benzimidazoles

Summary

Summary: Compounds with a BENZENE fused to IMIDAZOLES.

Top Publications

  1. doi Effects of the angiotensin-receptor blocker telmisartan on cardiovascular events in high-risk patients intolerant to angiotensin-converting enzyme inhibitors: a randomised controlled trial
    S Yusuf
    Lancet 372:1174-83. 2008
  2. ncbi Dabigatran versus warfarin in patients with atrial fibrillation
    Stuart J Connolly
    Population Health Research Institute, McMaster University and Hamilton Health Sciences, Hamilton, ON, Canada
    N Engl J Med 361:1139-51. 2009
  3. ncbi Calmodulin-dependent protein kinase kinase-beta is an alternative upstream kinase for AMP-activated protein kinase
    Simon A Hawley
    Division of Molecular Physiology University of Dundee, Dundee, Scotland, United Kingdom
    Cell Metab 2:9-19. 2005
  4. ncbi The Ca2+/calmodulin-dependent protein kinase kinases are AMP-activated protein kinase kinases
    Rebecca L Hurley
    Departments of Medicine and Biochemistry, Dartmouth Medical School and the Department of Biological Sciences, Dartmouth College, Hanover, NH 03755, USA
    J Biol Chem 280:29060-6. 2005
  5. ncbi Ca2+/calmodulin-dependent protein kinase kinase-beta acts upstream of AMP-activated protein kinase in mammalian cells
    Angela Woods
    Cellular Stress Group, MRC Clinical Sciences Centre, Imperial College, Hammersmith Hospital, Du Cane Road, London W12 0NN, United Kingdom
    Cell Metab 2:21-33. 2005
  6. ncbi Reversal of rivaroxaban and dabigatran by prothrombin complex concentrate: a randomized, placebo-controlled, crossover study in healthy subjects
    Elise S Eerenberg
    Department of Vascular Medicine, Academic Medical Center, Meibergdreef 9, 1105 AZ Amsterdam, Netherlands
    Circulation 124:1573-9. 2011
  7. ncbi Effects of candesartan on mortality and morbidity in patients with chronic heart failure: the CHARM-Overall programme
    Marc A Pfeffer
    Cardiovascular Division, Brigham and Women s Hospital, 75 Francis Street, Boston, MA 02115, USA
    Lancet 362:759-66. 2003
  8. ncbi Risk of bleeding with 2 doses of dabigatran compared with warfarin in older and younger patients with atrial fibrillation: an analysis of the randomized evaluation of long-term anticoagulant therapy (RE-LY) trial
    John W Eikelboom
    Population Health Research Institute, Hamilton Health Sciences and McMaster University, Hamilton, Ontario, Canada
    Circulation 123:2363-72. 2011
  9. ncbi Dabigatran versus warfarin in the treatment of acute venous thromboembolism
    Sam Schulman
    Department of Medicine, McMaster University and Henderson Research Centre, Hamilton, ON, Canada
    N Engl J Med 361:2342-52. 2009
  10. ncbi ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models
    Cherrie K Donawho
    Abbott Laboratories, Abbott Park, Illinois 60064 6074, USA
    Clin Cancer Res 13:2728-37. 2007

Research Grants

Detail Information

Publications356 found, 100 shown here

  1. doi Effects of the angiotensin-receptor blocker telmisartan on cardiovascular events in high-risk patients intolerant to angiotensin-converting enzyme inhibitors: a randomised controlled trial
    S Yusuf
    Lancet 372:1174-83. 2008
    ..We therefore assessed whether the angiotensin-receptor blocker telmisartan would be effective in patients intolerant to ACE inhibitors with cardiovascular disease or diabetes with end-organ damage...
  2. ncbi Dabigatran versus warfarin in patients with atrial fibrillation
    Stuart J Connolly
    Population Health Research Institute, McMaster University and Hamilton Health Sciences, Hamilton, ON, Canada
    N Engl J Med 361:1139-51. 2009
    ..Warfarin reduces the risk of stroke in patients with atrial fibrillation but increases the risk of hemorrhage and is difficult to use. Dabigatran is a new oral direct thrombin inhibitor...
  3. ncbi Calmodulin-dependent protein kinase kinase-beta is an alternative upstream kinase for AMP-activated protein kinase
    Simon A Hawley
    Division of Molecular Physiology University of Dundee, Dundee, Scotland, United Kingdom
    Cell Metab 2:9-19. 2005
    ..Our results suggest a potential Ca(2+)-dependent neuroprotective pathway involving phosphorylation and activation of AMPK by CaMKKbeta...
  4. ncbi The Ca2+/calmodulin-dependent protein kinase kinases are AMP-activated protein kinase kinases
    Rebecca L Hurley
    Departments of Medicine and Biochemistry, Dartmouth Medical School and the Department of Biological Sciences, Dartmouth College, Hanover, NH 03755, USA
    J Biol Chem 280:29060-6. 2005
    ..These data indicate that the CaMKKs function in intact cells as AMPKKs, predicting wider roles for these kinases in regulating AMPK activity in vivo...
  5. ncbi Ca2+/calmodulin-dependent protein kinase kinase-beta acts upstream of AMP-activated protein kinase in mammalian cells
    Angela Woods
    Cellular Stress Group, MRC Clinical Sciences Centre, Imperial College, Hammersmith Hospital, Du Cane Road, London W12 0NN, United Kingdom
    Cell Metab 2:21-33. 2005
    ..These results demonstrate that AMPK is regulated by at least two upstream kinases and suggest that AMPK may play a role in Ca(2+)-mediated signal transduction pathways...
  6. ncbi Reversal of rivaroxaban and dabigatran by prothrombin complex concentrate: a randomized, placebo-controlled, crossover study in healthy subjects
    Elise S Eerenberg
    Department of Vascular Medicine, Academic Medical Center, Meibergdreef 9, 1105 AZ Amsterdam, Netherlands
    Circulation 124:1573-9. 2011
    ..This study evaluated the potential of prothrombin complex concentrate (PCC) to reverse the anticoagulant effect of these drugs...
  7. ncbi Effects of candesartan on mortality and morbidity in patients with chronic heart failure: the CHARM-Overall programme
    Marc A Pfeffer
    Cardiovascular Division, Brigham and Women s Hospital, 75 Francis Street, Boston, MA 02115, USA
    Lancet 362:759-66. 2003
    ..Patients with chronic heart failure (CHF) are at high risk of cardiovascular death and recurrent hospital admissions. We aimed to find out whether the use of an angiotensin-receptor blocker could reduce mortality and morbidity...
