institute, University of California, Los Angeles, CA 90095, USA
    Science 293:876-80. 2001
    ..These studies provide evidence that genetically complex cancers retain dependence on an initial oncogenic event and suggest a strategy for identifying inhibitors of STI-571 resistance...
  15. ncbi Consensus meeting for the management of gastrointestinal stromal tumors. Report of the GIST Consensus Conference of 20-21 March 2004, under the auspices of ESMO
    J Y Blay
    Unité Inserm 590, Centre Leon Berard, 69008 Lyon and Hopital Edouard Herriot, Place d Arsonval, 69003 Lyon, France
    Ann Oncol 16:566-78. 2005
    ..The objectives of this international consensus meeting were to describe the optimal management procedures for patients with GIST in localized and advanced stages, as well as research issues for the future...
  16. ncbi Visualization of cellulose synthase demonstrates functional association with microtubules
    Alexander R Paredez
    Department of Biological Sciences, Stanford University, 260 Panama Street, Stanford, CA 94305, USA
    Science 312:1491-5. 2006
    ..Inhibition of microtubule polymerization changed the fine-scale distribution and pattern of moving CESA complexes in the membrane, indicating a relatively direct mechanism for guidance of cellulose deposition by the cytoskeleton...
  17. ncbi Dynamics of chronic myeloid leukaemia
    Franziska Michor
    Program for Evolutionary Dynamics, Department of Organismic and Evolutionary Biology, Department of Mathematics, Harvard University, Cambridge, Massachusetts 02138, USA
    Nature 435:1267-70. 2005
    ..We calculate the probability of developing imatinib resistance mutations and estimate the time until detection of resistance. Our model provides the first quantitative insights into the in vivo kinetics of a human cancer...
  18. pmc Activation of stress response gene SIRT1 by BCR-ABL promotes leukemogenesis
    Hongfeng Yuan
    Department of Cancer Biology, Beckman Research Institute, City of Hope, Duarte, CA, USA
    Blood 119:1904-14. 2012
    ..Our findings suggest further exploration of SIRT1 as a therapeutic target for CML treatment to overcome resistance...
  19. 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...
  20. ncbi Sirt1 inhibitor, Sirtinol, induces senescence-like growth arrest with attenuated Ras-MAPK signaling in human cancer cells
    H Ota
    Department of Anesthesia and Critical Care, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA 02129, USA
    Oncogene 25:176-85. 2006
    ..These results suggest that inhibitors for Sirt1 may have anticancer potential, and that impaired activation of Ras-MAPK pathway might take part in a senescence-like growth arrest program induced by Sirtinol...
  21. ncbi Tankyrase, a poly(ADP-ribose) polymerase at human telomeres
    S Smith
    The Rockefeller University, 1230 York Avenue, New York, NY 10021, USA
    Science 282:1484-7. 1998
    ..ADP-ribosylation of TRF1 diminished its ability to bind to telomeric DNA in vitro, suggesting that telomere function in human cells is regulated by poly(ADP-ribosyl)ation...
  22. ncbi Roflumilast in moderate-to-severe chronic obstructive pulmonary disease treated with longacting bronchodilators: two randomised clinical trials
    Leonardo M Fabbri
    University of Modena and Reggio Emilia, Modena, Italy
    Lancet 374:695-703. 2009
    ..The effect of roflumilast on lung function in patients with COPD that is moderate to severe who are already being treated with salmeterol or tiotropium was investigated...
  23. pmc 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...
  24. pmc Targeting autophagy potentiates tyrosine kinase inhibitor-induced cell death in Philadelphia chromosome-positive cells, including primary CML stem cells
    Cristian Bellodi
    University of Leicester, United Kingdom
    J Clin Invest 119:1109-23. 2009
    ..Together, these findings suggest that autophagy inhibitors may enhance the therapeutic effects of TKIs in the treatment of CML...
  25. ncbi A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as a therapeutic target of imatinib in idiopathic hypereosinophilic syndrome
    Jan Cools
    Brigham and Women s Hospital and Harvard Medical School, Boston, USA
    N Engl J Med 348:1201-14. 2003
    ..Recent reports of responses to imatinib in patients with the syndrome suggested that an activated kinase such as ABL, platelet-derived growth factor receptor (PDGFR), or KIT, all of which are inhibited by imatinib, might be the cause...
  26. pmc Antidepressant actions of histone deacetylase inhibitors
    Herbert E Covington
    Fishberg Department of Neuroscience, Mount Sinai School of Medicine, New York, New York 10029, USA
    J Neurosci 29:11451-60. 2009
    ....
  27. 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
    ....
  28. ncbi Resveratrol promotes autophagic cell death in chronic myelogenous leukemia cells via JNK-mediated p62/SQSTM1 expression and AMPK activation
    Alexandre Puissant
    INSERM 895, Team 2 Cell Death Differentiation and Cancer, Laboratoire d OncoHématologie, Centre Hospitalier Universitaire de Nice, Nice, France
    Cancer Res 70:1042-52. 2010
    ..We concluded that RSV triggered autophagic cell death in CML cells via both JNK-mediated p62 overexpression and AMPK activation. Our findings show that the JNK and AMPK pathways can cooperate to eliminate CML cells via autophagy...
  29. pmc Phase II trial of neoadjuvant/adjuvant imatinib mesylate for advanced primary and metastatic/recurrent operable gastrointestinal stromal tumors: long-term follow-up results of Radiation Therapy Oncology Group 0132
    Dian Wang
    Medical College of Wisconsin, Milwaukee, WI, USA
    Ann Surg Oncol 19:1074-80. 2012
    ..We have now updated the clinical outcomes including progression-free survival, disease-specific survival, and overall survival at a median follow-up of 5.1 years, and we correlate these end points with duration of imatinib therapy...
  30. 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
    ....
  31. ncbi The preclinical pharmacology of roflumilast--a selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease
    Armin Hatzelmann
    Nycomed GmbH, Konstanz, Germany
    Pulm Pharmacol Ther 23:235-56. 2010
    ..This enables roflumilast to offer effective, oral maintenance treatment for COPD, with an acceptable tolerability profile and the potential to favourably affect the extrapulmonary effects of the disease...
