thiazoles

Summary

Top Publications

  1. ncbi Imaging brain amyloid in Alzheimer's disease with Pittsburgh Compound-B
    William E Klunk
    Department of Psychiatry, PET Facility, University of Pittsburgh, 200 Lothrop Street, Pittsburgh, PA 15213 2582, USA
    Ann Neurol 55:306-19. 2004
  2. ncbi Effectiveness of antipsychotic drugs in patients with chronic schizophrenia
    Jeffrey A Lieberman
    Department of Psychiatry, College of Physicians and Surgeons, Columbia University, New York State Psychiatric Institute, New York, NY 10032, USA
    N Engl J Med 353:1209-23. 2005
  3. pmc Post-mortem correlates of in vivo PiB-PET amyloid imaging in a typical case of Alzheimer's disease
    Milos D Ikonomovic
    Department of Neurology, University of Pittsburgh School of Medicine, Pittsburgh, PA 15213, USA
    Brain 131:1630-45. 2008
  4. pmc Frequent amyloid deposition without significant cognitive impairment among the elderly
    Howard Jay Aizenstein
    Department of Psychiatry, University of Pittsburgh School of Medicine, Pittsburgh, PA, USA
    Arch Neurol 65:1509-17. 2008
  5. pmc Dasatinib combined with docetaxel for castration-resistant prostate cancer: results from a phase 1-2 study
    John C Araujo
    The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, USA
    Cancer 118:63-71. 2012
  6. pmc Small-molecule correctors of defective DeltaF508-CFTR cellular processing identified by high-throughput screening
    Nicoletta Pedemonte
    Department of Medicine, UCSF, San Francisco, California 94143 0521, USA
    J Clin Invest 115:2564-71. 2005
  7. ncbi Efficacy and tolerability of mirabegron, a β(3)-adrenoceptor agonist, in patients with overactive bladder: results from a randomised European-Australian phase 3 trial
    Vik Khullar
    St Mary s Hospital, Imperial College, London, UK
    Eur Urol 63:283-95. 2013
  8. pmc Functional amyloid formation within mammalian tissue
    Douglas M Fowler
    Department of Chemistry, The Skaggs Institute of Chemical Biology, The Scripps Research Institute, La Jolla, California, USA
    PLoS Biol 4:e6. 2006
  9. ncbi Effect of environmental factors on the kinetics of insulin fibril formation: elucidation of the molecular mechanism
    L Nielsen
    Department of Chemistry and Biochemistry, University of California, Santa Cruz, California 95064, USA
    Biochemistry 40:6036-46. 2001
  10. pmc The Alzheimer's Disease Neuroimaging Initiative positron emission tomography core
    William J Jagust
    Helen Wills Neuroscience Institute, University of California Berkeley, Berkeley, CA, USA
    Alzheimers Dement 6:221-9. 2010

Detail Information

Publications344 found, 100 shown here

  1. ncbi Imaging brain amyloid in Alzheimer's disease with Pittsburgh Compound-B
    William E Klunk
    Department of Psychiatry, PET Facility, University of Pittsburgh, 200 Lothrop Street, Pittsburgh, PA 15213 2582, USA
    Ann Neurol 55:306-19. 2004
    ..This relationship was most robust in the parietal cortex (r = -0.72; p = 0.0001). The results suggest that PET imaging with the novel tracer, PIB, can provide quantitative information on amyloid deposits in living subjects...
  2. ncbi Effectiveness of antipsychotic drugs in patients with chronic schizophrenia
    Jeffrey A Lieberman
    Department of Psychiatry, College of Physicians and Surgeons, Columbia University, New York State Psychiatric Institute, New York, NY 10032, USA
    N Engl J Med 353:1209-23. 2005
    ..We compared a first-generation antipsychotic, perphenazine, with several newer drugs in a double-blind study...
  3. pmc Post-mortem correlates of in vivo PiB-PET amyloid imaging in a typical case of Alzheimer's disease
    Milos D Ikonomovic
    Department of Neurology, University of Pittsburgh School of Medicine, Pittsburgh, PA 15213, USA
    Brain 131:1630-45. 2008
    ..The strong direct correlation of in vivo PiB retention with region-matched quantitative analyses of Abeta plaques in the same subject supports the validity of PiB-PET imaging as a method for in vivo evaluation of Abeta plaque burden...
  4. pmc Frequent amyloid deposition without significant cognitive impairment among the elderly
    Howard Jay Aizenstein
    Department of Psychiatry, University of Pittsburgh School of Medicine, Pittsburgh, PA, USA
    Arch Neurol 65:1509-17. 2008
    ....
  5. pmc Dasatinib combined with docetaxel for castration-resistant prostate cancer: results from a phase 1-2 study
    John C Araujo
    The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, USA
    Cancer 118:63-71. 2012
    ....
  6. pmc Small-molecule correctors of defective DeltaF508-CFTR cellular processing identified by high-throughput screening
    Nicoletta Pedemonte
    Department of Medicine, UCSF, San Francisco, California 94143 0521, USA
    J Clin Invest 115:2564-71. 2005
    ..Small-molecule correctors may be useful in the treatment of CF caused by the DeltaF508 mutation...
  7. ncbi Efficacy and tolerability of mirabegron, a β(3)-adrenoceptor agonist, in patients with overactive bladder: results from a randomised European-Australian phase 3 trial
    Vik Khullar
    St Mary s Hospital, Imperial College, London, UK
    Eur Urol 63:283-95. 2013
    ..Mirabegron, a β(3)-adrenoceptor agonist, has been developed for the treatment of overactive bladder (OAB)...
  8. pmc Functional amyloid formation within mammalian tissue
    Douglas M Fowler
    Department of Chemistry, The Skaggs Institute of Chemical Biology, The Scripps Research Institute, La Jolla, California, USA
    PLoS Biol 4:e6. 2006
    ....
  9. ncbi Effect of environmental factors on the kinetics of insulin fibril formation: elucidation of the molecular mechanism
    L Nielsen
    Department of Chemistry and Biochemistry, University of California, Santa Cruz, California 95064, USA
    Biochemistry 40:6036-46. 2001
    ..A kinetic model, involving the association of monomeric partially folded intermediates, whose concentration is stimulated by the air-water interface, leading to formation of the critical nucleus and thence fibrils, is proposed...
  10. pmc The Alzheimer's Disease Neuroimaging Initiative positron emission tomography core
    William J Jagust
    Helen Wills Neuroscience Institute, University of California Berkeley, Berkeley, CA, USA
    Alzheimers Dement 6:221-9. 2010
    ..This is a progress report of the Alzheimer's Disease Neuroimaging Initiative (ADNI) positron emission tomography (PET) Core...
  11. ncbi Dasatinib (BMS-354825) targets an earlier progenitor population than imatinib in primary CML but does not eliminate the quiescent fraction
    Mhairi Copland
    Division of Cancer Sciences and Molecular Pathology, University of Glasgow, UK
    Blood 107:4532-9. 2006
    ..These data confirm that dasatinib is more effective than IM within the CML stem cell compartment; however, the most primitive quiescent CML cells appear to be inherently resistant to both drugs...
  12. ncbi Small-molecule inhibition of the interaction between the translation initiation factors eIF4E and eIF4G
    Nathan J Moerke
    Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA
    Cell 128:257-67. 2007
    ..The identification of this compound provides a new tool for studying translational control and establishes a possible new strategy for cancer therapy...
  13. ncbi Results of a randomized phase III trial of mirabegron in patients with overactive bladder
    Victor W Nitti
    New York University Langone Medical Center, New York, New York 10016, USA
    J Urol 189:1388-95. 2013
    ..Many patients with overactive bladder discontinue pharmacotherapy due to suboptimal efficacy or side effects. Mirabegron, a β3-adrenoceptor agonist, may offer an effective and well tolerated alternative treatment for overactive bladder...