  8. ncbi Risk of bleeding with 2 doses of dabigatran compared with warfarin in older and younger patients with atrial fibrillation: an analysis of the randomized evaluation of long-term anticoagulant therapy (RE-LY) trial
    John W Eikelboom
    Population Health Research Institute, Hamilton Health Sciences and McMaster University, Hamilton, Ontario, Canada
    Circulation 123:2363-72. 2011
    ..The purpose of this study was to compare their risks of bleeding in the Randomized Evaluation of Long-Term Anticoagulant Therapy (RE-LY) trial...
  9. ncbi Dabigatran versus warfarin in the treatment of acute venous thromboembolism
    Sam Schulman
    Department of Medicine, McMaster University and Henderson Research Centre, Hamilton, ON, Canada
    N Engl J Med 361:2342-52. 2009
    ..The direct oral thrombin inhibitor dabigatran has a predictable anticoagulant effect and may be an alternative therapy to warfarin for patients who have acute venous thromboembolism...
  10. ncbi ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models
    Cherrie K Donawho
    Abbott Laboratories, Abbott Park, Illinois 60064 6074, USA
    Clin Cancer Res 13:2728-37. 2007
    ..To evaluate the preclinical pharmacokinetics and antitumor efficacy of a novel orally bioavailable poly(ADP-ribose) polymerase (PARP) inhibitor, ABT-888...
  11. ncbi Effects of candesartan in patients with chronic heart failure and preserved left-ventricular ejection fraction: the CHARM-Preserved Trial
    Salim Yusuf
    McMaster Clinic, Room 252, Hamilton General Hospital, 237 Barton Street East, ON, L8L 2X2, Hamilton, Canada
    Lancet 362:777-81. 2003
    ..We investigated the effect of addition of an angiotensin-receptor blocker to current treatments...
  12. ncbi Dabigatran etexilate--a novel, reversible, oral direct thrombin inhibitor: interpretation of coagulation assays and reversal of anticoagulant activity
    Joanne van Ryn
    Department of Drug Discovery Support, Boehringer Ingelheim Pharma GmbH and Co KG, Biberach an der Riss, Germany
    Thromb Haemost 103:1116-27. 2010
    ....
  13. ncbi Dabigatran association with higher risk of acute coronary events: meta-analysis of noninferiority randomized controlled trials
    Ken Uchino
    Cerebrovascular Center, Neurological Institute, Cleveland Clinic, 9500 Euclid Ave, Mail Code S80, Cleveland, OH 44195, USA
    Arch Intern Med 172:397-402. 2012
    ..We systematically evaluated the risk of MI or acute coronary syndrome (ACS) with the use of dabigatran...
  14. ncbi The use of dabigatran immediately after atrial fibrillation ablation
    Roger A Winkle
    Cardiovascular Medicine and Cardiac Arrhythmias, E Palo Alto, Sequoia Hospital, Redwood City, California, USA
    J Cardiovasc Electrophysiol 23:264-8. 2012
    ..Dabigatran is a new anticoagulant and may be useful after AF ablation to prevent thromboembolic events...
  15. ncbi Identification of telmisartan as a unique angiotensin II receptor antagonist with selective PPARgamma-modulating activity
    Stephen C Benson
    Department of Biological Sciences, California State University, Hayward, USA
    Hypertension 43:993-1002. 2004
    ....
  16. ncbi Efficacy and safety of dabigatran compared with warfarin at different levels of international normalised ratio control for stroke prevention in atrial fibrillation: an analysis of the RE-LY trial
    Lars Wallentin
    Uppsala Clinical Research Centre, Uppsala University, Uppsala, Sweden
    Lancet 376:975-83. 2010
    ..We aimed to investigate the primary and secondary outcomes of the RE-LY trial in relation to each centre's mean TTR (cTTR) in the warfarin population...
  17. ncbi Clinical pharmacokinetics and pharmacodynamics of the oral direct thrombin inhibitor dabigatran etexilate
    Joachim Stangier
    Boehringer Ingelheim Pharma GmbH and Co KG, Biberach, Germany
    Clin Pharmacokinet 47:285-95. 2008
    ....
  18. ncbi Feasibility and safety of dabigatran versus warfarin for periprocedural anticoagulation in patients undergoing radiofrequency ablation for atrial fibrillation: results from a multicenter prospective registry
    Dhanunjaya Lakkireddy
    Division of Cardiovascular Diseases, Cardiovascular Research Institute, Mid America Cardiology, University of Kansas Hospital and Medical Center, 3901 Rainbow Boulevard, Kansas City, KS 66160 7200, USA
    J Am Coll Cardiol 59:1168-74. 2012
    ..The purpose of this study was to evaluate the feasibility and safety of periprocedural dabigatran during atrial fibrillation (AF) ablation...
  19. pmc Cost-effectiveness of dabigatran etexilate for the prevention of stroke and systemic embolism in UK patients with atrial fibrillation
    Anuraag R Kansal
    United BioSource Corporation, Bethesda, Maryland, USA
    Heart 98:573-8. 2012
    ..To assess the cost-effectiveness of dabigatran etexilate, a new oral anticoagulant, versus warfarin and other alternatives for the prevention of stroke and systemic embolism in UK patients with atrial fibrillation (AF)...
  20. ncbi Dabigatran versus warfarin in patients with atrial fibrillation: an analysis of patients undergoing cardioversion
    Rangadham Nagarakanti
    Louisiana State University School of Medicine, New Orleans, LA, USA
    Circulation 123:131-6. 2011
    ..The Randomized Evaluation of Long-Term Anticoagulation Therapy (RE-LY) trial compared dabigatran 110 mg BID (D110) and 150 mg BID (D150) with warfarin for stroke prevention in 18 113 patients with nonvalvular atrial fibrillation...
  21. ncbi Dabigatran etexilate versus enoxaparin for prevention of venous thromboembolism after total hip replacement: a randomised, double-blind, non-inferiority trial
    Bengt I Eriksson
    Department of Orthopaedic Surgery, Sahlgrenska University Hospital Ostra, Gothenburg, Sweden
    Lancet 370:949-56. 2007
    ..After hip replacement surgery, prophylaxis following discharge from hospital is recommended to reduce the risk of venous thromboembolism. Our aim was to assess the oral, direct thrombin inhibitor dabigatran etexilate for such prophylaxis...
  22. ncbi Dabigatran versus enoxaparin for prevention of venous thromboembolism after hip or knee arthroplasty: a pooled analysis of three trials
    R J Friedman
    Medical University of South Carolina and Charleston Orthopedic Associates, Charleston, South Carolina 29414, USA
    Thromb Res 126:175-82. 2010
    ..Three randomized, double-blind trials compared dabigatran, an oral direct thrombin inhibitor, with enoxaparin for the primary prevention of venous thromboembolism (VTE) in patients undergoing elective total hip and knee arthroplasty...