  32. ncbi Preclinical studies of TW-37, a new nonpeptidic small-molecule inhibitor of Bcl-2, in diffuse large cell lymphoma xenograft model reveal drug action on both Bcl-2 and Mcl-1
    Ramzi M Mohammad
    Division of Hematology and Oncology, Department of Internal Medicine, Karmanos Cancer Institute, Wayne State University School of Medicine, Detroit, Michigan, USA
    Clin Cancer Res 13:2226-35. 2007
    ..We have previously employed the natural product (-)-gossypol to test its therapeutic potential as a small-molecule inhibitor of Bcl-2 for the treatment of B-cell lymphomas...
  33. ncbi Identification of a class of small molecule inhibitors of the sirtuin family of NAD-dependent deacetylases by phenotypic screening
    C M Grozinger
    Department of Chemistry and Chemical Biology, The Howard Hughes Medical Institute, Harvard University, Cambridge, Massachusetts 02138, USA
    J Biol Chem 276:38837-43. 2001
    ..Preliminary studies using one of these compounds suggest that inhibition of sirtuins interferes with body axis formation in Arabidopsis...
  34. ncbi Mechanisms of BCR-ABL in the pathogenesis of chronic myelogenous leukaemia
    Ruibao Ren
    Rosenstiel Basic Medical Sciences Research Center, MS029, Brandeis University, 415 South Street, Waltham, Massachusetts 02454 9110, USA
    Nat Rev Cancer 5:172-83. 2005
    ..What have clinical trials of imatinib and studies using mouse models for BCR-ABL leukaemogenesis taught us about the functions of BCR-ABL beyond its kinase activity, and how these functions contribute to CML pathogenesis?..
  35. pmc ETV1 is a lineage survival factor that cooperates with KIT in gastrointestinal stromal tumours
    Ping Chi
    Department of Medicine, Memorial Sloan Kettering Cancer Center, New York, New York 10065, USA
    Nature 467:849-53. 2010
    ..It also represents a novel mechanism of oncogenic transcription factor activation...
  36. pmc Improved early event-free survival with imatinib in Philadelphia chromosome-positive acute lymphoblastic leukemia: a children's oncology group study
    Kirk R Schultz
    Department of Pediatrics, Division of Hematology Oncology Bone Marrow Transplantation, University of British Columbia, B C s Children s Hospital, Vancouver, BC, V6H 3V4, Canada
    J Clin Oncol 27:5175-81. 2009
    ..Imatinib mesylate is a targeted agent that may be used against Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL), one of the highest risk pediatric ALL groups...
  37. 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...
  38. ncbi Phase II study of imatinib in advanced chordoma
    Silvia Stacchiotti
    Fondazione Istitutodi Ricovero e Cura a Carattere Scientifico Istituto Nazionale Tumori, Milan, Italy
    J Clin Oncol 30:914-20. 2012
    ..To explore the antitumor activity of imatinib in patients with advanced platelet-derived growth factor β (PDGFB)/PDGF receptor β (PDGFRB)-positive chordomas...
  39. ncbi A novel tyrosine kinase switch is a mechanism of imatinib resistance in gastrointestinal stromal tumors
    D Mahadevan
    Arizona Cancer Center, Tucson, AZ 85724, USA
    Oncogene 26:3909-19. 2007
    ..MP470 synergizes with docetaxel (taxotere) and is cytotoxic to GIST cells...
  40. pmc HDAC2 regulates atypical antipsychotic responses through the modulation of mGlu2 promoter activity
    Mitsumasa Kurita
    Department of Psychiatry, Mount Sinai School of Medicine, New York, New York, USA
    Nat Neurosci 15:1245-54. 2012
    ..These observations support the view of HDAC2 as a promising new target for schizophrenia treatment...
  41. pmc 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...
  42. pmc Aurora B couples chromosome alignment with anaphase by targeting BubR1, Mad2, and Cenp-E to kinetochores
    Claire Ditchfield
    School of Biological Sciences, University of Manchester, 2 205 Stopford Building, Oxford Rd, Manchester M13 9PT, UK
    J Cell Biol 161:267-80. 2003
    ..Together, these results suggest that by targeting checkpoint proteins to kinetochores, Aurora B couples chromosome alignment with anaphase onset...
  43. pmc NCCN Task Force report: update on the management of patients with gastrointestinal stromal tumors
    George D Demetri
    Ludwig Center at Dana Farber Harvard Cancer Center, USA
    J Natl Compr Canc Netw 8:S1-41; quiz S42-4. 2010
    ..The task force met for the first time in October 2003 and again in December 2006 and October 2009. This supplement describes the recent developments in the field of GIST as discussed at the October 2009 meeting...
  44. ncbi Psychosocial stress is associated with in vivo dopamine release in human ventromedial prefrontal cortex: a positron emission tomography study using [¹⁸F]fallypride
    Johan Lataster
    Department of Psychiatry and Neuropsychology, South Limburg Mental Health Research and Teaching Network, EURON, Maastricht University Medical Center, Maastricht, The Netherlands
    Neuroimage 58:1081-9. 2011
    ....
  45. ncbi Molecular pathobiology of gastrointestinal stromal sarcomas
    Christopher L Corless
    Department of Pathology, Oregon Health and Science University Cancer Institute, Portland, OR 97239, USA
    Annu Rev Pathol 3:557-86. 2008
    ....
  46. ncbi Roflumilast with long-acting β2-agonists for COPD: influence of exacerbation history
    E D Bateman
    University of Cape Town Lung Institute, Cape Town, South Africa
    Eur Respir J 38:553-60. 2011
    ..No differences arose in adverse events between these subgroups. Roflumilast may be used to reduce exacerbations and improve dyspnoea and lung function, without increasing adverse events in COPD patients receiving concomitant LABAs...
  47. ncbi Molecular targeting of platelet-derived growth factor B by imatinib mesylate in a patient with metastatic dermatofibrosarcoma protuberans
    Brian P Rubin
    Department of Pathology, University of Washington Medical Center, Seattle, WA 98195, USA
    J Clin Oncol 20:3586-91. 2002
    ..We investigated the response of dermatofibrosarcoma protuberans to the tyrosine kinase inhibitor imatinib mesylate...
  48. ncbi Effect of 1-year treatment with roflumilast in severe chronic obstructive pulmonary disease
    Peter M A Calverley
    Department of Medicine, Clinical Sciences, University Hospital Aintree, Liverpool L97AL, UK
    Am J Respir Crit Care Med 176:154-61. 2007
    ..Whether treatment is effective in more severe COPD (GOLD [Global Initiative for Chronic Obstructive Lung Disease] stages III and IV) over a longer period is unknown...