  14. ncbi Antipsychotic-induced weight gain: a comprehensive research synthesis
    D B Allison
    Obesity Research Center, St Luke s Roosevelt Hospital, Columbia University College of Physicians and Surgeons, NY 10025, UDA
    Am J Psychiatry 156:1686-96. 1999
    ..The purpose of this study was to estimate and compare the effects of antipsychotics-both the newer ones and the conventional ones-on body weight...
  15. ncbi Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity
    Marcos L Sznaidman
    GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709 3398, USA
    Bioorg Med Chem Lett 13:1517-21. 2003
    ..Optimization of these hits by structure-guided design led to 7k (GW501516) and 7l (GW0742), which shows an EC(50) of 1.1 nM against PPARdelta with 1000-fold selectivity over the other human subtypes...
  16. ncbi Glycogen synthase kinase-3beta participates in nuclear factor kappaB-mediated gene transcription and cell survival in pancreatic cancer cells
    Andrei V Ougolkov
    Division of Oncology Research and GI Research Unit, Mayo Clinic College of Medicine, Rochester, Minnesota, USA
    Cancer Res 65:2076-81. 2005
    ..Taken together, our results simultaneously identify a previously unrecognized role for GSK-3beta in cancer cell survival and proliferation and suggest GSK-3beta as a potential therapeutic target in the treatment of pancreatic cancer...
  17. ncbi Manipulation of alternative splicing by a newly developed inhibitor of Clks
    Michiko Muraki
    Laboratory of Gene Expression, School of Biomedical Science, Department of Functional Genomics, Medical Research Institute, Tokyo Medical and Dental University, Japan
    J Biol Chem 279:24246-54. 2004
    ....
  18. ncbi In vitro and in vivo activity of SKI-606, a novel Src-Abl inhibitor, against imatinib-resistant Bcr-Abl+ neoplastic cells
    Miriam Puttini
    Department of Clinical Medicine, S Gerardo Hospital University of Milano Bicocca, Monza, Italy
    Cancer Res 66:11314-22. 2006
    ..Modeling considerations attribute the superior activity of SKI-606 to its ability to bind a conformation of Bcr-Abl different from imatinib...
  19. pmc The urate-lowering efficacy and safety of febuxostat in the treatment of the hyperuricemia of gout: the CONFIRMS trial
    Michael A Becker
    The University of Chicago Pritzker School of Medicine, MC0930, University of Chicago Medical Center, 5841 S, Maryland Avenue, Chicago, IL 60637, USA
    Arthritis Res Ther 12:R63. 2010
    ..The purpose of this study was to compare urate-lowering (UL) efficacy and safety of daily febuxostat and allopurinol in subjects with gout and serum urate (sUA) > or = 8.0 mg/dL in a six-month trial...
  20. ncbi Dasatinib induces rapid hematologic and cytogenetic responses in adult patients with Philadelphia chromosome positive acute lymphoblastic leukemia with resistance or intolerance to imatinib: interim results of a phase 2 study
    Oliver Ottmann
    Medizinische Klinik II, Johann Wolfgang Goethe Universitat, Frankfurt, Germany
    Blood 110:2309-15. 2007
    ..Dasatinib represents a safe and effective treatment option and an important therapeutic advance for patients with Ph-positive ALL. This trial was registered at www.clinicaltrials.gov as #CA180015...
  21. ncbi Peroxisome proliferator-activated receptor β/δ agonism protects the kidney against ischemia/reperfusion injury in diabetic rats
    Massimo Collino
    Department of Anatomy, Pharmacology, and Forensic Medicine, University of Turin, Turin, Italy
    Free Radic Biol Med 50:345-53. 2011
    ..Thus, we report herein that PPARβ/δ activation protects the diabetic kidney against I/R injury by a mechanism that may involve changes in renal expression of SOCS-3 resulting in a reduced local inflammatory response...
  22. pmc A randomized trial of dasatinib 100 mg versus imatinib 400 mg in newly diagnosed chronic-phase chronic myeloid leukemia
    Jerald P Radich
    Fred Hutchinson Cancer Research Center, Seattle, WA 98109, USA
    Blood 120:3898-905. 2012
    ..In summary, DAS compared with IM appeared to have more short-term cytogenetic and molecular response, more hematologic toxicity, and similar overall survival. This trial is registered at www.clinicaltrials.gov as NCT00070499...
  23. pmc First report of phase 2 study of dasatinib with hyper-CVAD for the frontline treatment of patients with Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukemia
    Farhad Ravandi
    Department of Leukemia, University of Texas M D Anderson Cancer Center, Houston, TX 77030, USA
    Blood 116:2070-7. 2010
    ..The combination of chemotherapy with dasatinib is effective in achieving long-term remissions in patients with newly diagnosed Ph(+) ALL. This study was registered at www.ClinicalTrials.gov as NCT00390793...
  24. ncbi Dasatinib, a multi-kinase inhibitor increased radiation sensitivity by interfering with nuclear localization of epidermal growth factor receptor and by blocking DNA repair pathways
    Uma Raju
    University of Texas M D Anderson Cancer Center, Houston, TX 77030, USA
    Radiother Oncol 105:241-9. 2012
    ....
  25. ncbi Neonicotinoid insecticide toxicology: mechanisms of selective action
    Motohiro Tomizawa
    Environmental Chemistry and Toxicology Laboratory, Department of Environmental Science, Policy and Management, University of California, Berkeley, California 94720 3112, USA
    Annu Rev Pharmacol Toxicol 45:247-68. 2005
    ..The low affinity of neonicotinoids for vertebrate relative to insect nicotinic receptors is a major factor in their favorable toxicological profile...
  26. ncbi Inhibition of SRC family kinases and receptor tyrosine kinases by dasatinib: possible combinations in solid tumors
    Juan Carlos Montero
    Instituto de Biología Molecular y Celular del Cáncer Centro de Investigación del Cáncer CIC, Consejo Superior de Investigaciones Científicas CSIC Universidad de Salamanca, Salamanca, Spain
    Clin Cancer Res 17:5546-52. 2011
    ..Here, we review the preclinical evidence that supports the use of dasatinib in combination for the treatment of solid tumors and describe various clinical trials developed following a preclinical rationale...
  27. ncbi Targeting SRC family kinases inhibits growth and lymph node metastases of prostate cancer in an orthotopic nude mouse model
    Serk In Park
    The Program in Cancer Biology, Graduate School of Biomedical Sciences, The University of Texas Health Science Center at Houston, TX 77030, USA
    Cancer Res 68:3323-33. 2008
    ..Therefore, we conclude that SFKs are promising therapeutic targets for treatment of human prostate cancer and that Src and Lyn activities affect different cellular functions required for prostate tumor growth and progression...
  28. ncbi Pharmacokinetics of intravenous and oral meloxicam in ruminant calves
    Johann F Coetzee
    Department of Clinical Sciences, College of Veterinary Medicine, Kansas State University, Manhattan, KS 66506, USA
    Vet Ther 10:E1-8. 2009
    ..00 (range, 0.64 to 1.66). These findings indicate that oral meloxicam administration might be an effective and convenient means of providing long-lasting analgesia to ruminant calves...
  29. ncbi Poly(lactide)-vitamin E derivative/montmorillonite nanoparticle formulations for the oral delivery of Docetaxel
    Si Shen Feng
    Department of Chemical and Biomolecular Engineering, National University of Singapore, Block E5, 02 11, 4 Engineering Drive 4, Singapore 117576, Singapore
    Biomaterials 30:3297-306. 2009
    ..59% for Taxotere((R)) to 78% for the PLA-TPGS/MMT NP formulation and 91% for the PLA-TPGS NP formulation respectively. Oral chemotherapy by nanoparticles of biodegradable polymers is feasible...
  30. pmc Dasatinib: a potent SRC inhibitor in clinical development for the treatment of solid tumors
    John Araujo
    Genitourinary Center, M D Anderson Cancer Centre, Houston, TX 77030, USA
    Cancer Treat Rev 36:492-500. 2010
    ..Future clinical trials will further assess the clinical value of SRC inhibition with dasatinib...