  23. ncbi Rationale and design of RE-LY: randomized evaluation of long-term anticoagulant therapy, warfarin, compared with dabigatran
    Michael D Ezekowitz
    Lankenau Institute for Medical Research and The Heart Center, Wynnewood, PA, USA
    Am Heart J 157:805-10, 810.e1-2. 2009
    ..The worldwide site distribution and broad range of stroke risk further increase the general applicability of the trial. Results are expected in 2009...
  24. ncbi Oral thrombin inhibitor dabigatran etexilate vs North American enoxaparin regimen for prevention of venous thromboembolism after knee arthroplasty surgery
    Jeffrey S Ginsberg
    McMaster University Medical Centre, Ontario, Canada
    J Arthroplasty 24:1-9. 2009
    ..Dabigatran, effective compared to once-daily enoxaparin, showed inferior efficacy to the twice-daily North American enoxaparin regimen, probably because of the latter's more intense and prolonged dosing...
  25. ncbi AZD6244 (ARRY-142886), a potent inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 1/2 kinases: mechanism of action in vivo, pharmacokinetic/pharmacodynamic relationship, and potential for combination in preclinical
    Barry R Davies
    Cancer and Infection Research Area, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom
    Mol Cancer Ther 6:2209-19. 2007
    ..Moreover, enhanced antitumor efficacy can be obtained by combining AZD6244 with the cytotoxic drugs irinotecan or docetaxel...
  26. pmc The pharmacokinetics, pharmacodynamics and tolerability of dabigatran etexilate, a new oral direct thrombin inhibitor, in healthy male subjects
    Joachim Stangier
    Boehringer Ingelheim Pharma GmbH and Co KG, Ingelheim, Germany
    Br J Clin Pharmacol 64:292-303. 2007
    ..Two double-blind, randomized trials were undertaken to investigate the pharmacokinetics (PK), pharmacodynamics (PD) and tolerability of orally administered dabigatran etexilate in healthy male subjects...
  27. ncbi The metabolism and disposition of the oral direct thrombin inhibitor, dabigatran, in humans
    Stefan Blech
    Boehringer Ingelheim Pharma GmbH and Co KG, Department of Drug Metabolism and Pharmacokinetics, Biberach, Germany
    Drug Metab Dispos 36:386-99. 2008
    ..o. administration of dabigatran etexilate and that the potential for clinically relevant interactions between dabigatran and drugs metabolized by cytochrome P450 is low...
  28. ncbi Cost-effectiveness of dabigatran for stroke prophylaxis in atrial fibrillation
    Shimoli V Shah
    Department of Medicine, Washington University School of Medicine, Campus Box 8005, 660 S Euclid Ave, St Louis, MO 63110, USA
    Circulation 123:2562-70. 2011
    ..Recent studies have investigated alternatives to warfarin for stroke prophylaxis in patients with atrial fibrillation (AF), but whether these alternatives are cost-effective is unknown...
  29. pmc Telmisartan to prevent recurrent stroke and cardiovascular events
    Salim Yusuf
    Population Health Research Institute, McMaster University, Hamilton, ON, Canada
    N Engl J Med 359:1225-37. 2008
    ..We evaluated the effects of therapy with an angiotensin-receptor blocker, telmisartan, initiated early after a stroke...
  30. ncbi Dovitinib induces apoptosis and overcomes sorafenib resistance in hepatocellular carcinoma through SHP-1-mediated inhibition of STAT3
    Wei Tien Tai
    Department of Medical Research, National Taiwan University Hospital, Chung Shan S Rd, Taipei 100, Taiwan
    Mol Cancer Ther 11:452-63. 2012
    ..In conclusion, dovitinib induces significant apoptosis in HCC cells and sorafenib-resistant cells via SHP-1-mediated inhibition of STAT3...
  31. ncbi An indirect comparison of dabigatran, rivaroxaban and apixaban for atrial fibrillation
    Simon Mantha
    Department of Hematology, Lahey Clinic, Burlington, MA 01805, USA
    Thromb Haemost 108:476-84. 2012
    ..Such an indirect comparison should be used only to generate hypotheses which need to be tested in a dedicated randomised trial comparing the three drugs directly...
  32. ncbi Indirect comparisons of new oral anticoagulant drugs for efficacy and safety when used for stroke prevention in atrial fibrillation
    Gregory Y H Lip
    University of Birmingham Centre for Cardiovascular Sciences, City Hospital, Birmingham, UK
    J Am Coll Cardiol 60:738-46. 2012
    ..This study sought to perform an indirect comparison analysis of dabigatran etexilate (2 doses), rivaroxaban, and apixaban for their relative efficacy and safety against each other...
  33. ncbi Basal and treatment-induced activation of AKT mediates resistance to cell death by AZD6244 (ARRY-142886) in Braf-mutant human cutaneous melanoma cells
    Y N Vashisht Gopal
    Departments of Melanoma Medical Oncology, The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, USA
    Cancer Res 70:8736-47. 2010
    ....
  34. pmc Phase I pharmacokinetic and pharmacodynamic study of the oral, small-molecule mitogen-activated protein kinase kinase 1/2 inhibitor AZD6244 (ARRY-142886) in patients with advanced cancers
    Alex A Adjei
    Roswell Park Cancer Institute, Elm and Carlton Streets, Buffalo, NY 14263, USA
    J Clin Oncol 26:2139-46. 2008
    ..To assess the tolerability, pharmacokinetics (PKs), and pharmacodynamics (PDs) of the mitogen-activated protein kinase kinase (MEK) 1/2 inhibitor AZD6244 (ARRY-142886) in patients with advanced cancer...
  35. ncbi Concomitant use of antiplatelet therapy with dabigatran or warfarin in the Randomized Evaluation of Long-Term Anticoagulation Therapy (RE-LY) trial
    Antonio L Dans
    College of Medicine, University of the Philippines Manila, Ermita, Manila, Philippines 1000
    Circulation 127:634-40. 2013
    ..In this subgroup analysis, we assess the efficacy and safety of dabigatran in patients who did and did not receive concomitant antiplatelets...
  36. ncbi Angiotensin type 1 receptor blockers induce peroxisome proliferator-activated receptor-gamma activity
    Michael Schupp
    Center for Cardiovascular Research, Institut fur Pharmakologie und Toxikologie, Campus Charite Mitte, Charite Universitatsmedizin Berlin, Berlin, Germany
    Circulation 109:2054-7. 2004
    ..The peroxisome proliferator-activated receptor-gamma (PPARgamma) is the central regulator of insulin and glucose metabolism improving insulin sensitivity. We investigated the regulation of PPARgamma function by ARBs...
  37. ncbi Low dose of telmisartan prevents ischemic brain damage with peroxisome proliferator-activated receptor-gamma activation in diabetic mice
    Jun Iwanami
    Department of Molecular Cardiovascular Biology and Pharmacology, Ehime University, Graduate School of Medicine, Tohon, Ehime, Japan
    J Hypertens 28:1730-7. 2010
    ..Telmisartan is a unique AT1 receptor blocker with a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonistic action. Activation of PPAR-gamma could prevent inflammation and brain damage...
