- 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...
- 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...
- 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...
- 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
- 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
- Small-molecule correctors of defective DeltaF508-CFTR cellular processing identified by high-throughput screening
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...
- Efficacy and tolerability of mirabegron, a β(3)-adrenoceptor agonist, in patients with overactive bladder: results from a randomised European-Australian phase 3 trial
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)...
- 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
- Effect of environmental factors on the kinetics of insulin fibril formation: elucidation of the molecular mechanism
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...
- 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...
- Dasatinib (BMS-354825) targets an earlier progenitor population than imatinib in primary CML but does not eliminate the quiescent fraction
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...
- 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...
- 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...
- 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...
- 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...
- 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...
- Manipulation of alternative splicing by a newly developed inhibitor of Clks
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
- In vitro and in vivo activity of SKI-606, a novel Src-Abl inhibitor, against imatinib-resistant Bcr-Abl+ neoplastic cells
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...
- 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...
- 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
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...
- Peroxisome proliferator-activated receptor β/δ agonism protects the kidney against ischemia/reperfusion injury in diabetic rats
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...
- 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...
- 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
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...
- Dasatinib, a multi-kinase inhibitor increased radiation sensitivity by interfering with nuclear localization of epidermal growth factor receptor and by blocking DNA repair pathways
University of Texas M D Anderson Cancer Center, Houston, TX 77030, USA
Radiother Oncol 105:241-9. 2012
- Neonicotinoid insecticide toxicology: mechanisms of selective action
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...
- 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...
- 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...
- 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...
- 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...
- Dasatinib: a potent SRC inhibitor in clinical development for the treatment of solid tumors
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...
- 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...
- PPARdelta modulates lipopolysaccharide-induced TNFalpha inflammation signaling in cultured cardiomyocytes
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...
- Evidence for the role of peroxisome proliferator-activated receptor-beta/delta in the development of spinal cord injury
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...
- 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...
- 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...
- Measurement of cellular 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reduction activity and lactate dehydrogenase release using MTT
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...
- Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias
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)...
- 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...
- 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...
- Arabidopsis local resistance to Botrytis cinerea involves salicylic acid and camalexin and requires EDS4 and PAD2, but not SID2, EDS5 or PAD4
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...
- Selectivity of febuxostat, a novel non-purine inhibitor of xanthine oxidase/xanthine dehydrogenase
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...
- Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity
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...
- 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)...
- 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...
- Bead-based profiling of tyrosine kinase phosphorylation identifies SRC as a potential target for glioblastoma therapy
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...
- 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...
- Protein synthesis is resistant to rapamycin and constitutes a promising therapeutic target in acute myeloid leukemia
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...
- 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...
- Solution conformations and dynamics of ABL kinase-inhibitor complexes determined by NMR substantiate the different binding modes of imatinib/nilotinib and dasatinib
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...
- Activation of MAPK kinase 9 induces ethylene and camalexin biosynthesis and enhances sensitivity to salt stress in Arabidopsis
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...
- Risk assessment for side-effects of neonicotinoids against bumblebees with and without impairing foraging behavior
Laboratory of Cellular Genetics, Department of Biology, Faculty of Sciences, Free University of Brussels, Brussels, Belgium
Ecotoxicology 19:207-15. 2010
- Effects of food on the pharmacokinetics of edoxaban, an oral direct factor Xa inhibitor, in healthy volunteers
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...
- Design and synthesis of C-2 substituted thiazolo and dihydrothiazolo ring-fused 2-pyridones: pilicides with increased antivirulence activity
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...
- 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
- 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...
- 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...
- An extremely potent inhibitor of xanthine oxidoreductase. Crystal structure of the enzyme-inhibitor complex and mechanism of inhibition
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...
- 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...
- CPTH6, a thiazole derivative, induces histone hypoacetylation and apoptosis in human leukemia cells
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...
- 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
- Oxidative stress is involved in Dasatinib-induced apoptosis in rat primary hepatocytes
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...
- Use of xanthine oxidase inhibitor febuxostat inhibits renal interstitial inflammation and fibrosis in unilateral ureteral obstructive nephropathy
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...
- 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...
- 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...
- Epidemiology and control of intestinal parasites with nitazoxanide in children in Mexico
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...
- An improved 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) reduction assay for evaluating the viability of Escherichia coli cells
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...
- 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...
- 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...
- Assays for studying nucleated aggregation of polyglutamine proteins
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...
- 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...
- Mirabegron, a β₃-adrenoceptor agonist for the potential treatment of urinary frequency, urinary incontinence or urgency associated with overactive bladder
William Beaumont Hospital, Department of Urology, 3811 West 13 Mile Road, Royal Oak, MI 48073, USA
IDrugs 13:713-22. 2010
- 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...
- 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...
- Activities of SYK and PLCgamma2 predict apoptotic response of CLL cells to SRC tyrosine kinase inhibitor dasatinib
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...
- 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...
- Rapid analysis of neonicotinoid insecticides in guttation drops of corn seedlings obtained from coated seeds
Universita degli Studi di Padova, Dipartimento di Scienze Chimiche, Via Marzolo 1, 35131 Padova, Italy
J Environ Monit 13:1564-8. 2011
- Dasatinib as first-line treatment for adult patients with Philadelphia chromosome-positive acute lymphoblastic leukemia
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...
- Role of the Yersinia pestis yersiniabactin iron acquisition system in the incidence of flea-borne plague
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...
- 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...
- 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...
- 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...
- Allosteric drugs: the interaction of antitumor compound MKT-077 with human Hsp70 chaperones
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...
- 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)...
- The tyrosine kinase inhibitor dasatinib dysregulates bone remodeling through inhibition of osteoclasts in vivo
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...
- 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...
- 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
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...
- Interaction of mGlu2/3 agonism with clozapine and lurasidone to restore novel object recognition in subchronic phencyclidine-treated rats
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...
- Congo red and thioflavin-T analogs detect Abeta oligomers
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...
- Identification of candidate molecular markers predicting sensitivity in solid tumors to dasatinib: rationale for patient selection
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...
- 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
- Cross-resistance study and biochemical mechanisms of thiamethoxam resistance in B-biotype Bemisia tabaci (Hemiptera: Aleyrodidae)
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...
- Resveratrol inhibits beta-amyloid oligomeric cytotoxicity but does not prevent oligomer formation
Tsinghua University School of Medicine, Haidian District, Beijing 100084, China
Neurotoxicology 30:986-95. 2009
- Mechanism of thioflavin T binding to amyloid fibrils
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...
- The role of Src in prostate cancer
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...
- 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...
- Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT
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...
- 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...
- Lurasidone in the treatment of acute schizophrenia: a double-blind, placebo-controlled trial
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...
- 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
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...
- 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
- Fibrillar aggregates of the tumor suppressor p53 core domain
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...