  31. ncbi Lurasidone in the treatment of schizophrenia: a randomized, double-blind, placebo- and olanzapine-controlled study
    Herbert Y Meltzer
    Department of Psychiatry, Vanderbilt University School of Medicine, Nashville, Tenn, USA
    Am J Psychiatry 168:957-67. 2011
    ..The study was designed to evaluate the short-term efficacy and safety of lurasidone in the treatment of acute schizophrenia...
  32. ncbi PPARdelta modulates lipopolysaccharide-induced TNFalpha inflammation signaling in cultured cardiomyocytes
    Guoliang Ding
    Cardiovascular Research Institute, Morehouse School of Medicine, 720 Westview Drive SW, Atlanta, GA 30310, USA
    J Mol Cell Cardiol 40:821-8. 2006
    ..Therefore, PPARdelta is an important determinant of TNFalpha expression via the NF-kappaB signaling pathway, thus serving as therapeutic targets to attenuate inflammation that are involved in cardiac pathological progression...
  33. ncbi Evidence for the role of peroxisome proliferator-activated receptor-beta/delta in the development of spinal cord injury
    Irene Paterniti
    Department of Clinical and Experimental Medicine and Pharmacology, School of Medicine, University of Messina, Messina, Italy
    J Pharmacol Exp Ther 333:465-77. 2010
    ..Our results clearly demonstrate that GW0742 treatment reduces the development of inflammation and tissue injury associated with spinal cord trauma...
  34. pmc A phase 2 trial of dasatinib in advanced melanoma
    Harriet M Kluger
    Yale Cancer Center, Yale University School of Medicine, New Haven, Connecticut 06510, USA
    Cancer 117:2202-8. 2011
    ..Dasatinib inhibits c-kit, PDGFβR, and EPHA2 and src kinases c-src, c-Yes, Lck, and Fyn. A phase 2 trial of dasatinib in melanoma was conducted to assess response rate (RR), progression-free survival (PFS), and toxicity...
  35. ncbi 15-Deoxy-delta 12, 14-prostaglandin J2 is a ligand for the adipocyte determination factor PPAR gamma
    B M Forman
    Salk Institute for Biological Studies, La Jolla, California 92037, USA
    Cell 83:803-12. 1995
    ..These findings suggest a pivotal role for PPAR gamma and its endogenous ligand in adipocyte development and glucose homeostasis and as a target for intervention in metabolic disorders...
  36. ncbi Measurement of cellular 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reduction activity and lactate dehydrogenase release using MTT
    K Abe
    Laboratory of Chemical Pharmacology, Graduate School of Pharmaceutical Sciences, The University of Tokyo, Tokyo 113 0033, Japan
    Neurosci Res 38:325-9. 2000
    ..Our method is economical and convenient especially for measuring cellular MTT reduction and LDH release in the same culture...
  37. ncbi Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias
    Moshe Talpaz
    Department of Leukemia, M D Anderson Cancer Center, Houston, USA
    N Engl J Med 354:2531-41. 2006
    ..We evaluated dasatinib, a BCR-ABL inhibitor that targets most imatinib-resistant BCR-ABL mutations, in patients with chronic myelogenous leukemia (CML) or Ph-positive acute lymphoblastic leukemia (ALL)...
  38. pmc Serial PIB and MRI in normal, mild cognitive impairment and Alzheimer's disease: implications for sequence of pathological events in Alzheimer's disease
    Clifford R Jack
    Clifford R Jack, Mayo Clinic, Diagnostic Radiology, 200 First Street SW, Rochester, MN 55905, USA
    Brain 132:1355-65. 2009
    ..This model implies a complimentary role for MRI and PIB imaging in Alzheimer's disease, with each reflecting one of the major pathologies, amyloid dysmetabolism and neurodegeneration...
  39. 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...
  40. ncbi Arabidopsis local resistance to Botrytis cinerea involves salicylic acid and camalexin and requires EDS4 and PAD2, but not SID2, EDS5 or PAD4
    Simone Ferrari
    Department of Genetics, Harvard Medical School, Massachusetts General Hospital, Boston, MA 02114, USA
    Plant J 35:193-205. 2003
    ..cinerea requires ethylene-, jasmonate-, and SA-mediated signaling, that the SA affecting this resistance does not require ICS1 and is likely synthesized via PAL, and that camalexin limits lesion development...
  41. ncbi Selectivity of febuxostat, a novel non-purine inhibitor of xanthine oxidase/xanthine dehydrogenase
    Yasuhiro Takano
    Pharmaceutical Development Research Laboratories, Teijin Institute for Bio Medical Research, Teijin Pharma Limited, 4 3 2, Asahigaoka Hino, Tokyo 191 8512, Japan
    Life Sci 76:1835-47. 2005
    ..These results demonstrate that febuxostat is a potent non-purine, selective inhibitor of XO, and could be useful for the treatment of hyperuricemia and gout...
  42. ncbi Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity
    Tadashi Ishibashi
    Pharmacology Research Laboratories, Dainippon Sumitomo Pharma Co, Ltd, Suita, Osaka, Japan
    J Pharmacol Exp Ther 334:171-81. 2010
    ..These results demonstrate that lurasidone possesses antipsychotic activity and antidepressant- or anxiolytic-like effects with potentially reduced liability for extrapyramidal and CNS depressant side effects...
  43. pmc Phase II study of dasatinib in patients with metastatic castration-resistant prostate cancer
    Evan Y Yu
    University of Washington, Seattle, Washington, USA
    Clin Cancer Res 15:7421-8. 2009
    ..This phase II study investigated the activity of dasatinib in patients with metastatic castration-resistant prostate cancer (CRPC)...
  44. ncbi Evaluation of the novel factor Xa inhibitor edoxaban compared with warfarin in patients with atrial fibrillation: design and rationale for the Effective aNticoaGulation with factor xA next GEneration in Atrial Fibrillation-Thrombolysis In Myocardial Infar
    Christian T Ruff
    TIMI Study Group, Cardiovascular Division, Department of Medicine, Brigham and Women s Hospital, Harvard Medical School, Boston, MA, USA
    Am Heart J 160:635-41. 2010
    ..Edoxaban is a selective and direct factor Xa inhibitor that may provide effective, safe, and more convenient anticoagulation...
  45. pmc Bead-based profiling of tyrosine kinase phosphorylation identifies SRC as a potential target for glioblastoma therapy
    Jinyan Du
    The Broad Institute of Harvard University and Massachusetts Institute of Technology, 7 Cambridge Center, Cambridge, Massachusetts 02142, USA
    Nat Biotechnol 27:77-83. 2009
    ..These studies establish the feasibility of tyrosine kinome-wide phosphorylation profiling and point to SRC as a possible therapeutic target in glioblastoma...
  46. ncbi Overriding imatinib resistance with a novel ABL kinase inhibitor
    Neil P Shah
    Division of Hematology and Oncology, Department of Medicine, The David Geffen School of Medicine, University of California, Los Angeles, CA, 90095, USA
    Science 305:399-401. 2004
    ..These data illustrate how molecular insight into kinase inhibitor resistance can guide the design of second-generation targeted therapies...
  47. ncbi Protein synthesis is resistant to rapamycin and constitutes a promising therapeutic target in acute myeloid leukemia
    Jerome Tamburini
    Institut Cochin, Universite Paris Descartes, Centre National de la Recherche Scientifique CNRS, UMR8104, Paris, France
    Blood 114:1618-27. 2009
    ..Direct inhibition of the translation initiating complex thus represents an attractive option for the development of new therapies in AML...
  48. ncbi The ABC transporter BcatrB from Botrytis cinerea exports camalexin and is a virulence factor on Arabidopsis thaliana
    Francesca L Stefanato
    Department of Biology, University of Fribourg, Chemin du Musée 8, CH 1700 Fribourg, Switzerland
    Plant J 58:499-510. 2009
    ..Here we demonstrate that an ABC transporter is a virulence factor that increases tolerance of the pathogen towards a phytoalexin, and the complete restoration of virulence on host plants lacking this phytoalexin...