  38. pmc A distinct "side population" of cells with high drug efflux capacity in human tumor cells
    C Hirschmann-Jax
    Center for Cell and Gene Therapy, Baylor College of Medicine, Methodist Hospital and Texas Children s Hospital, and DeBakey Department of Surgery, One Baylor Plaza, Houston, TX 77030, USA
    Proc Natl Acad Sci U S A 101:14228-33. 2004
    ....
  39. ncbi Canadian Cardiovascular Society atrial fibrillation guidelines 2010: prevention of stroke and systemic thromboembolism in atrial fibrillation and flutter
    John A Cairns
    University of British Columbia, Vancouver, British Columbia, Canada
    Can J Cardiol 27:74-90. 2011
    ..Alternatives to antithrombotic therapies are briefly discussed...
  40. pmc Phase 0 clinical trial of the poly (ADP-ribose) polymerase inhibitor ABT-888 in patients with advanced malignancies
    Shivaani Kummar
    Center for Cancer Research and the Division of Cancer Treatment and Diagnosis, National Cancer Institute, NIH, Bethesda, MD 20892, USA
    J Clin Oncol 27:2705-11. 2009
    ..It was a first-in-human study of the poly (ADP-ribose) polymerase (PARP) inhibitor ABT-888 in patients with advanced malignancies...
  41. ncbi Oxidative stress and nitric oxide synthase in rat diabetic nephropathy: effects of ACEI and ARB
    Maristela Lika Onozato
    Division of Nephrology and Endocrinology, University of Tokyo, Tokyo, Japan
    Kidney Int 61:186-94. 2002
    ..We tested the hypothesis that Ang II subtype 1 (AT1) receptor activation enhances oxidative stress and nitrotyrosine deposition in the kidneys of rats with diabetes mellitus (DM)...
  42. ncbi Dabigatran compared with warfarin in patients with atrial fibrillation and previous transient ischaemic attack or stroke: a subgroup analysis of the RE-LY trial
    Hans Christoph Diener
    Department of Neurology, University Hospital Essen, Essen, Germany
    Lancet Neurol 9:1157-63. 2010
    ..We aimed to assess the effects of dabigatran compared with warfarin in the subgroup of patients with previous stroke or transient ischaemic attack...
  43. ncbi In vitro antagonistic properties of a new angiotensin type 1 receptor blocker, azilsartan, in receptor binding and function studies
    Mami Ojima
    Pharmacology Research Laboratories, Pharmaceutical Research Division, Takeda Pharmaceutical Company, Ltd, Osaka, Japan
    J Pharmacol Exp Ther 336:801-8. 2011
    ..Its tight receptor binding might be expected to produce potent and long-lasting antihypertensive effects in preclinical and clinical settings...
  44. ncbi Influence of renal impairment on the pharmacokinetics and pharmacodynamics of oral dabigatran etexilate: an open-label, parallel-group, single-centre study
    Joachim Stangier
    Boehringer Ingelheim Pharma GmbH and Co KG, Biberach, Germany
    Clin Pharmacokinet 49:259-68. 2010
    ..A decrease in the dose and/or an increase in the administration interval in these patients may be appropriate. In patients with ESRD, dabigatran can be partly removed from the plasma by haemodialysis...
  45. ncbi Cost-effectiveness of dabigatran etexilate for the prevention of stroke and systemic embolism in atrial fibrillation: a Canadian payer perspective
    S V Sorensen
    United BioSource Corporation, Bethesda, Maryland, USA
    Thromb Haemost 105:908-19. 2011
    ..This study demonstrates that dabigatran etexilate is a highly cost-effective alternative to current care for the prevention of stroke and systemic embolism among Canadian AF patients...
  46. ncbi The comparative effects of azilsartan medoxomil and olmesartan on ambulatory and clinic blood pressure
    George L Bakris
    Hypertensive Diseases Unit, University of Chicago Pritzker School of Medicine, Chicago, IL 60637, USA
    J Clin Hypertens (Greenwich) 13:81-8. 2011
    ..0 to -0.1; P=.038), while AZL-M 40 mg was noninferior to OLM-M 40 mg. The side effect profiles of both ARBs were similar to placebo. AZL-M is well tolerated and more efficacious at its maximal dose than the highest dose of OLM-M...
  47. ncbi Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor
    Tammie C Yeh
    Array BioPharma, Inc, Boulder, Colorado 80301, USA
    Clin Cancer Res 13:1576-83. 2007
    ..We have developed a highly potent and selective inhibitor of MEK1/2. The purpose of these studies has been to show the biological efficacy of ARRY-142886 (AZD6244) in enzymatic, cellular, and animal models...
  48. ncbi Cost-effectiveness of dabigatran compared with warfarin for stroke prevention in atrial fibrillation
    James V Freeman
    Stanford University School of Medicine, California, USA
    Ann Intern Med 154:1-11. 2011
    ..Dabigatran is a fixed-dose, oral direct thrombin inhibitor with similar or reduced rates of ischemic stroke and intracranial hemorrhage in patients with AF compared with those of warfarin...
  49. ncbi Inhibition of poly(ADP-ribose) polymerase enhances cell death and improves tumor growth delay in irradiated lung cancer models
    Jeffrey M Albert
    Vanderbilt Ingram Cancer Center, Vanderbilt University School of Medicine, Nashville, Tennessee, USA
    Clin Cancer Res 13:3033-42. 2007
    ..Ionizing radiation induces DNA strand breaks, suggesting that PARP-1 inhibition may sensitize tumor cells to radiation...
  50. pmc Transcriptional pathway signatures predict MEK addiction and response to selumetinib (AZD6244)
    Jonathan R Dry
    Cancer Bioscience, DECS, and Clinical Biomarker Group, AstraZeneca R and D, Alderley Park, Macclesfield, United Kingdom
    Cancer Res 70:2264-73. 2010
    ..These signatures offer useful tools for the study of MEK biology and clinical application of MEK inhibitors, and the novel approaches taken may benefit other targeted therapies...
  51. ncbi Lack of significant effect of bilastine administered at therapeutic and supratherapeutic doses and concomitantly with ketoconazole on ventricular repolarization: results of a thorough QT study (TQTS) with QT-concentration analysis
    Benoit Tyl
    Robert Ballanger s Hospital, Department of Cardiology, Aulnay sous Bois, France
    J Clin Pharmacol 52:893-903. 2012
    ..3 ms; UCL, 12.16 ms). This result was most likely related to the cardiac effect of ketoconazole because for all time points, bilastine plasma concentrations were lower than those observed following the supratherapeutic dose...