  49. pmc The structure of the leukemia drug imatinib bound to human quinone reductase 2 (NQO2)
    Jonathan A Winger
    Department of Molecular and Cell Biology, California Institute for Quantitative Biosciences, Howard Hughes Medical Institute, University of California, Berkeley, USA
    BMC Struct Biol 9:7. 2009
    ..Recent screens carried out to find off-target proteins that bind to imatinib identified the oxidoreductase NQO2, a flavoprotein that is phosphorylated in a chronic myelogenous leukemia cell line...
  50. ncbi Amphetamine-induced displacement of [18F] fallypride in striatum and extrastriatal regions in humans
    Patrizia Riccardi
    Department of Radiology, Vanderbilt University, Nashville, TN 37232 2675, USA
    Neuropsychopharmacology 31:1016-26. 2006
    ..43 mg/kg) can be used to study D-AMPH-induced DA release in the striatal and extrastriatal regions in humans, and their relationship with cognition and sensation-seeking behavior...
  51. ncbi Imatinib for newly diagnosed patients with chronic myeloid leukemia: incidence of sustained responses in an intention-to-treat analysis
    Hugues de Lavallade
    Department of Haematology, Imperial College London, Du Cane Rd, London W12 0NN, United Kingdom
    J Clin Oncol 26:3358-63. 2008
    ..Here, we report our experience in treating patients at a single institution in a setting where all events were recorded...
  52. ncbi Gain-of-function mutations of platelet-derived growth factor receptor alpha gene in gastrointestinal stromal tumors
    Seiichi Hirota
    Department of Pathology, Osaka University Medical School, Suita, Japan
    Gastroenterology 125:660-7. 2003
    ..We investigated the cause of GISTs without KIT mutations. Because GISTs apparently expressed platelet-derived growth factor receptor (PDGFR) alpha, we examined whether GISTs without KIT mutations had a mutation of PDGFR alpha...
  53. pmc 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...
  54. ncbi Proteomic analysis of an imatinib-resistant K562 cell line highlights opposing roles of heat shock cognate 70 and heat shock 70 proteins in resistance
    Marion Pocaly
    U876 INSERM, Universite Victor Segalen Bordeaux 2, Hématopoïèse Leucémique et Cibles Thérapeutiques, Bordeaux, France
    Proteomics 8:2394-406. 2008
    ..In contrast, the induced decreased expression of Hsc70 was accompanied by a greater overexpression of Hsp70. This proteomic study therefore suggests opposing roles of Hsp70 and Hsc70 in imatinib resistance...
  55. ncbi Persistent activation of the Fyn/ERK kinase signaling axis mediates imatinib resistance in chronic myelogenous leukemia cells through upregulation of intracellular SPARC
    Nina Fenouille
    Universite de Nice Sophia Antipolis, Nice, France
    Cancer Res 70:9659-70. 2010
    ..Taken together, our results highlight an important role for the Fyn/ERK signaling pathway in imatinib-resistant cells that is driven by accumulation of intracellular SPARC...
  56. ncbi Phase I pharmacokinetic and pharmacodynamic study of the oral MAPK/ERK kinase inhibitor PD-0325901 in patients with advanced cancers
    Patricia M LoRusso
    Karmanos Cancer Institute, Wayne State University, Detroit, Michigan 48201, USA
    Clin Cancer Res 16:1924-37. 2010
    ..To determine tolerability, pharmacokinetics, and pharmacodynamics of PD-0325901, a highly potent, selective, oral mitogen-activated protein kinase/extracellular signal-regulated kinase (ERK) kinase 1/2 inhibitor in advanced cancer patients...
  57. ncbi Acquired resistance to imatinib in gastrointestinal stromal tumor occurs through secondary gene mutation
    Cristina R Antonescu
    Department of Pathology, Sloan Kettering Institute, New York, New York, USA
    Clin Cancer Res 11:4182-90. 2005
    ..That acquired resistance to imatinib in GIST commonly occurs via secondary gene mutation in the KIT kinase domain has implications for strategies to delay or prevent imatinib resistance and to employ newer targeted therapies...
  58. ncbi STI571 inactivation of the gastrointestinal stromal tumor c-KIT oncoprotein: biological and clinical implications
    D A Tuveson
    MIT Cancer Center and Department of Biology, Cambridge, MA 02139, USA
    Oncogene 20:5054-8. 2001
    ..These cell-culture-based studies support an important role for c-KIT signaling in GIST and suggest therapeutic potential for STI571 in patients afflicted by this chemoresistant tumor...
  59. pmc Gene expression changes associated with progression and response in chronic myeloid leukemia
    Jerald P Radich
    Division of Clinical Research, Fred Hutchinson Cancer Research Center, Seattle, WA 98109, USA
    Proc Natl Acad Sci U S A 103:2794-9. 2006
    ..These studies point to specific gene pathways that might be exploited for both prognostic indicators as well as new targets for therapy...
  60. pmc Development and validation of a prognostic nomogram for recurrence-free survival after complete surgical resection of localised primary gastrointestinal stromal tumour: a retrospective analysis
    Jason S Gold
    Department of Surgery VA Boston Healthcare System Brigham and Women s Hospital West Roxbury, MA, USA
    Lancet Oncol 10:1045-52. 2009
    ..We aimed to develop a nomogram to predict RFS after surgery in the absence of adjuvant therapy to help guide patient selection for adjuvant imatinib therapy...
  61. ncbi Tolerability-adapted imatinib 800 mg/d versus 400 mg/d versus 400 mg/d plus interferon-α in newly diagnosed chronic myeloid leukemia
    Rudiger Hehlmann
    Medizinische Klinik, Medizinische Fakultat Mannheim, Universitat Heidelberg, Pettenkoferstr 22, 68169 Mannheim, Germany
    J Clin Oncol 29:1634-42. 2011
    ..Treatment of chronic-phase (CP) chronic myeloid leukemia (CML) with imatinib 400 mg/d can be unsatisfactory. Optimization of treatment is warranted...
  62. ncbi Imatinib plus peginterferon alfa-2a in chronic myeloid leukemia
    Claude Preudhomme
    Laboratoire d Hematologie, Centre Hospitalier Universitaire de Lille, and INSERM Unité 837, Lille, France
    N Engl J Med 363:2511-21. 2010
    ..However, only a minority of patients treated with imatinib have a complete molecular remission...