  49. ncbi Solution conformations and dynamics of ABL kinase-inhibitor complexes determined by NMR substantiate the different binding modes of imatinib/nilotinib and dasatinib
    Navratna Vajpai
    Novartis Institutes for BioMedical Research, Basel, Switzerland
    J Biol Chem 283:18292-302. 2008
    ..Nanosecond as well as microsecond dynamics can be detected for certain residues in the activation loop in the inactive and active conformation complexes...
  50. ncbi Activation of MAPK kinase 9 induces ethylene and camalexin biosynthesis and enhances sensitivity to salt stress in Arabidopsis
    Juan Xu
    State Key Laboratory of Plant Physiology and Biochemistry, College of Biological Sciences, China Agricultural University, Beijing 100094, China
    J Biol Chem 283:26996-7006. 2008
    ..The results reported here reveal that the MKK9-MPK3/MPK6 cascade participates in the regulation of the biosynthesis of ethylene and camalexin and may be an important axis in the stress responses of Arabidopsis...
  51. ncbi Risk assessment for side-effects of neonicotinoids against bumblebees with and without impairing foraging behavior
    Veerle Mommaerts
    Laboratory of Cellular Genetics, Department of Biology, Faculty of Sciences, Free University of Brussels, Brussels, Belgium
    Ecotoxicology 19:207-15. 2010
    ....
  52. ncbi Effects of food on the pharmacokinetics of edoxaban, an oral direct factor Xa inhibitor, in healthy volunteers
    Jeanne Mendell
    MPH, Daiichi Sankyo Pharma Development, 399 Thornall St, Edison, NJ 08837, USA
    J Clin Pharmacol 51:687-94. 2011
    ..Both Japanese and Caucasian volunteers demonstrated a modest but clinically insignificant food effect. It was concluded that edoxaban can be administered without regard to food...
  53. pmc Design and synthesis of C-2 substituted thiazolo and dihydrothiazolo ring-fused 2-pyridones: pilicides with increased antivirulence activity
    Erik Chorell
    Department of Chemistry, Umea University, SE 90187 Umea, Sweden
    J Med Chem 53:5690-5. 2010
    ..The structural basis of the PapD chaperone-pilicide interactions was determined by X-ray crystallography...
  54. pmc LYN is a mediator of epithelial-mesenchymal transition and a target of dasatinib in breast cancer
    Yoon La Choi
    Department of Pathology and Division of Breast and Endocrine Surgery, Samsung Medical Center, Sungkyunkwan University School of Medicine, Seoul, Korea
    Cancer Res 70:2296-306. 2010
    ....
  55. ncbi Gab2 signaling in chronic myeloid leukemia cells confers resistance to multiple Bcr-Abl inhibitors
    F U Wöhrle
    Centre for Biological Systems Analysis, Albert Ludwigs University of Freiburg, Freiburg, Germany
    Leukemia 27:118-29. 2013
    ..The identification of Gab2 as a novel modulator of TKI sensitivity in CML suggests that Gab2 could be exploited as a biomarker and therapeutic target in TKI-resistant disease...
  56. pmc Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk)
    Andrew S Rosenthal
    NIH Chemical Genomics Center, National Human Genome Research Institute, NIH, 9800 Medical Center Drive, MSC 3370, Bethesda, MD 20892 3370, USA
    Bioorg Med Chem Lett 21:3152-8. 2011
    ..Several of the most potent inhibitors were validated as being highly selective within a comprehensive kinome scan...
  57. ncbi An extremely potent inhibitor of xanthine oxidoreductase. Crystal structure of the enzyme-inhibitor complex and mechanism of inhibition
    Ken Okamoto
    Department of Biochemistry and Molecular Biology, Nippon Medical School, 1 1 5 Sendagi, Bunkyo ku, Tokyo 113 0022, Japan
    J Biol Chem 278:1848-55. 2003
    ..Although the inhibitor did not directly coordinate to the molybdenum ion, numerous hydrogen bonds as well as hydrophobic interactions with the protein matrix were observed, most of which are also used in substrate recognition...
  58. pmc Phase 2 study of dasatinib in the treatment of head and neck squamous cell carcinoma
    Heather D Brooks
    Division of Cancer Medicine, The University of Texas M D Anderson Cancer Center, Houston, Texas, USA
    Cancer 117:2112-9. 2011
    ..Treatment options for patients with advanced head and neck squamous cell carcinoma (HNSCC) are scarce. This phase 2 study was conducted to evaluate the safety, tolerability, pharmacokinetics, and efficacy of dasatinib in this setting...
  59. ncbi CPTH6, a thiazole derivative, induces histone hypoacetylation and apoptosis in human leukemia cells
    Daniela Trisciuoglio
    Experimental Chemotherapy Laboratory, Regina Elena National Cancer Institute, Via delle Messi d Oro 156, 00158 Rome, Italy
    Clin Cancer Res 18:475-86. 2012
    ..Among these compounds, 3-methylcyclopentylidene-[4-(4'-chlorophenyl)thiazol-2-yl]hydrazone (CPTH6) has been selected and used throughout this study...
  60. pmc Febuxostat inhibition of endothelial-bound XO: implications for targeting vascular ROS production
    Umair Z Malik
    University of Aga Khan Medical School, Karachi, Pakistan
    Free Radic Biol Med 51:179-84. 2011
    ....
  61. ncbi Oxidative stress is involved in Dasatinib-induced apoptosis in rat primary hepatocytes
    Tao Xue
    Institute of Pharmacology and Toxicology, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China
    Toxicol Appl Pharmacol 261:280-91. 2012
    ..Thus, relieving oxidative stress is a viable strategy for reducing Dasatinib-induced hepatotoxicity...
  62. ncbi Use of xanthine oxidase inhibitor febuxostat inhibits renal interstitial inflammation and fibrosis in unilateral ureteral obstructive nephropathy
    Hiroki Omori
    Department of Geriatric Medicine and Nephrology, Osaka University Graduate School of Medicine, Suita, Osaka 565 0871, Japan
    Clin Exp Nephrol 16:549-56. 2012
    ..While some reports suggest a relationship between hyperuricemia and chronic kidney disease (CKD), the renoprotective mechanism of an XO inhibitor in CKD remains unknown. Recent reports have focused on XO as a source of oxidative stress...
  63. ncbi Activation of peroxisome proliferator-activated receptor-β/-δ (PPARβ/δ) prevents endothelial dysfunction in type 1 diabetic rats
    Ana María Quintela
    Department of Pharmacology, School of Pharmacy, University of Granada, 18071 Granada, Spain
    Free Radic Biol Med 53:730-41. 2012
    ..This effect seems to be related to an increase in nitric oxide bioavailability as a result of reduced NADPH oxidase-driven superoxide production and downregulation of prepro endothelin-1...
  64. ncbi Modulation of non-voiding activity by the muscarinergic antagonist tolterodine and the β(3)-adrenoceptor agonist mirabegron in conscious rats with partial outflow obstruction
    James I Gillespie
    The Uro physiology Research Group, The Dental and Medical School, Newcastle University, Newcastle upon Tyne, UK
    BJU Int 110:E132-42. 2012
    ..Such concepts could provide insights into the nature of overactive bladder and the site of action of key therapeutic drugs...
  65. ncbi Epidemiology and control of intestinal parasites with nitazoxanide in children in Mexico
    Elvia Diaz
    Unidad de Medicina Familiar 91, Instituto Mexicano del Seguro Social, Estado de Mexico, Mexico
    Am J Trop Med Hyg 68:384-5. 2003
    ..Overall, 84% of the protozoa and 95% of the helminths were completely eliminated from the patients. Nitazoxanide was very well tolerated, with no serious adverse effects reported...