  52. ncbi Phase I/II and pharmacodynamic study of dovitinib (TKI258), an inhibitor of fibroblast growth factor receptors and VEGF receptors, in patients with advanced melanoma
    Kevin B Kim
    Department of Melanoma Medical Oncology, The University of Texas MD Anderson Cancer Center, Houston, USA
    Clin Cancer Res 17:7451-61. 2011
    ..This phase I/II dose-escalation study was conducted to evaluate the safety, pharmacodynamics, and preliminary efficacy of dovitinib in the treatment of advanced melanoma...
  53. ncbi In vivo target modulation and biological activity of CHIR-258, a multitargeted growth factor receptor kinase inhibitor, in colon cancer models
    Sang Hoon Lee
    Department of Pharmacology, Chiron Corp, Emeryville, California, USA
    Clin Cancer Res 11:3633-41. 2005
    ..To evaluate the therapeutic and biological effects of CHIR-258, an orally bioavailable, potent inhibitor of class III-V receptor tyrosine kinases, in colon cancer models...
  54. ncbi Twice daily dosing of dabigatran for stroke prevention in atrial fibrillation: a pharmacokinetic justification
    Andreas Clemens
    Boehringer Ingelheim Pharma GmbH and Co KG, Ingelheim, Germany
    Curr Med Res Opin 28:195-201. 2012
    ..Based on its pharmacokinetic profile, dabigatran is dosed twice daily. This analysis provides a quantitative rationale for the selection of the dose regimen in this population...
  55. ncbi Comparison of the efficacy and safety of bilastine 20 mg vs levocetirizine 5 mg for the treatment of chronic idiopathic urticaria: a multi-centre, double-blind, randomized, placebo-controlled study
    T Zuberbier
    Department of Dermatology and Allergy, Charite Universitatsmedizin Berlin, Germany
    Allergy 65:516-28. 2010
    ..The aim of this study was to compare the clinical efficacy and safety of bilastine 20 mg vs levocetirizine 5 mg and placebo in CU patients with moderate-to-severe symptoms...
  56. ncbi A novel poly(ADP-ribose) polymerase inhibitor, ABT-888, radiosensitizes malignant human cell lines under hypoxia
    Stanley K Liu
    Department of Radiation Oncology, University of Toronto, Ont, Canada
    Radiother Oncol 88:258-68. 2008
    ..To our knowledge, this is the first study to demonstrate that inhibition of PARP activity can sensitize hypoxic cancer cells and the combination of IR-PARPi has the potential to improve the therapeutic ratio of radiotherapy...
  57. ncbi Pharmacology, pharmacokinetics, and pharmacodynamics of dabigatran etexilate, an oral direct thrombin inhibitor
    Joachim Stangier
    Department of Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharma GmbH and Co KG, Birkendorfer Strasse, Biberach an der Riss, Germany
    Clin Appl Thromb Hemost 15:9S-16S. 2009
    ....
  58. ncbi Targeted inhibition of the extracellular signal-regulated kinase kinase pathway with AZD6244 (ARRY-142886) in the treatment of hepatocellular carcinoma
    Hung Huynh
    Laboratory of Molecular Endocrinology, Division of Cellular and Molecular Research, National Cancer Centre of Singapore, Singapore 169610, Singapore
    Mol Cancer Ther 6:138-46. 2007
    ..Targeted inhibition of the MEK-ERK pathway with AZD6244 may represent an alternative approach for the treatment of this disease...
  59. ncbi Comparison of the efficacy and safety of bilastine 20 mg vs desloratadine 5 mg in seasonal allergic rhinitis patients
    C Bachert
    Department of Oto Rhino Laryngology, Ghent University Hospital, Ghent, Belgium
    Allergy 64:158-65. 2009
    ..The objective of this study was to compare the efficacy and safety of bilastine 20 mg vs placebo and desloratadine 5 mg in subjects with seasonal allergic rhinitis (SAR)...
  60. ncbi Efficacy and safety of bilastine 20 mg compared with cetirizine 10 mg and placebo for the symptomatic treatment of seasonal allergic rhinitis: a randomized, double-blind, parallel-group study
    P Kuna
    Division of Internal Medicine, Asthma and Allergy, Barlicki University Hospital, Lodz, Poland
    Clin Exp Allergy 39:1338-47. 2009
    ..Bilastine is a new non-sedative H(1) receptor antagonist, indicated for the treatment of allergic rhinitis (AR) (seasonal and perennial)...
  61. ncbi Comparison of the novel angiotensin II receptor blocker azilsartan medoxomil vs valsartan by ambulatory blood pressure monitoring
    Domenic Sica
    Section of Clinical Pharmacology and Hypertension, Virginia Commonwealth University, Richmond, VA 23298 0160, USA
    J Clin Hypertens (Greenwich) 13:467-72. 2011
    ..These findings suggest that AZL-M could provide higher rates of hypertension control compared with other ARBs in the class...
  62. ncbi Population pharmacokinetic analysis of the oral thrombin inhibitor dabigatran etexilate in patients with non-valvular atrial fibrillation from the RE-LY trial
    K H Liesenfeld
    Boehringer Ingelheim Pharma GmbH and Co KG, Biberach, Germany
    J Thromb Haemost 9:2168-75. 2011
    ..Dabigatran etexilate (DE) is an orally absorbed prodrug of dabigatran, a thrombin inhibitor that exerts potent anticoagulant and antithrombotic activity...
  63. pmc Rivaroxaban vs dabigatran for thromboprophylaxis after joint-replacement surgery: exploratory indirect comparison based on meta-analysis of pivotal clinical trials
    Vladimir Trkulja
    Department of Pharmacology, Zagreb University School of Medicine, Salata 11, 10000 Zagreb, Croatia
    Croat Med J 51:113-23. 2010
    ..To indirectly compare rivaroxaban and dabigatran for prevention of venous thromboembolism (VTE) after total hip or knee arthroplasty (THA, TKA) based on their pivotal efficacy/safety trials embracing a total of 20618 patients...
  64. ncbi Oral dabigatran versus enoxaparin for thromboprophylaxis after primary total hip arthroplasty (RE-NOVATE II*). A randomised, double-blind, non-inferiority trial
    Bengt I Eriksson
    University of Gothenburg, Department of Orthopaedics, Sahlgrenska University Hospital, Molndal, Sweden
    Thromb Haemost 105:721-9. 2011
    ..The risk of bleeding and safety profiles were similar...
  65. ncbi Dabigatran with or without concomitant aspirin compared with warfarin alone in patients with nonvalvular atrial fibrillation (PETRO Study)
    Michael D Ezekowitz
    Lankenau Institute for Medical Research and The Heart Center, Wynnewood, PA, USA
    Am J Cardiol 100:1419-26. 2007
    ..The 2 highest doses of dabigatran suppress D-dimer concentrations. Serious liver toxicity was not seen. The significance of the increase of DTB2 concentrations in dabigatran-treated patients needs resolution...