  63. pmc Insulin-like growth factor 1 receptor is a potential therapeutic target for gastrointestinal stromal tumors
    Chi Tarn
    Departments of Medical Oncology and Pathology and Human Genetics Program, Fox Chase Cancer Center, Philadelphia, PA 19111, USA
    Proc Natl Acad Sci U S A 105:8387-92. 2008
    ....
  64. ncbi Identification of mcl-1 as a BCR/ABL-dependent target in chronic myeloid leukemia (CML): evidence for cooperative antileukemic effects of imatinib and mcl-1 antisense oligonucleotides
    Karl J Aichberger
    Department of Internal Medicine I, Division of Hematology and Hemostaseology, Medical University of Vienna, AKH Wien, Waehringer Guertel 18 20, A 1097 Vienna, Austria
    Blood 105:3303-11. 2005
    ..Moreover, the mcl-1 ASO was found to synergize with imatinib in producing growth inhibition in these cells. Together, our data identify MCL-1 as a BCR/ABL-dependent survival factor and interesting target in CML...
  65. ncbi Validation of the Joensuu risk criteria for primary resectable gastrointestinal stromal tumour - the impact of tumour rupture on patient outcomes
    P Rutkowski
    Department of Soft Tissue Bone Sarcoma and Melanoma, Maria Sklodowska Curie Memorial Cancer Centre and Institute of Oncology, Roentgena 5, 02 781 Warsaw, Poland
    Eur J Surg Oncol 37:890-6. 2011
    ..Approval of imatinib for adjuvant treatment of gastrointestinal stromal tumours (GIST) raised discussion about accuracy of prognostic factors in GIST and the clinical significance of the available risk stratification criteria...
  66. ncbi Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor
    Michael C Heinrich
    R and D 19 3710 SW US Veterans Hospital Rd, Portland, OR 97207, USA
    J Clin Oncol 21:4342-9. 2003
    ..The relationship between mutations in these kinases and clinical response to imatinib was examined in a group of patients with advanced GIST...
  67. ncbi Frequency of major molecular responses to imatinib or interferon alfa plus cytarabine in newly diagnosed chronic myeloid leukemia
    Tim P Hughes
    Institute of Medical and Veterinary Science, Adelaide, SA, Australia
    N Engl J Med 349:1423-32. 2003
    ..We measured levels of BCR-ABL transcripts in the blood of all patients in this trial who had a complete cytogenetic remission...
  68. 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...
  69. pmc Striatal and extrastriatal dopamine release measured with PET and [(18)F] fallypride
    Mark Slifstein
    Columbia University, New York, NY, USA
    Synapse 64:350-62. 2010
    ....
  70. ncbi Adherence is the critical factor for achieving molecular responses in patients with chronic myeloid leukemia who achieve complete cytogenetic responses on imatinib
    David Marin
    Department of Haematology, Imperial College London, Hammersmith Hospital, Du Cane Rd, London W12 0NN, United Kingdom
    J Clin Oncol 28:2381-8. 2010
    ..There is a considerable variability in the level of molecular responses achieved with imatinib therapy in patients with chronic myeloid leukemia (CML). These differences could result from variable therapy adherence...
  71. ncbi Bosutinib is active in chronic phase chronic myeloid leukemia after imatinib and dasatinib and/or nilotinib therapy failure
    H Jean Khoury
    Winship Cancer Institute of Emory University, Atlanta, GA 30322, USA
    Blood 119:3403-12. 2012
    ..Bosutinib may offer a new treatment option for patients with chronic-phase CML after treatment with multiple TKIs. This trial was registered at www.clinicaltrials.gov as NCT00261846...
  72. ncbi Patterns of care, prognosis, and survival in patients with metastatic gastrointestinal stromal tumors (GIST) refractory to first-line imatinib and second-line sunitinib
    Antoine Italiano
    Institut Bergonie, Bordeaux, France
    Ann Surg Oncol 19:1551-9. 2012
    ..Data regarding the management and outcome of patients with metastatic gastrointestinal stromal tumors (GIST) refractory to 1st-line imatinib and 2nd-line sunitinib are limited...
  73. ncbi The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901
    Stephen D Barrett
    Department of Chemistry, Pfizer Global Research and Development, Ann Arbor, MI 48105, USA
    Bioorg Med Chem Lett 18:6501-4. 2008
    ....
  74. ncbi Transient potent BCR-ABL inhibition is sufficient to commit chronic myeloid leukemia cells irreversibly to apoptosis
    Neil P Shah
    Division of Hematology Oncology, Department of Medicine, UCSF School of Medicine, San Francisco, CA 94143, USA
    Cancer Cell 14:485-93. 2008
    ..In CML patients receiving dasatinib once daily, response correlates with the magnitude of BCR-ABL kinase inhibition, thereby demonstrating the potential clinical utility of intermittent potent kinase inhibitor therapy...
  75. ncbi Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides
    Jerome C Bressi
    Takeda San Diego, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 20:3142-5. 2010
    A series of N-(2-amino-5-substituted phenyl)benzamides (3-21) were designed, synthesized and evaluated for their inhibition of HDAC2 and their cytotoxicity in HCT116 cancer cells...
  76. ncbi Nilotinib in the treatment of advanced gastrointestinal stromal tumours resistant to both imatinib and sunitinib
    M Montemurro
    University Hospital Lausanne, Cancer Center, Lausanne, Switzerland
    Eur J Cancer 45:2293-7. 2009
    ..Nilotinib is active in GIST resistant to both imatinib and sunitinib. These results warrant further investigation of nilotinib in GIST...
  77. ncbi A phase II study of PD-0325901, an oral MEK inhibitor, in previously treated patients with advanced non-small cell lung cancer
    Eric B Haura
    H Lee Moffitt Cancer Center and Research Institute, Tampa, Florida, USA
    Clin Cancer Res 16:2450-7. 2010
    ....
  78. pmc Persistence of leukemia stem cells in chronic myelogenous leukemia patients in prolonged remission with imatinib treatment
    Su Chu
    Division of Hematopoietic Stem Cell and Leukemia Research, City of Hope National Medical Center, Duarte, CA, USA
    Blood 118:5565-72. 2011
    ..These results directly demonstrate that BCR-ABL(+) stem cells persist in CML patients despite prolonged treatment with imatinib, and support ongoing efforts to target this population...