  66. ncbi An improved 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) reduction assay for evaluating the viability of Escherichia coli cells
    Hengwei Wang
    Newworld Institute of Biotechnology, State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, China
    J Microbiol Methods 82:330-3. 2010
    ..5-mL centrifuge tubes and formazan dissolution in test tubes. Our study is helpful in developing protocols for measuring the viability of other gram-negative bacteria...
  67. ncbi Dasatinib inhibits migration and invasion in diverse human sarcoma cell lines and induces apoptosis in bone sarcoma cells dependent on SRC kinase for survival
    Audrey C Shor
    Gonzmart Laboratory, Sarcoma Program, H Lee Moffitt Cancer Center and Research Institute, Tampa, Florida, USA
    Cancer Res 67:2800-8. 2007
    ..Therefore, dasatinib may provide therapeutic benefit by preventing the growth and metastasis of sarcomas in patients...
  68. pmc The aryl hydrocarbon receptor ligand ITE inhibits TGFβ1-induced human myofibroblast differentiation
    Geniece M Lehmann
    Department of Environmental Medicine, University of Rochester, Rochester, NY 14642, USA
    Am J Pathol 178:1556-67. 2011
    ..As supported by the results of this study, the small molecule ITE inhibits myofibroblast differentiation and may be useful clinically as an antiscarring agent...
  69. pmc Assays for studying nucleated aggregation of polyglutamine proteins
    Murali Jayaraman
    Department of Structural Biology and Pittsburgh Institute for Neurodegenerative Diseases, Biomedical Sciences Tower 3, 3501 Fifth Avenue, Pittsburgh, PA 15260, USA
    Methods 53:246-54. 2011
    ..Here we describe a series of methods for determining mechanistic details of the spontaneous aggregation of polyQ-containing sequences, including the identification and structural examination of aggregation intermediates...
  70. pmc Targeted inhibition of SRC kinase signaling attenuates pancreatic tumorigenesis
    Nagathihalli S Nagaraj
    Department of Surgery, Vanderbilt University School of Medicine, Nashville, TN, USA
    Mol Cancer Ther 9:2322-32. 2010
    ..These results establish a mechanistic rationale for Src inhibition with dasatinib as a therapeutic target in the treatment of pancreatic cancer and identify potential biomarkers of resistance to Src inhibition...
  71. ncbi Mirabegron, a β₃-adrenoceptor agonist for the potential treatment of urinary frequency, urinary incontinence or urgency associated with overactive bladder
    Pradeep Tyagi
    William Beaumont Hospital, Department of Urology, 3811 West 13 Mile Road, Royal Oak, MI 48073, USA
    IDrugs 13:713-22. 2010
    ....
  72. ncbi Gout therapeutics: new drugs for an old disease
    Christopher M Burns
    Dartmouth Medical School, Lebanon, NH 03756, USA
    Lancet 377:165-77. 2011
    ..Finally, we issue a word of caution about the proper use of the new drugs and the already available drugs for gout. At a time of important advances, we need to recommit ourselves to a rational approach to the treatment of gout...
  73. ncbi Double-blind comparison of the safety and efficacy of lurasidone and ziprasidone in clinically stable outpatients with schizophrenia or schizoaffective disorder
    Steven G Potkin
    Department of Psychiatry, Human Behavior, University of California at Irvine, Irvine, CA 92617, United States
    Schizophr Res 132:101-7. 2011
    ..The current study evaluated the safety and efficacy of lurasidone and ziprasidone in stable outpatients diagnosed with schizophrenia or schizoaffective disorder...
  74. ncbi Activities of SYK and PLCgamma2 predict apoptotic response of CLL cells to SRC tyrosine kinase inhibitor dasatinib
    Zibo Song
    Department of Pathology and Laboratory Medicine, Weill Cornell Medical College, New York, New York 10065, USA
    Clin Cancer Res 16:587-99. 2010
    ..We aim to define the molecular mechanisms underlying the differential dasatinib sensitivity and to uncover more effective therapeutic targets in CLL...
  75. ncbi A small-molecule c-Myc inhibitor, 10058-F4, induces cell-cycle arrest, apoptosis, and myeloid differentiation of human acute myeloid leukemia
    Ming Jer Huang
    Department of Medicine, Mackay Memorial Hospital, Taipei, Taiwan
    Exp Hematol 34:1480-9. 2006
    ..Inhibition of the c-Myc/Max heterodimerization by the recently identified small-molecule compound, 10058-F4, might be a novel antileukemic strategy...
  76. ncbi Rapid analysis of neonicotinoid insecticides in guttation drops of corn seedlings obtained from coated seeds
    Andrea Tapparo
    Universita degli Studi di Padova, Dipartimento di Scienze Chimiche, Via Marzolo 1, 35131 Padova, Italy
    J Environ Monit 13:1564-8. 2011
    ....
  77. ncbi Dasatinib as first-line treatment for adult patients with Philadelphia chromosome-positive acute lymphoblastic leukemia
    Robin Foa
    Department of Cellular Biotechnologies and Hematology, Sapienza University of Rome, Via Benevento 6, Rome, Italy
    Blood 118:6521-8. 2011
    ..In adult Ph(+) ALL, induction treatment with dasatinib plus steroids is associated with a CHR in virtually all patients, irrespective of age, good compliance, no deaths, and a very rapid debulking of the neoplastic clone...
  78. pmc Role of the Yersinia pestis yersiniabactin iron acquisition system in the incidence of flea-borne plague
    Florent Sebbane
    Equipe Peste et Yersinia pestis, Centre d Infection et d Immunité de Lille, Institut Pasteur de Lille, Lille, France
    PLoS ONE 5:e14379. 2010
    ..The results provide new evidence that primary septicemic plague is a distinct clinical entity and suggest that unusual forms of plague may be caused by atypical Y. pestis strains...
  79. pmc Klebsiella pneumoniae yersiniabactin promotes respiratory tract infection through evasion of lipocalin 2
    Michael A Bachman
    Department of Pathology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104, USA
    Infect Immun 79:3309-16. 2011
    ..However, Lcn2 retained partial protection against disseminated disease. In summary, Ybt is a virulence factor that is prevalent among KPC-producing K. pneumoniae isolates and promotes respiratory tract infections through evasion of Lcn2...
  80. ncbi 11C-PiB PET assessment of change in fibrillar amyloid-beta load in patients with Alzheimer's disease treated with bapineuzumab: a phase 2, double-blind, placebo-controlled, ascending-dose study
    Juha O Rinne
    Turku PET Centre and Clinical Research Services Turku, University of Turku and Turku University Hospital, Turku, Finland
    Lancet Neurol 9:363-72. 2010
    ..We used (11)C-PiB PET to investigate whether bapineuzumab, a humanised anti-amyloid-beta monoclonal antibody, would reduce cortical fibrillar amyloid-beta load in patients with Alzheimer's disease...
  81. ncbi Synthesis of novel triheterocyclic thiazoles as anti-inflammatory and analgesic agents
    R G Kalkhambkar
    Department of Chemistry, Karnatak Science College, College Road, Dharwad 580001, Karnataka, India
    Eur J Med Chem 42:1272-6. 2007
    Triheterocyclic thiazoles containing coumarin and carbostyril (1-aza coumarin) have been synthesized by the reaction of the in situ generated 4-thioureidomethyl carbostyril and 3-bromoacetyl coumarins...
  82. pmc Allosteric drugs: the interaction of antitumor compound MKT-077 with human Hsp70 chaperones
    Aikaterini Rousaki
    Program in Biophysics, The University of Michigan, Ann Arbor, MI 48109, USA
    J Mol Biol 411:614-32. 2011
    ..Suggestions for the improvement of the compound's properties are made on the basis of the binding location and pose...