  66. pmc Angiotensin II AT1 receptor blockade prevents the hypothalamic corticotropin-releasing factor response to isolation stress
    Ines Armando
    Section on Pharmacology, Division of Intramural Research Programs, National Institute of Mental Health, National Institutes of Health, Department of Health and Human Services, Bethesda, MD 20892, USA
    Brain Res 1142:92-9. 2007
    ..Inhibition of central AT(1) receptors limits the CRF response to stress and should be considered as a therapeutic tool to preserve homeostasis under chronic stress conditions...
  67. ncbi Treating the metabolic syndrome: telmisartan as a peroxisome proliferator-activated receptor-gamma activator
    T W Kurtz
    Laboratory of Medicine, University of California San Francisco, 185 Berry Street, Suite 290, San Francisco, CA 94107, USA
    Acta Diabetol 42:S9-16. 2005
    ..If the preliminary data are supported by the results of ongoing large-scale clinical studies, telmisartan could have a central role in the prevention and treatment of metabolic syndrome, diabetes and atherosclerosis...
  68. ncbi Telmisartan, ramipril, or both in patients at high risk for vascular events
    Salim Yusuf
    Population Health Research Institute, McMaster University and Hamilton Health Sciences, Hamilton, ON, Canada
    N Engl J Med 358:1547-59. 2008
    ..We compared the ACE inhibitor ramipril, the ARB telmisartan, and the combination of the two drugs in patients with vascular disease or high-risk diabetes...
  69. ncbi A Phase II, open-label, randomised study to assess the efficacy and safety of the MEK1/2 inhibitor AZD6244 (ARRY-142886) versus capecitabine monotherapy in patients with colorectal cancer who have failed one or two prior chemotherapeutic regimens
    Jaafar Bennouna
    Medical Oncology Branch, Centre Rene Gauducheau, Bd J Monod, 44805 Saint Herblain, France
    Invest New Drugs 29:1021-8. 2011
    ..To assess the efficacy and safety of the MEK1/2 inhibitor AZD6244 (ARRY-142886) in patients with metastatic colorectal cancer who had failed one or two previous chemotherapeutic regimens that included oxaliplatin and/or irinotecan...
  70. ncbi The angiotensin-receptor blocker candesartan for treatment of acute stroke (SCAST): a randomised, placebo-controlled, double-blind trial
    Else Charlotte Sandset
    Department of Internal Medicine, Oslo University Hospital Ulleval, Oslo, Norway
    Lancet 377:741-50. 2011
    ..We aimed to examine whether careful blood-pressure lowering treatment with the angiotensin-receptor blocker candesartan is beneficial in patients with acute stroke and raised blood pressure...
  71. ncbi Effects of the angiotensin receptor blocker azilsartan medoxomil versus olmesartan and valsartan on ambulatory and clinic blood pressure in patients with stages 1 and 2 hypertension
    William B White
    Division of Hypertension and Clinical Pharmacology, Calhoun Cardiology Center, University of Connecticut Health Center, 263 Farmington Ave, Farmington, CT 06030 3940, USA
    Hypertension 57:413-20. 2011
    ..Azilsartan medoxomil could provide higher rates of hypertension control within the ARB class...
  72. ncbi Myocardial ischemic events in patients with atrial fibrillation treated with dabigatran or warfarin in the RE-LY (Randomized Evaluation of Long-Term Anticoagulation Therapy) trial
    Stefan H Hohnloser
    Division of Clinical Electrophysiology, J W Goethe University Hospital, Theodor Stern Kai 7, Frankfurt, Germany
    Circulation 125:669-76. 2012
    ..There is a modest risk of myocardial infarction (MI) and myocardial ischemic events in patients with atrial fibrillation...
  73. pmc Poly(ADP-ribose) polymerase inhibitor induces accelerated senescence in irradiated breast cancer cells and tumors
    Elena V Efimova
    Ludwig Center for Metastasis Research, The University of Chicago, Chicago, Illinois 60637, USA
    Cancer Res 70:6277-82. 2010
    ..PARP inhibition markedly enhanced IRIF persistence and increased breast cancer cell senescence both in vitro and in vivo, arguing for targeting IRIF resolution as a novel therapeutic strategy...
  74. ncbi A phase II, open-label, randomized study to assess the efficacy and safety of AZD6244 (ARRY-142886) versus pemetrexed in patients with non-small cell lung cancer who have failed one or two prior chemotherapeutic regimens
    John D Hainsworth
    Sarah Cannon Research Institute, Nashville, TN 37203, USA
    J Thorac Oncol 5:1630-6. 2010
    ..AZD6244 (ARRY-142886) is a potent, selective MEK inhibitor. This study aimed to evaluate the efficacy and safety of AZD6244 versus pemetrexed as second- or third-line treatment in patients with advanced non-small cell lung cancer (NSCLC)...
  75. ncbi Treatments for stroke prevention in atrial fibrillation: a network meta-analysis and indirect comparisons versus dabigatran etexilate
    Neil S Roskell
    Neil Roskell, RTI Health Solutions, Williams House, Manchester Science Park, Lloyd Street North, Manchester M15 6SE, UK
    Thromb Haemost 104:1106-15. 2010
    ..There was no indication of increased intracranial or extracranial haemorrhage with dabigatran etexilate compared to antiplatelet agents...
  76. ncbi Cognitive deficit in amyloid-beta-injected mice was improved by pretreatment with a low dose of telmisartan partly because of peroxisome proliferator-activated receptor-gamma activation
    Kana Tsukuda
    Department of Molecular Cardiovascular Biology and Pharmacology, Ehime University, Graduate School of Medicine, Shitsukawa, Tohon, Ehime, Japan
    Hypertension 54:782-7. 2009
    ..Taken together, our findings suggest that even a low dose of telmisartan had a preventive effect on cognitive decline in an Alzheimer disease mouse model, partly because of PPAR-gamma activation...
  77. ncbi Telmisartan: a different angiotensin II receptor blocker protecting a different population?
    M Burnier
    Division of Nephrology and Hypertension Consultation, Centre Hospitalier Universitaire Vaudois, Lausanne, Switzerland
    J Int Med Res 37:1662-79. 2009
    ..A class effect for ARBs cannot be assumed. To date, telmisartan is the only ARB that has been shown to reduce cardiovascular risk in at-risk cardiovascular patients...
  78. ncbi In-vitro profile and ex-vivo anticoagulant activity of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate
    Wolfgang Wienen
    Department of Pulmonary Research, Boehringer Ingelheim Pharma GmbH and Co KG, Birkendorfer Strasse, 88397 Biberach, Germany
    Thromb Haemost 98:155-62. 2007
    ..These data suggest that dabigatran is a potent, selective thrombin inhibitor and an orally active anticoagulant as the prodrug, dabigatran etexilate...