  79. pmc Concurrent intensive chemotherapy and imatinib before and after stem cell transplantation in newly diagnosed Philadelphia chromosome-positive acute lymphoblastic leukemia. Final results of the CSTIBES02 trial
    Josep Maria Ribera
    Department of Hematology of the Hospitals Institut Català d Oncologia Hospital Germans Trias i Pujol, Badalona, Spain
    Haematologica 95:87-95. 2010
    ....
  80. ncbi Cathepsin B release after imatinib-mediated lysosomal membrane permeabilization triggers BCR-ABL cleavage and elimination of chronic myelogenous leukemia cells
    A Puissant
    INSERM 895, Team 2 Cell Death Differentiation and Cancer, Nice, France
    Leukemia 24:115-24. 2010
    ..Hence, we describe an original pathway by which Imatinib participates to the elimination of CML cells through LMP and CB-mediated specific degradation of BCR-ABL...
  81. ncbi Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib
    Paul W Manley
    Novartis Institutes for BioMedical Research, Basel, Switzerland
    Bioorg Med Chem 18:6977-86. 2010
    ....
  82. 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...
  83. ncbi Inhibition of tumor necrosis factor-alpha -induced nuclear translocation and activation of NF-kappa B by dehydroxymethylepoxyquinomicin
    Akiko Ariga
    Department of Applied Chemistry, Faculty of Science and Technology, Keio University, 3 14 1 Hiyoshi, Kohoku Ku, Yokohama 223 0061, Japan
    J Biol Chem 277:24625-30. 2002
    ..Taken together, these data indicate that DHMEQ is a unique inhibitor of NF-kappaB acting at the level of nuclear translocation...
  84. 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...
  85. pmc Modifications of cellulose synthase confer resistance to isoxaben and thiazolidinone herbicides in Arabidopsis Ixr1 mutants
    W R Scheible
    Department of Plant Biology, Carnegie Institution, Stanford, CA 94305-4150, USA
    Proc Natl Acad Sci U S A 98:10079-84. 2001
    ..Although the IXR1 gene is expressed in the same cells as the structurally related RSW1 (AtCESA1) cellulose synthase gene, these two CESA genes are not functionally redundant...
  86. ncbi The tumor suppressor PP2A is functionally inactivated in blast crisis CML through the inhibitory activity of the BCR/ABL-regulated SET protein
    Paolo Neviani
    Human Cancer Genetics Program, Department of Molecular Virology, Immunology and Medical Genetics, The Ohio State University, Columbus, Ohio 43210, USA
    Cancer Cell 8:355-68. 2005
    ..Thus, functional inactivation of PP2A is essential for BCR/ABL leukemogenesis and, perhaps, required for blastic transformation...
  87. ncbi Gene expression profiling of imatinib and PD166326-resistant CML cell lines identifies Fyn as a gene associated with resistance to BCR-ABL inhibitors
    Sebastien Grosso
    INSERM U895, Cell Death, Differentiation and Cancer Team, Faculté de Médecine de Nice, Nice Cedex 2, France
    Mol Cancer Ther 8:1924-33. 2009
    ..Our findings provide a comprehensive picture of the transcriptional events associated with imatinib and PD166326 resistance and identify Fyn as a new potential target for therapeutic intervention in CML...
  88. 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...
  89. ncbi Natural killer cell IFN-gamma levels predict long-term survival with imatinib mesylate therapy in gastrointestinal stromal tumor-bearing patients
    Cedric Menard
    Institut National de la Sante et de la Recherche Medicale INSERM, Unit U805 Tumor immunology and immunotherapy, Villejuif, France
    Cancer Res 69:3563-9. 2009
    ..The NK cell IFN-gamma production after 2 months of treatment could be considered an independent predictor of long term survival in advanced GISTs treated with IM...
  90. ncbi beta-Catenin is essential for survival of leukemic stem cells insensitive to kinase inhibition in mice with BCR-ABL-induced chronic myeloid leukemia
    Y Hu
    Department of Medicine, Division of Hematology, University of Massachusetts Medical School, Worcester, MA 01605, USA
    Leukemia 23:109-16. 2009
    ..Furthermore, we show that beta-catenin in the Wnt signaling pathway is essential for survival and self-renewal of LSCs, providing a new strategy for targeting these cells...
  91. ncbi Resistance to imatinib: mutations and beyond
    Paul La Rosée
    Klinik fur Innere Medizin II, Hämatologie Onkologie, Universitatsklinikum Jena, Jena, Germany
    Semin Hematol 47:335-43. 2010
    ..The intent of this review is to shed light on the various aspects of TKI resistance in CML with respect to their biology and clinical implications...
  92. ncbi OCT-1-mediated influx is a key determinant of the intracellular uptake of imatinib but not nilotinib (AMN107): reduced OCT-1 activity is the cause of low in vitro sensitivity to imatinib
    Deborah L White
    Division of Hematology, Institute of Medical and Veterinary Science IMVS and Hanson Institute, Adelaide, South Australia
    Blood 108:697-704. 2006
    ..Determining interpatient and interdrug differences in cellular uptake and retention could allow individual optimization of kinase inhibitor therapy...
  93. ncbi PARP inhibitors in oncology: a new synthetic lethal approach to cancer therapy
    V Kruse
    Department of Medical Oncology, Ghent University Hospital, Belgium
    Acta Clin Belg 66:2-9. 2011
    ..In conclusion, it can be stated that an exciting new class of drugs has entered the arena of cancer therapy. However, additional clinical studies are needed before PARP inhibitors can definitely enter daily clinical practice...
  94. pmc Inhibition of protein-tyrosine phosphatase 1B (PTP1B) mediates ubiquitination and degradation of Bcr-Abl protein
    Daniel Alvira
    Tumour Biology Laboratory, Biochemistry Department, Bioscience Research Institute, University College Cork, Cork, Ireland
    J Biol Chem 286:32313-23. 2011
    ....
  95. ncbi Phase I and pharmacodynamic study of the oral MEK inhibitor CI-1040 in patients with advanced malignancies
    Patricia M LoRusso
    Barbara Ann Karmanos Cancer Institute, 4100 John R 4 HWCRC, Room 4206, Detroit, MI 48201, USA
    J Clin Oncol 23:5281-93. 2005
    ....
  96. pmc Absence of progression as assessed by response evaluation criteria in solid tumors predicts survival in advanced GI stromal tumors treated with imatinib mesylate: the intergroup EORTC-ISG-AGITG phase III trial
    Axel Le Cesne
    Department of Medicine, Institut Gustave Roussy, Villejuif, France
    J Clin Oncol 27:3969-74. 2009
    ..This analysis investigates whether the response classification assessed by RECIST (Response Evaluation Criteria in Solid Tumors), predicts for time to progression (TTP) and overall survival (OS)...