  83. ncbi Interaction of thioflavin T with amyloid fibrils: stoichiometry and affinity of dye binding, absorption spectra of bound dye
    Anna I Sulatskaya
    Laboratory of Structural Dynamics, Stability and Folding of Proteins of the Institute of Cytology, Russian Academy of Sciences, St Petersburg 194064, Russia
    J Phys Chem B 115:11519-24. 2011
    ..1 × 10(4) M(-1) cm(-1), ε(b2,max) = 6.7 × 10(4) M(-1)cm(-1), λ(max) = 449 nm) and significantly differ from that of free ThT in aqueous solution (ε(max) = 3.2 × 10(4) M(-1)cm(-1), λ(max) = 412 nm)...
  84. ncbi The tyrosine kinase inhibitor dasatinib dysregulates bone remodeling through inhibition of osteoclasts in vivo
    Kate Vandyke
    Myeloma Research Laboratory, Department of Haematology, Centre for Cancer Biology, Institute of Medical and Veterinary Science, Adelaide, Australia
    J Bone Miner Res 25:1759-70. 2010
    ..These studies show that dasatinib increases trabecular bone volume at least in part by inhibiting osteoclast activity, suggesting that dasatinib therapy may result in dysregulated bone remodeling...
  85. pmc Insight into amyloid structure using chemical probes
    Ashley A Reinke
    Department of Biological Chemistry, Pathology and The Life Sciences Institute, University of Michigan, Ann Arbor, MI 48109 2216, USA
    Chem Biol Drug Des 77:399-411. 2011
    ..Moreover, we discuss how design and deployment of conformationally selective probes might be used to test emerging models of AD...
  86. pmc Activation of peroxisome proliferator-activated receptor beta/delta inhibits lipopolysaccharide-induced cytokine production in adipocytes by lowering nuclear factor-kappaB activity via extracellular signal-related kinase 1/2
    Ricardo Rodríguez-Calvo
    Pharmacology Unit, Department of Pharmacology and Therapeutic Chemistry, Faculty of Pharmacy, Institut de Biomedicina de la UB IBUB and CIBERDEM Instituto de Salud Carlos III, University of Barcelona, Barcelona, Spain
    Diabetes 57:2149-57. 2008
    ..It is presently unknown whether peroxisome proliferator-activated receptor (PPAR) beta/delta activation prevents inflammation in adipocytes...
  87. ncbi Interaction of mGlu2/3 agonism with clozapine and lurasidone to restore novel object recognition in subchronic phencyclidine-treated rats
    Masakuni Horiguchi
    Division of Psychopharmacology, Vanderbilt University Medical Center, Nashville, TN 37212, USA
    Psychopharmacology (Berl) 217:13-24. 2011
    ..Atypical antipsychotic drugs (APDs) reverse the effects of subchronic PCP on NOR. The effect of metabotropic glutamate₂/₃ receptor (mGlu₂/₃) agonists upon NOR is unknown...
  88. ncbi Congo red and thioflavin-T analogs detect Abeta oligomers
    Izumi Maezawa
    M I N D Institute and Department of Pathology, University of California Davis, Sacramento, California 95817, USA
    J Neurochem 104:457-68. 2008
    ..We propose that by improving the binding affinity of current ligands, in vivo imaging of AbetaO is feasible by a 'signal subtraction' procedure. This approach may facilitate the identification of individuals with early AD...
  89. ncbi Identification of candidate molecular markers predicting sensitivity in solid tumors to dasatinib: rationale for patient selection
    Fei Huang
    Departments of Clinical Discovery and Oncology Discovery, Bristol Myers Squibb Co, Princeton, NJ 08543, USA
    Cancer Res 67:2226-38. 2007
    ..Our results implicate that dasatinib may represent a valuable treatment option in this difficult-to-treat population. To test this hypothesis, clinical studies are now under way to determine the activity of dasatinib in these patients...
  90. ncbi The thioflavin T fluorescence assay for amyloid fibril detection can be biased by the presence of exogenous compounds
    Sean A Hudson
    School of Chemistry and Physics, The University of Adelaide, Australia
    FEBS J 276:5960-72. 2009
    ....
  91. ncbi Cross-resistance study and biochemical mechanisms of thiamethoxam resistance in B-biotype Bemisia tabaci (Hemiptera: Aleyrodidae)
    Yuntao Feng
    Department of Plant Protection, Institute of Vegetables and Flowers, Chinese Academy of Agricultural Sciences, Beijing, PR China
    Pest Manag Sci 66:313-8. 2010
    ..tabaci, a resistant strain was selected in the laboratory. Cross-resistance and the biochemical mechanisms of thiamethoxam resistance were investigated in the present study...
  92. ncbi Resveratrol inhibits beta-amyloid oligomeric cytotoxicity but does not prevent oligomer formation
    Ying Feng
    Tsinghua University School of Medicine, Haidian District, Beijing 100084, China
    Neurotoxicology 30:986-95. 2009
    ....
  93. ncbi Mechanism of thioflavin T binding to amyloid fibrils
    Ritu Khurana
    Department of Chemistry and Biochemistry, University of California, Santa Cruz, CA 95064, USA
    J Struct Biol 151:229-38. 2005
    ..Our data suggests that the micelles of thioflavin T bind amyloid fibrils leading to enhancement of fluorescence emission...
  94. ncbi The role of Src in prostate cancer
    K Fizazi
    Department of Medicine, Institut Gustave Roussy, 39 rue Camille Desmoulins, 94800 Villejuif, France
    Ann Oncol 18:1765-73. 2007
    ..Src inhibitors may be specifically evaluated in prostate cancer clinical trials in the near future...
  95. ncbi Plasma apolipoprotein E and Alzheimer disease risk: the AIBL study of aging
    V B Gupta
    Centre of Excellence for Alzheimer s Disease Research and Care, School of Exercise Biomedical and Health Sciences, Edith Cowan University, Joondalup, Western Australia, Australia
    Neurology 76:1091-8. 2011
    ..The major objective of this cross-sectional study was to investigate total plasma apoE as well as levels of the apoE4 form in a large, highly characterized cohort which included both healthy controls and participants with early-stage AD...
  96. pmc Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT
    Patrice Dubreuil
    INSERM, U891, Centre de Recherche en Cancerologie de Marseille, Signalisation, Hematopoiesis and Mechanisms of Oncogenesis, centre de référence des mastocytoses, Marseille, France
    PLoS ONE 4:e7258. 2009
    ..Here, we characterise the in vitro and in vivo profiles of masitinib (AB1010), a novel phenylaminothiazole-type tyrosine kinase inhibitor that targets KIT...
  97. ncbi Ribosomally synthesized thiopeptide antibiotics targeting elongation factor Tu
    Rowan P Morris
    Natural Products Unit, Novartis Institutes for BioMedical Research, Basel, 4056, Switzerland
    J Am Chem Soc 131:5946-55. 2009
    ..Thiopeptides are a class of macrocyclic, highly modified peptides that are decorated by thiazoles and defined by a central six-membered heterocyclic ring system...
  98. ncbi Lurasidone in the treatment of acute schizophrenia: a double-blind, placebo-controlled trial
    Mitsutaka Nakamura
    Dainippon Sumitomo Pharma America Inc, Fort Lee, NJ 07024, USA
    J Clin Psychiatry 70:829-36. 2009
    ..The objective of the study was to evaluate the safety and efficacy of lurasidone in patients hospitalized for an acute exacerbation of DSM-IV-defined schizophrenia...
  99. pmc In vitro high affinity alpha-synuclein binding sites for the amyloid imaging agent PIB are not matched by binding to Lewy bodies in postmortem human brain
    Liang Ye
    GlaxoSmithKline, Clinical Science and Technology, Neurology DM, New Frontiers Science Park, Harlow, UK
    J Neurochem 105:1428-37. 2008
    ..Lewy bodies pathology is therefore unlikely to contribute significantly to the retention of PIB in positron emission tomography imaging studies...
  100. ncbi Dynamics of resistance to the neonicotinoids acetamiprid and thiamethoxam in Bemisia tabaci (Homoptera: Aleyrodidae)
    A Rami Horowitz
    Agricultural Research Organization, Department of Entomology, Gilat Research Center, M P Negev, 85280, Israel
    J Econ Entomol 97:2051-6. 2004
    ....