  79. ncbi Pharmacokinetics and pharmacodynamics of the direct oral thrombin inhibitor dabigatran in healthy elderly subjects
    Joachim Stangier
    Boehringer Ingelheim Pharma GmbH and Co KG, Biberach, Germany
    Clin Pharmacokinet 47:47-59. 2008
    ....
  80. ncbi Acute and subchronic effects of bilastine (20 and 40 mg) and hydroxyzine (50 mg) on actual driving performance in healthy volunteers
    Silke Conen
    Department of Neuropsychology and Psychopharmacology, Faculty of Psychology and Neuroscience, Maastricht University, Maastricht, The Netherlands
    J Psychopharmacol 25:1517-23. 2011
    ..Bilastine did not produce any driving impairment after single and repeated doses and can be safely used in traffic in doses up to 40 mg...
  81. ncbi Dabigatran: an oral novel potent reversible nonpeptide inhibitor of thrombin
    Wolfgang G Eisert
    Clinical Development and Medical Affairs, Boehringer Ingelheim GmbH, 172 Binger St, Ingelheim 55216, Germany
    Arterioscler Thromb Vasc Biol 30:1885-9. 2010
    ..For the first time, it has been demonstrated clinically that there may be an effective and safe alternative to warfarin...
  82. ncbi STO-609, a specific inhibitor of the Ca(2+)/calmodulin-dependent protein kinase kinase
    Hiroshi Tokumitsu
    Department of Chemistry, Kagawa Medical University, 1750 1 Miki cho, Kita gun, Kagawa 761 0793, Japan
    J Biol Chem 277:15813-8. 2002
    ....
  83. ncbi Pharmacokinetics and pharmacodynamics of dabigatran etexilate, an oral direct thrombin inhibitor, are not affected by moderate hepatic impairment
    Joachim Stangier
    Boehringer Ingelheim GmbH and Co KG, Birkendorferstr 69, 88397 Biberach an der Riss, Germany
    J Clin Pharmacol 48:1411-9. 2008
    ..This study shows that moderate hepatic impairment does not affect the PK/PD or safety profile of dabigatran. Therefore, patients with moderate hepatic impairment can be given dabigatran etexilate without the need for dose adjustment...
  84. ncbi Genetic analysis of a relationship between macrocyclic lactone and benzimidazole anthelmintic selection on Haemonchus contortus
    Maria de Lourdes Mottier
    Institute of Parasitology, McGill University, Sainte Anne de Bellevue, Quebec, Canada
    Pharmacogenet Genomics 18:129-40. 2008
    ..contortus with known treatment history and status for susceptibility or resistance to macrocyclic lactone (ML) or benzimidazole anthelmintics...
  85. ncbi Effects of candesartan compared with amlodipine in hypertensive patients with high cardiovascular risks: candesartan antihypertensive survival evaluation in Japan trial
    Toshio Ogihara
    Osaka University Graduate School of Medicine, Osaka, Japan
    Hypertension 51:393-8. 2008
    ..We disclosed that candesartan-based and amlodipine-based regimens produced no statistical differences in terms of the primary cardiovascular end point, whereas candesartan prevented new-onset diabetes more effectively than amlodipine...
  86. ncbi Beneficial role of telmisartan on cardiovascular complications associated with STZ-induced type 2 diabetes in rats
    Bhoomika R Goyal
    Department of Pharmacology, L M College of Pharmacy, Ahmedabad 380 009, Gujarat, India
    Pharmacol Rep 63:956-66. 2011
    ..In conclusion, our data suggest that telmisartan prevented STZ-induced metabolic abnormalities and cardiovascular complications in type 2 diabetes...
  87. ncbi Blood pressure control by the nifedipine GITS-telmisartan combination in patients at high cardiovascular risk: the TALENT study
    Giuseppe Mancia
    Department of Clinical Medicine and Prevention, University of Milano Bicocca, Italy
    J Hypertens 29:600-9. 2011
    ..Because of the complementary mechanism of action and the evidence of cardiovascular protective effects they include the combination of a calcium antagonist and an angiotensin receptor antagonist among the priorital ones to employ...
  88. ncbi Telmisartan acts through the modulation of ACE-2/ANG 1-7/mas receptor in rats with dilated cardiomyopathy induced by experimental autoimmune myocarditis
    Vijayakumar Sukumaran
    Department of Clinical Pharmacology, Faculty of Pharmaceutical Sciences, Niigata University of Pharmacy and Applied Life Sciences, Niigata, Japan
    Life Sci 90:289-300. 2012
    ..We investigated the cardioprotective effects of telmisartan in rats with dilated cardiomyopathy [DCM] after experimental autoimmune myocarditis [EAM]...
  89. pmc A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma
    Yuan Yuan
    Chemical Biology Program, Broad Institute, Cambridge, Massachusetts 02142, United States
    ACS Chem Biol 7:1152-7. 2012
    ..ATM-pathway activation, caused by either genetic or small-molecule inhibition of G9a, may mediate BRD4770-induced cell senescence. BRD4770 may be a useful tool to study G9a and its role in senescence and cancer cell biology...
  90. ncbi Pyrido[1,2-a]benzimidazole-based agents active against tuberculosis (TB), multidrug-resistant (MDR) TB and extensively drug-resistant (XDR) TB
    Marco Pieroni
    Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 S Wood St, Chicago, IL 60612, USA
    ChemMedChem 6:334-42. 2011
    ....
  91. ncbi Dabigatran etexilate for stroke prevention in patients with atrial fibrillation: resolving uncertainties in routine practice
    Menno V Huisman
    Department of Thrombosis and Haemostasis, Leiden University Medical Center, Leiden, The Netherlands
    Thromb Haemost 107:838-47. 2012
    ..In addition, cut-off values for different coagulation assay results associated with an increased risk of bleeding are given...
  92. ncbi Taenia solium porcine cysticercosis: viability of cysticerci and persistency of antibodies and cysticercal antigens after treatment with oxfendazole
    C S Sikasunge
    School of Veterinary Medicine, University of Zambia, P O Box 32379, Lusaka, Zambia
    Vet Parasitol 158:57-66. 2008
    ....
  93. ncbi Structure-based design of novel potent nonpeptide thrombin inhibitors
    Norbert H Hauel
    Boehringer Ingelheim Pharma KG, Research Division, Birkendorfer Strasse 65, D 88397 Biberach Riss, Germany
    J Med Chem 45:1757-66. 2002
    ..This zwitterionic molecule was converted into the double-prodrug 31 (BIBR 1048), which showed strong oral activity in different animal species. On the basis of these results, 31 was chosen for clinical development...