  97. ncbi Chidamide (CS055/HBI-8000): a new histone deacetylase inhibitor of the benzamide class with antitumor activity and the ability to enhance immune cell-mediated tumor cell cytotoxicity
    Zhi Qiang Ning
    Chipscreen Biosciences Ltd, Bio Incubator 2 601, 1st Ave of Gaoxin Road, Hi Tech Industrial Park, Shenzhen 518057, Guangdong, China
    Cancer Chemother Pharmacol 69:901-9. 2012
    ..This study reports the in vitro and in vivo antitumor characteristics of the compound...
  98. ncbi A randomized, phase II study of preoperative plus postoperative imatinib in GIST: evidence of rapid radiographic response and temporal induction of tumor cell apoptosis
    John C McAuliffe
    The University of Texas Houston, Houston, TX, USA
    Ann Surg Oncol 16:910-9. 2009
    ..02). Imatinib appears to be safe and may be considered for patients undergoing surgical resection of their GIST. Radiographic response and tumor cell apoptosis occur within the first week of imatinib therapy...
  99. ncbi Genetic ablation of delta opioid receptors in nociceptive sensory neurons increases chronic pain and abolishes opioid analgesia
    Claire Gaveriaux-Ruff
    IGBMC Institut de Génétique et de Biologie Moléculaire et Cellulaire, Neurobiology and Genetic Department, Illkirch F 67400, France
    Pain 152:1238-48. 2011
    ..The conditional knockout of delta-opioid receptor in primary afferent Na(V)1.8 neurons augmented mechanical allodynia in persistent pain models and abolished delta opioid analgesia in these models...
  100. pmc Identification of a low-molecular weight TrkB antagonist with anxiolytic and antidepressant activity in mice
    Maxime Cazorla
    Neurobiology and Molecular Pharmacology, Centre de psychiatrie et Neurosciences, UMR 894 INSERM Université Paris Descartes, Paris, France
    J Clin Invest 121:1846-57. 2011
    ..We further propose that ANA-12 may be a valuable tool for studying BDNF/TrkB signaling and may constitute a lead compound for developing the next generation of therapeutic agents for the treatment of mood disorders...
  101. 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
    ....

Research Grants77

  1. Mouse models for GABA epigenetic dysfunction
    Alessandro Guidotti; Fiscal Year: 2009
    ..Hence, we have focused our attention on the action of HDAC inhibitors (i.e., valproate and benzamides) as putative drugs that may, by increasing core histone tail acetylation at nucleosomal sites, normalize in ..
  2. NEW CNS DOPAMINE RECEPTOR IMAGING AGENTS
    HANK KUNG; Fiscal Year: 2002
    ..The structure-activity relationship of the proposed benzamides will be evaluated. 2) Studies of radiochemistry for preparation of Tc-99m, Tc-99 and Re labeled target molecules...
  3. D2 RECEPTORS IN SCHIZOPHRENIA: OPTIMIZED PET LIGANDS
    Robert Kessler; Fiscal Year: 1993
    ..Our group has synthesized and studied iodinated benzamides with relatively low lipophilicity, very high affinity (KD = 25 picomolar), and selectivity for the D2 receptor ..
  4. IMAGING OF THE BRAIN USING SMALL GAMMA CAMERAS
    JOHN AARSVOLD; Fiscal Year: 2001
    ..Substituted benzamides, in particular, have received significant interest because of their selective, high affinity and the reversible ..
  5. Phase I Clinical Trials of Anti-Cancer Agents
    Francis Giles; Fiscal Year: 2007
    ..abstract_text> ..
  6. Can beta-lactam antibiotics decrease morphine physical dependence?
    SCOTT RAWLS; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  7. Cannabinoid Regulation of Basal Ganglia Glutamate and GABA
    SCOTT RAWLS; Fiscal Year: 2007
    ..Our outcomes will be a first step in determining whether blocking endocannabinoid inactivation offers any therapeutic advantage over direct activation of cannabinoid receptors with marijuana. [unreadable] [unreadable] [unreadable]..
  8. Small Animal PET (microPET)
    JOGESH MUKHERJEE; Fiscal Year: 2007
    ..abstract_text> ..
  9. Phase II Study of 44Gy from 131I-81C6 for CNS Tumors
    David Reardon; Fiscal Year: 2004
    ..To further define the toxicity of this approach and Specific Aim 3.To determine the impact of this therapy on quality of life. ..
  10. Transition to Cocaine Abuse in Monkey:Role of Dopamine
    Michael Nader; Fiscal Year: 2005
    ....
  11. Pet Imaging of Extrastriatial Dopamine Levels
    Robert Kessler; Fiscal Year: 2005
    ..abstract_text> ..
  12. RNAi-medicated inhibition of BDNF expression and alcohol-drinking behavior
    QINGSHAN YAN; Fiscal Year: 2008
    ..abstract_text> ..
  13. SMALL ANIMAL PET SCANNER
    Robert Kessler; Fiscal Year: 2003
    ..It will be sited physically within the PET Center administratively within the newly formed Center for Research Imaging under the Direction of Dr. John Gore. ..
  14. OCCUPANCY OF EXTRASTRIATAL D2 RECEPTORS BY CLOZAPINE
    Robert Kessler; Fiscal Year: 2002
    ..Secondary goals include examining if psychopathological symptom complexes, i.e., positive, negative, and disorganization, as well as cognitive abnormalities in schizophrenia are related to regional levels of D2 receptors. ..
  15. ALCOHOL AND MESOLIMBIC DOPAMINE PATHWAY
    QINGSHAN YAN; Fiscal Year: 2002
    ..This will elucidate the relative contribution of 5-HT2 receptors to the regulation of ethanol-induced DA release and help to explain the effects of 5-HT2 antagonists on alcohol consumption reported in the literature. ..
  16. Novel Delta Opioids: Analgesic Effects & Abuse Liability
    SIDNEY NEGUS; Fiscal Year: 2009
    ....
  17. DOSE RESPONSE EFFECTS OF ALCOHOL ON BONE METABOLISM
    Russell Turner; Fiscal Year: 2006
    ....
  18. ESTROGEN METABOLITES EFFECTS ON BONE
    Russell Turner; Fiscal Year: 2002
    ..abstract_text> ..