  101. ncbi Fibrillar aggregates of the tumor suppressor p53 core domain
    Daniella Ishimaru
    Departamento de Bioquímica Médica and Centro Nacional de Ressonância Magnética Nuclear, Universidade Federal do Rio de Janeiro, 21941 590 Rio de Janeiro, RJ, Brazil
    Biochemistry 42:9022-7. 2003
    ..Fibrillar aggregates of p53C contribute to the loss of function of p53 and seed the accumulation of conformationally altered protein in some cancerous cells...

Research Grants71

  1. Chemical and biological exploration of a new natural product family, the thiazole
    DOUGLAS ALAN MITCHELL; Fiscal Year: 2013
    ..mutagenesis will be used to kinetically evaluate a key enzyme that catalyzes the first step in the formation of thiazoles and oxazoles...
  2. Modular Enzymatic Assembly Lines for Antibiotics
    Christopher T Walsh; Fiscal Year: 2013
    ..residues of the prethiocillin 52mer undergo a cascade of 14 posttranslational modifications, including 6 Cys to thiazoles, two threonines to dehydrobutyrines and two serines to the central pyridine heterocycle...
  3. Synthesis and Biology of Bengazole Analogs
    Peter Wipf; Fiscal Year: 2003
    ..Our specific aims in this collaborative project are: - Synthesis of bis-oxazoles, bis-oxazolines, bis-thiazoles and bis-thiazolines analogs of the anthelminthic marine natural product bengazole...
  4. Course of Functional Deficits in Late-Life Schizophrenia
    Philip Harvey; Fiscal Year: 2007
    ..unreadable] [unreadable]..
  5. CHEMICAL SYNTHESIS OF NOVEL NATURAL PRODUCTS
    David Williams; Fiscal Year: 2009
    ..Daphnicyclidin A. This recent discovery has revealed a new molecular architecture which exhibits significant antitumor activity. Our research will investigate strategies for chemical synthesis of these complex polycyclic systems. ..
  6. REGULATION OF PURINE NUCLEOTIDE SYNTHESIS IN HUMANS
    Michael Becker; Fiscal Year: 2001
    ....
  7. Effects of antipsychotic drugs on brain and behavior
    FRANK TARAZI; Fiscal Year: 2005
    ..adult rats, and should evolve new principles for improved treatments for childhood-onset schizophrenia and other major pediatric psychiatric disorders. ..
  8. Treatment Outcome of Vascular Depression
    Yvette Sheline; Fiscal Year: 2005
    ..The proposed trial will provide information of value to the practitioner and also provide data to build a more comprehensive model of the prognostic impact of frontal-subcortical brain changes on the outcome of late-life depression. ..
  9. Transdisciplinary Imaging Genetics Center (1 of 2)(RMI)
    Steven Potkin; Fiscal Year: 2006
    ..The new knowledge generated by the Center holds considerable promise for improving diagnosis and treatment of mental illness. [unreadable] [unreadable]..
  10. OU Developmental Center for Injury Prevention Research
    Gary Raskob; Fiscal Year: 2005
    ..abstract_text> ..
  11. Hybrid Drugs: Novel Pharmacotherapy for ADHD
    FRANK TARAZI; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  12. Neuroimaging in Depression Treatment Studies
    Yvette Sheline; Fiscal Year: 2006
    ..abstract_text> ..
  13. Center For Aging
    John Morris; Fiscal Year: 2006
    ..Dr. Morris is firmly committed to accomplishing these aims and, with this award and with outstanding institutional support, to establishing a preeminent Center for Aging at Washington University. ..
  14. INTERESTING BIOACTIVE SUBSTANCES
    David Williams; Fiscal Year: 2006
    ..The selective synthesis of contiguous stereotriads will advance basic methodology for asymmetric conjugate additions. ..
  15. Phase I Clinical Trials of Anti-Cancer Agents
    Francis Giles; Fiscal Year: 2007
    ..abstract_text> ..
  16. PET Amyloid Plaque Imaging in Late Life Depression
    Yvette Sheline; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable] [unreadable]..
  17. Alzheimer's Diagnosis by Real-Time Motion Corrected FMRI
    Clifford Jack; Fiscal Year: 2004
    ..Aim number 4: to assess motion corrected fMRI as a diagnostic test for early Alzheimer's disease. ..
  18. OU Human Research Protection Program, Year 2
    Gary Raskob; Fiscal Year: 2003
    ..The University of Oklahoma is committed to maintaining these initiatives after the term of this award. ..
  19. Desferrithiocin Analogue Actinide Decorporation Agents
    RAYMOND BERGERON; Fiscal Year: 2008
    ..abstract_text> ..
  20. IRON CHELATORS PREDICATED ON DESFERRITHIOCIN
    RAYMOND BERGERON; Fiscal Year: 2004
    ....
  21. Vascular Depression: Longitudinal Followup
    Yvette I Sheline; Fiscal Year: 2010
    ..The proposal will provide important new data on neuroradiologic and neuropsychological factors contributing to recurrent or chronic depression in older individuals. ..
  22. Novel pharmacotherapies for treatment of ADHD
    FRANK TARAZI; Fiscal Year: 2003
    ..Expected findings should evolve new principles and lead to novel compounds that can be used as much-needed innovative treatments for ADHD and other major neuropsychiatric disorders. ..
  23. Norepinephrine Transporters: Targets for ADHD
    FRANK TARAZI; Fiscal Year: 2004
    ..Expected findings should lead to novel compounds that can be developed as much needed innovative non-stimulant treatments for ADHD and other major neuropsychiatric disorders. ..
  24. Discovery of a Selective Agent that Activates PON1 Enzymatic Activity
    John Scott; Fiscal Year: 2007
    ..Atherosclerosis is the number one cause of mortality in Western societies. This research proposal focuses on generating research tools to evaluate a novel therapeutic strategy to prevent atherosclerosis. ..
  25. Magnetic Resonance Imaging of Alzheimer's Amyloid Plaque
    JOSEPH PODUSLO; Fiscal Year: 2007
    ..unreadable] [unreadable]..
  26. Bioreactor Expansion and Transplantation of ES Cell Derived Osteoblasts and Chond
    John Matyas; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  27. Bipolar II Depression: Lithium, SSRI, or the Combination
    Trisha Suppes; Fiscal Year: 2010
    ..We also hypothesize that the frequency of side effects will be significantly less in patients on SSRI monotherapy. Thus, secondary aims include assessment of patient satisfaction, which may affect compliance in the clinical setting. ..
  28. Mechanisms for hypoxic Ca2+ release in pulmonary artery myocytes
    Yong Xiao Wang; Fiscal Year: 2010
    ..The findings from this proposal will enhance our understanding of cellular molecular mechanisms for hypoxic [Ca2+]i rise in PASMCs and associated HPV, and may lead to identify potential novel targets to treat pulmonary hypertension. ..
  29. Chemopreventive Effect of NSAIDs Against Prostate Cancer
    Bhagavathi Narayanan; Fiscal Year: 2009
    ..Clear delineation of the chemopreventive efficacy of celecoxib and exisulind in this preclinical model of prostate cancer will allow the rational design of human clinical trials. ..
  30. Hepcidin and the pathogenesis of anemia in older adults.
    Richard D Semba; Fiscal Year: 2010
    ..This study should provide new insight into the epidemiology and biological mechanisms of anemia among older adults and help identify strategies aimed at the prevention and treatment of anemia. ..
  31. Amyloid Imaging Agents for Position Emission Tomography
    Chester A Mathis; Fiscal Year: 2010
    ....
  32. Molecular and Functional Imaging of Age Related Cognitive Decline
    William Jagust; Fiscal Year: 2009
    ....
  33. Effects of Chemotherapy on Brain Function
    William J Jagust; Fiscal Year: 2010
    ..They are also relevant to the overall mission of the NIH because of the negative impact that cognitive dysfunction has on quality of life. ..
  34. PET Insert for MAGNETOM Trio
    Chester Mathis; Fiscal Year: 2008
    ..unreadable] [unreadable] PUBLIC HEALTH RELEVANCE: [unreadable] [unreadable] [unreadable]..
  35. Amyloid Imaging in Frontotemporal Dementia and Alzheimer's Disease
    William Jagust; Fiscal Year: 2009
    ..PIB could become a diagnostic tool that is useful in diagnosing AD and FTLD during life. This will be especially important as new treatments for both disorders are developed. ..
  36. Predicting Melanoma Response to BAY 43-9006/Chemotherapy
    Harriet Kluger; Fiscal Year: 2008
    ..We will assess individual markers as well as panels of markers. [unreadable] [unreadable]..
  37. Yersiniabactin and plague pathogenesis
    Robert Perry; Fiscal Year: 2008
    ..abstract_text> ..
  38. Enterogenesis with the Use of an Implanted Mechanotransduction Device
    Daniel Teitelbaum; Fiscal Year: 2008
    ..Knowledge gained from this project could greatly improve the care of patients who suffer from short bowel syndrome. [unreadable] [unreadable] [unreadable]..
  39. COMT genotype and response to cognitive remediation in schizophrenia
    Jean Pierre Lindenmayer; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable] [unreadable] [unreadable]..
  40. Bipolar Statistical Summit:Methodologies to Advance Long Term Intervention Trials
    Charles Bowden; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  41. High End Computing for PET/SPECT
    DEAN WONG; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  42. Pharmacotherapy for Minor Depression
    Robert Howland; Fiscal Year: 2004
    ..The results of this study will have profound public health implications by improving our understanding of the efficacy of SJW and standard antidepressants for the treatment of MinorD. ..
  43. IMAGING DOPAMINE RELEASE/ENDOCRINE CHANGES IN ALCOHOLISM
    DEAN WONG; Fiscal Year: 2004
    ..If the initial D2 receptor deficits are exacerbated by alcohol abuse one can envision a positive feedback loop hard to break. ..
  44. BACTERIAL MODULATION OF LUNG INFLAMMATORY RESPONSE
    Thomas Russo; Fiscal Year: 2004
    ..g. hemolysin) and bacterially induced host response elements in directly mediating the pathogenesis of lung injury. ..
  45. Dedicated High Performance Human Brain/Preclinical PET
    DEAN WONG; Fiscal Year: 2004
    ..abstract_text> ..
  46. P21 transcriptional inhibitors as proapoptotic compounds
    Andrei Gartel; Fiscal Year: 2003
    ..This study may improve treatment of cancer by leading to the identification of new compounds that will increase the efficiency of cell death promoting anticancer drugs for cancer treatment. ..
  47. Poly (ADP-Ribose) synthetase in expression of endothelia
    Basilia Zingarelli; Fiscal Year: 2003
    ..abstract_text> ..
  48. TRAINING IN ALCOHOL AND NEURODEGENERATIVE DISEASE
    MARIETA HEATON; Fiscal Year: 2002
    ..abstract_text> ..
  49. IMAGING DOPAMINE/SEROTONIN MECHANISMS IN COCAINE CRAVING
    DEAN WONG; Fiscal Year: 2003
    ..Testing of these hypotheses will provide novel and fundamental answers to craving mechanisms. ..
  50. TREATMENT OF BEHAVIORAL SYMPTOMS IN ALZHEIMERS DISEASE
    Davangere Devanand; Fiscal Year: 2001
    ..These clinical data will be important in improving the management of AD patients with behavioral complications. ..
  51. 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. ..
  52. Correlative Imaging of Tumor Angiogenesis
    Sanjiv Gambhir; Fiscal Year: 2004
    ..We plan to perform pharmacokinetics and toxicology studies with preclinical materials and prepare an agent for gamma and SPECT imaging in clinical studies and file an IRB for cancer angiogenesis evaluation. ..
  53. Iron Deficiency and Anemia in HIV and HCV-Infected Women
    Richard Semba; Fiscal Year: 2005
    ..S. and elsewhere. ..
  54. Academy of Molecular Imaging 2006 Annual Meeting
    Sanjiv Gambhir; Fiscal Year: 2006
    ..The annual conference is being held March 25-29, 2006 at the Gaylord Palms Resort Hotel and Convention Center in Orlando, Florida. [unreadable] [unreadable] [unreadable]..
  55. A screen for small molecule inhibitors of soluble Abeta oligomer assembly
    Harry LeVine; Fiscal Year: 2007
    ..Anti-oligomer compounds could potentially block the cognitive impairment symptoms that oligomers elicit in animal models and interfere with the progression of Alzheimer's disease. [unreadable] [unreadable] [unreadable]..
  56. Heterogeneity of hypoxic Ca2+ release in pulmonary and *
    Yong Xiao Wang; Fiscal Year: 2006
    ..The proposed studies are also of fundamental physiological significance with respect to the regulation of Ca2+ release in other cell types. ..
  57. ADJUNCT VITAMIN A THERAPY FOR TUBERCULOSIS AND HIV/AIDS
    Richard Semba; Fiscal Year: 2005
    ....
  58. Expression of Proapoptotic Genes for Cancer Therapy
    Bingliang Fang; Fiscal Year: 2006
    ..Success of the proposed studies will lead to new therapeutics for refractory metastatic disease. It will also provide insight into mechanisms of resistance to apoptosis induction in cancer cells. ..
  59. VITAMIN A SUPPLEMENTATION FOR HIV INFECTED CHILDREN
    Richard Semba; Fiscal Year: 2002
    ....
  60. Development of PET radioligands for cerebral cannabinoid receptor (CB1)
    ANDREW HORTI; Fiscal Year: 2008
    ....
  61. Antipsychotic Discontinuation in Alzheimer s Disease
    Davangere Devanand; Fiscal Year: 2008
    ..The results will be of considerable value to the practicing clinician and have substantial implications for the regulatory oversight of elder care. ..
  62. Oxidative Stress and the Pathogenesis of Sarcopenia and Disability in Older Women
    Richard Semba; Fiscal Year: 2008
    ..AGEs are a potentially modifiable risk factor, as circulating AGEs can be lowered by dietary modification and by pharmacological intervention. ..
  63. Reconstruction of skin model containing Langerhans cells
    Seyoum Ayehunie; Fiscal Year: 2003
    ..Finally, based on these studies, an assay kit to predict whether a material is likely to act as a contact allergen will be developed. ..
  64. EFFECTS OF AGING & PGP ON AB EFFLUX FROM THE BRAIN
    ANNE FAGAN NIVEN; Fiscal Year: 2005
    ..Support for the hypothesis would establish a role for age-dependent defects in A-beta clearance from the brain in the pathogenesis of AD and, importantly, provide a novel therapeutic target for treatment of the disease. ..
  65. Antitumor Mechanisms of SRC Inhibitors in Lung Cancer
    Eric Haura; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  66. Host factors involved in viral RNA recombination
    Peter Nagy; Fiscal Year: 2006
    ..Knowledge of recombination promises untold health benefits by providing means to limit virus infections and to develop safer vaccines. ..
  67. Dissecting the mechanism of viral RNA recombination
    Peter Nagy; Fiscal Year: 2004
    ..Knowledge of recombination promises untold health benefits by providing means to limit virus infections and safer vaccines. ..
  68. NUCLEOSIDE ANALOGS AS ANTICANCER COMPOUNDS
    Yung Chi Cheng; Fiscal Year: 2007
    ..It should yield novel information for understanding the biochemical determinants of the action of L-OddC, the biochemistry of the enzymes studied and possible novel use of L-OddC for the treatment of solid tumor. ..
  69. Role of an essential RNA chaperone in virus replication
    Peter Nagy; Fiscal Year: 2006
    ....
  70. MODELS FOR TESTING CANDIDATE TOPICAL MICROBICIDES FOR CYTOTOXICITY AND ACTIVITY A
    Mary Lampe; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..