  19. Etiology and Treatment of Parathyroid Bone Disease
    Russell Turner; Fiscal Year: 2005
    ..Since PDGF antagonists such as trapidil are available for human use, positive results could be quickly extended to clinical practice. ..
  20. 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]..
  21. Novel TNF Chimeric Vector for Treatment of Pancreatic Cancer
    Tony Reid; Fiscal Year: 2008
    ..To improve therapeutic efficacy, we have developed a stabilized form of TNF that cannot be released from the surface of the tumor cells. [unreadable] [unreadable] [unreadable]..
  22. Distal Lung Inflammation Effect on Asthma Exacerbations
    Donald Tashkin; Fiscal Year: 2008
    ..This study has the potential to clarify the contribution of the "silent zone" to the persistent morbidity encountered with asthma. ..
  23. Tyrosine Kinase Pathways in Autoimmune Arthritis.
    Ricardo Paniagua; Fiscal Year: 2008
    ....
  24. Antitumor Mechanisms of SRC Inhibitors in Lung Cancer
    Eric Haura; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  25. Differential effects of TARPs on AMPA receptor subunits
    AMY ARAI; Fiscal Year: 2008
    ..unreadable] [unreadable]..
  26. Prenatal Cannabis Effect on the Endocannabinoid System
    VINOD YARAGUDRI; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  27. THERAPEUTICS STUDIES OF PRIMARY CNS MALIGNANCIES
    Patrick Wen; Fiscal Year: 2008
    ..abstract_text> ..
  28. Statistical Genetic Methods for Cancer Gene Studies
    Susan Slager; Fiscal Year: 2006
    ..abstract_text> ..
  29. delta-Catenin and Cell-Cell Adhesion in Prostate Cancer
    Qun Lu; Fiscal Year: 2010
    ..Understanding the posttranslational modifications that control 8-catenin functions will unravel mechanisms by which S-catenin modulates gene expression and promotes CaP in vivo. ..
  30. Radiolabeled Probes for Imaging Caspase 3 Activation
    Robert Mach; Fiscal Year: 2008
    ..abstract_text> ..
  31. Type-1 Diabetes: Zn2+ Potentiated Beta-Cell Death By Sirtuin-Mediated NAD+ Loss
    CHRISTIAN THOMAS SHELINE; Fiscal Year: 2010
    ..These experiments will test novel therapeutic compounds (pyruvate, sirtinol) and mechanisms (NAD+loss, sirtuins) involved in Zn2+ mediation of beta-cell death in type-1 diabetes. ..
  32. Targeting HIF-1alpha in renal cell carcinoma: the role of HDAC inhibitors
    Roberto Pili; Fiscal Year: 2010
    ....
  33. DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORS
    Arun K Ghosh; Fiscal Year: 2010
    ..This research integrates organic synthesis, protein-ligand x-ray crystallography, molecular modeling and in-depth virus and cell-biological studies to design the next generation of HIV-1 protease inhibitors. ..
  34. Lymphocyte Survival: Implications for lymphomagenesis
    Craig B Thompson; Fiscal Year: 2010
    ....
  35. PHYSICOCHEMICAL INVESTIGATION OF TASTE
    Vijay Lyall; Fiscal Year: 2010
    ..The research will reveal how the sour taste defense mechanism functions to prevent the ingestion of acids. ..
  36. Structural and Cellular Biology of GPH Receptors
    JAMES ALAN DIAS; Fiscal Year: 2010
    ..The overall goal of the studies is to provide new information to better our understanding of regulation of gonadal function by gonadotropins and provide new avenues for fertility ..
  37. DEVELOPMENT OF LIGAND ASSISTED ASYMMETRIC SYNTHESES
    Arun Ghosh; Fiscal Year: 2001
    ..Besides the broad range of scope and generality, this line of research will provide excellent opportunities to teach and train graduate and undergraduate students in the laboratory. ..
  38. Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.
    BARRY TROST; Fiscal Year: 2009
    ..These new synthetic methods apply to many structural types beyond those illustrated and constitutes a significant to gain access to complex molecular targets more easily. ..
  39. Dopamine D2 Selective Imaging Agents
    Robert Mach; Fiscal Year: 2008
    ..A secondary goal of this project is to develop an iodine-125 labeled radiotracer for in vitro binding studies of the D2 receptor. ..
  40. Vascular and Metabolic Mechanisms in Alzheimer's Disease
    Robert Mach; Fiscal Year: 2009
    ..Through the use of the unique resources and personnel at Washington University Medical Center, we have the opportunity to provide answers to important clinical and mechanistic questions in AD. ..
  41. Mathematical Models of Programmed CTL Proliferation
    Dominik Wodarz; Fiscal Year: 2009
    ..These are the role of effector molecules (such as perform and IFN-g) for CTL dynamics, and the role of CD4 T cell help. The modeling work will be complemented by experiments with VSV and LCMV infected mice. ..
  42. Effect of Drugs on Myocardial Hypoxia
    Garrett Gross; Fiscal Year: 2009
    ..Information gained from these studies will hopefully lead to new therapies to treat patients with ischemic heart disease. ..
  43. APE EXPRESSION/LEUKEMIA RESPONSE TO CHEMO/RADIOTHERAPY
    Kent Robertson; Fiscal Year: 2001
    ....
  44. The Effect of a Mixture of Pesticides on the Rat Cardiac Proteome
    John Crow; Fiscal Year: 2007
    ..Our long-term objective is to better understand the extent to which commonly used pesticides and other environmental chemicals influence heart disease and its treatment. [unreadable] [unreadable] [unreadable]..
  45. LUNG HEALTH STUDY--LONG TERM FOLLOW UP
    Donald Tashkin; Fiscal Year: 2002
    ..All ten of the original LHS clinical centers plan to participate in this study. To minimize bias, all surviving participants of the LHS will be invited to participate, giving a potential sample size of 5600. ..
  46. PERMEATION OF IRRITANT MIXTURES THRU PROTECTIVE MATERIAL
    SHANE QUE HEE; Fiscal Year: 2002
    ..The relationship of the fundamental independent variables to the kinetic parameters of permeation and to the Corrositex rating as the index of irritation will be determined and compared. ..
  47. Gene Methylation and Therapeutic Response in Lung Cancer
    Steven Belinsky; Fiscal Year: 2005
    ..The validation of these genes as biomarkers of lung cancer risk and their detection in sputum and/or serum could ultimately support chemoprevention trials for preventing lung cancer. ..
  48. Clofarabine: Cytarabine Activation for Leukemia Response
    Stefan Faderl; Fiscal Year: 2004
    ..abstract_text> ..
  49. PET Radiotracers for Imaging Apoptosis
    Robert Mach; Fiscal Year: 2004
    ..If successful, the research described in this research proposal will provide a PET-based imaging procedure for measuring apoptosis that will be of tremendous value to the PET research community. ..
  50. Mapping the D2/D3 Dopamine Receptor Binding Sites
    ROBERT LUEDTKE; Fiscal Year: 2004
    ..LB dopamine receptor selective compounds bind to the neumtransmitter binding sate and 2) provide additional structural information that will assist us in the design of novel compounds with increased selectivity for LB dopamine receptors ..
  51. Inductively Coupled Plasma- Mass Spectrometer
    SHANE QUE HEE; Fiscal Year: 2003
    ..A team of researchers has been assembled whose research needs for elemental analyses are in the broad areas of environmental health, nutrition, biomedical and behavioral research. ..
  52. DIFFERENCES IN SYNAPTIC VS NONSYNAPTIC AMPA RECEPTORS
    AMY ARAI; Fiscal Year: 2004
    ..Determining which cellular factor stabilizes the low-affinity receptors will constitute the Fifth Aim of this application. ..
  53. SCLERODERMA LUNG STUDY
    Donald Tashkin; Fiscal Year: 2003
    ..abstract_text> ..
  54. DEVELOPMENT OF D3 ANTAGONISTS TO TREAT COCAINE ADDICTION
    Robert Mach; Fiscal Year: 2002
    ..In addition, this research will result in the development of radiolabeled probes for studying both the function of D3 receptors in the CNS and the alteration in D3 receptor density thatoccurs as a consequence of cocaine abuse. ..
  55. COCAINE SELF ADMINISTRATION IN DOPAMINE KNOCKOUT MICE
    SIMON CAINE; Fiscal Year: 2003
    ..abstract_text> ..
  56. TRAINING IN HEMATOPOIETIC & VASCULAR CELL FUNCTIONS
    Bruno Calabretta; Fiscal Year: 2003
    ..The objective of this research training is to develop competent research scientists capable of performing and eventually directing research with a comprehensive approach in the area of cell function. ..
  57. Novel Animal Model System of AIDS-Kaposi Sarcoma
    Patricio Ray; Fiscal Year: 2005
    ....
  58. PET Imaging of Breast Cancer via Sigma-2 Receptors
    Robert Mach; Fiscal Year: 2006
    ..abstract_text> ..
  59. Regulation- Medulloblastoma Growth by alpha-v integrins
    Tobey Macdonald; Fiscal Year: 2006
    ..The long-range goal of this work is to broaden our understanding of medulloblastoma growth, so that novel biologic therapies may be developed into new treatments for medulloblastoma, the most common malignant brain tumor in children. ..
  60. Metabolomics: From Bioenergetics To Apoptosis
    Craig Thompson; Fiscal Year: 2005
    ..Understanding the relationships between metabolism and apoptosis may lead to novel approaches for the prevention and/or treatment of cancer and degenerative disorders. ..
  61. Iron and Vitamin E in Childhood HIV-Associated Renal Disease
    Patricio Ray; Fiscal Year: 2006
    ..The proposed studies should have a substantial impact on the goals of the National Center for Complementary and Alternative Medicine and NIH, according to the program announcement PA-02-124. [unreadable] [unreadable]..
  62. CALCITRIOL & DEXAMETHASONE FOR MYELODYSPLASTIC SYNDROMES
    ROBERT REDNER; Fiscal Year: 2004
    ..Abstract Not Provided ..
  63. Dopamine D3 Receptor Imaging Agents for PET and SPECT
    Robert Mach; Fiscal Year: 2006
    ..A secondary goal of this project is to develop an iodine-125 labeled radiotracer for in vitro binding studies of the D3 receptor. ..
  64. Delta-Catenin Cleavage by Presenilin and Synaptic Remodeling
    Qun Lu; Fiscal Year: 2006
    ..It will also lay the foundation for future R01 investigation of the roles of delta-catenin proteolytic fragments in AD pathogenesis. ..
  65. Nitric Oxide Control of CGRP in Trigeminal Neurons
    Paul Durham; Fiscal Year: 2002
    ..abstract_text> ..
  66. Aging, Adenosine and Platelet-Mediated Thrombosis
    Karin Przyklenk; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  67. Detection of Dopamine Release During a Cognitive Task
    RAJENDRA BADGAIYAN; Fiscal Year: 2006
    ..This study will determine whether the molecular imaging technique can be reliably used to investigate an unexplored aspect (neurotransmission) of human cognition. [unreadable] [unreadable]..
  68. ALTERED KCa CHANNEL EXPRESSION IN DEVELOPING CEREBELLUM
    ANDREA YOOL; Fiscal Year: 2002
    ..The rat provides a useful model for studying postnatal cerebellar development and neuropathological damage, and may provide insights into methods to manipulate developmental abnormalities in the cerebellum. ..
  69. Individual Differences in Extrastriatal DA Release
    David Zald; Fiscal Year: 2009
    ..abstract_text> ..
  70. Cellular Regulation of Salt Taste Transduction
    Vijay Lyall; Fiscal Year: 2008
    ..The identification of natural and synthetic analogues similar to cetylpyridinium chloride that modulate the non-specific cation receptor channel may be potentially useful as salt taste enhancers or suppressers. ..
  71. Role of inositol trisphosphate in preconditioning
    Karin Przyklenk; Fiscal Year: 2004
    ....
  72. Prefrontal cortical dopamine and cognition-schizophrenia
    Anissa Abi Dargham; Fiscal Year: 2007
    ..abstract_text> ..
  73. PET Imaging of Serotonin Transmission in MDMA Users
    Anissa Abi Dargham; Fiscal Year: 2008
    ..abstract_text> ..
  74. DOPAMINE TRANSMISSION IN ALCOHOLISM
    Anissa Abi Dargham; Fiscal Year: 2002
    ..Understanding the neurochemical abnormalities underlying vulnerability to alcoholism would guide future treatment interventions and risk prevention strategies. ..
  75. Preconditioning Improves Coronary Patency
    Karin Przyklenk; Fiscal Year: 2007
    ..The resulting mechanistic insights may, ultimately, be exploited in the future design of novel therapies for the clinical treatment of recurrent thrombosis. ..