  94. ncbi Population pharmacokinetic analysis of the new oral thrombin inhibitor dabigatran etexilate (BIBR 1048) in patients undergoing primary elective total hip replacement surgery
    Inaki F Troconiz
    Boehringer Ingelheim Pharma GmbH and Co KG, Birkendorfer Strasse 68, 88397 Biberach, Germany
    J Clin Pharmacol 47:371-82. 2007
    ..As a consequence, the rate of absorption is reduced and interindividual variability in drug exposure increased. On the following days, the disposition in plasma of BIBR 953 ZW is less variable...
  95. pmc Clinical presentation and management of Fasciola hepatica infection: single-center experience
    Muhsin Kaya
    Department of Gastroenterology, Dicle University School of Medicine, Diyarbakir 21280, Turkey
    World J Gastroenterol 17:4899-904. 2011
    ..To identify the characteristic clinical, laboratory and radiological findings and response to treatment in patients with fascioliasis...
  96. ncbi Evaluation of a proposed in vitro test strategy using neuronal and non-neuronal cell systems for detecting neurotoxicity
    J Gartlon
    ECVAM, European Commission Joint Research Centre, via E Fermi 1, Ispra 21020, Italy
    Toxicol In Vitro 20:1569-81. 2006
    ....
  97. ncbi The Study on COgnition and Prognosis in the Elderly (SCOPE)--recent analyses
    Peter Trenkwalder
    Department of Internal Medicine, Starnberg Hospital, Ludwig Maximilian University Munich, Starnberg, Germany
    J Hypertens Suppl 24:S107-14. 2006
    ..Results in other subgroups were generally consistent with those in the entire SCOPE study population. In patients with slightly low cognitive function at baseline, the MMSE score declined less in the candesartan group...
  98. ncbi Long-term treatment with the AT1-receptor antagonist telmisartan inhibits biglycan accumulation in murine atherosclerosis
    Nadine Nagy
    Institut fur Pharmakologie, Universitatsklinikum Essen, Universitat Duisburg Essen, Hufelandstrasse 55, 45122, Essen, Germany
    Basic Res Cardiol 105:29-38. 2010
    ..Thus, biglycan is a pleiotropic target of telmisartan that might contribute to the anti-atherogenic effects of this AT1-antagonist...
  99. pmc Regulation of the energy sensor AMP-activated protein kinase by antigen receptor and Ca2+ in T lymphocytes
    Peter Tamas
    Division of Cell Biology and Immunology, School of Life Sciences, University of Dundee, Dundee DD1 5EH, Scotland, United Kingdom
    J Exp Med 203:1665-70. 2006
    ..Moreover, AMPK does not just react to cellular energy depletion but also anticipates it...
  100. ncbi Dual repressive effect of angiotensin II-type 1 receptor blocker telmisartan on angiotensin II-induced and estradiol-induced uterine leiomyoma cell proliferation
    Aki Isobe
    Department of Obstetrics and Gynecology, Osaka University Graduate School of Medicine, 2 2 Yamadaoka, Suita, Osaka 565 0871, Japan
    Hum Reprod 23:440-6. 2008
    ..Elevated blood pressure has an independent, positive association with risk for clinically detected uterine leiomyoma. Angiotensin II (Ang II) is a key biological peptide in the renin-angiotensin system that regulates blood pressure...
  101. pmc Antioxidants prevent ethanol-associated apoptosis in fetal rhombencephalic neurons
    Angeline M Antonio
    Department of Cell Biology, Neurobiology, and Anatomy, Loyola University Stritch School of Medicine, Maywood, IL 60153, USA
    Brain Res 1204:16-23. 2008
    ..e., those cultured in the absence of ethanol. These studies showed that several classes of antioxidants can exert neuroprotection against ethanol-associated apoptosis in fetal rhombencephalic neurons...

Research Grants60

  1. Oxidative Stress in Oral Streptococci
    Robert E Marquis; Fiscal Year: 2010
    ..Aim 3 is focused on translational research with investigation of small molecules, such as zinc cations, benzimidazoles or other sulfhydryl-reacting agents, such as allicin, chelators, fluoride and other halogens, transition metal ..
  2. Novel Antimicrobials Targeting Cell Division
    Iwao Ojima; Fiscal Year: 2013
    ..tubulin/microtubules and has hypothesized that a certain class of taxanes (microtubule-stabilizer) and benzimidazoles (tubulin polymerization inhibitors) should inhibit the depolymerization or polymerization of FtsZ from ..
  3. ANTIFUNGAL RESPONSE--MDR INDUCTION
    Thomas Edlind; Fiscal Year: 2002
    ..indicate that MDR induction is the most likely explanation for the intrinsic resistance of Candida species to benzimidazoles and for the antagonistic activity between compounds that induce MDR (albendazole and sulfadiazine) and ..
  4. Enantioselective Total Synthesis of Marcfortine B via SmI2-mediated C-C Bond Form
    TIMOTHY KUM BENG; Fiscal Year: 2013
    ..Macrocyclic lactones, benzimidazoles, and imidazothiazoles are at present being used for the eradication of gastrointestinal nematodes in ..
  5. DICATIONIC DRUGS--TREATMENT FOR AIDS-RELATED INFECTIONS
    Richard Tidwell; Fiscal Year: 1999
    ..and pyrimidine ring systems as spacers between the cationic centers, while the UNC-CH group will focus on benzimidazoles, carbazoles and alpha, omega, dioxyalkanes. The choice of these spacing units is based on our previous studies...
  6. Synthesis and Biology of Bengazole Analogs
    Peter Wipf; Fiscal Year: 2003
    ..has suffered major setbacks, since resistance of nematodes to the anthelminthic drugs of general use such as benzimidazoles levamizole and praziquantel has emerged...
  7. STRUCTURAL AND GENETIC ASPECTS OF TUBULIN INTERACTIONS
    LYNWOOD YARBROUGH; Fiscal Year: 1992
    ..in terms of its assembly, stability, and susceptibility to antimitotic agents such as colchicine and the benzimidazoles. 3...
  8. HUMAN CYTOMEGALOVIRUS DNA CLEAVAGE AND PACKAGING
    Michael McVoy; Fiscal Year: 2005
    ..Recent findings in GPCMV and HCMV suggest that the benzimidazoles induce a premature cleavage to produce truncated genomes...
  9. DINITROANILINE HERBICIDE METABOLISM & TOXICOLOGY
    JUDD NELSON; Fiscal Year: 1980
    ..to synthesize prospective metabolites of dinitroaniline herbicides, particularly the polar derivatives such as benzimidazoles and their N-oxides, dihydroxy-benzimidazolines, etc., for use as reference standards...
  10. MPT INHIBITOR IND 50,820 IN FAMILIAL HYPERCHOLESTEROLEM*
    Marina Cuchel; Fiscal Year: 2009
    ..This study would serve as basis for approval of BMS-201038 for hoFH. ..
  11. Salsalate: A Diabetes Treatment for Carbonyl, Oxidative & Nitrosative Stress
    JOSHUA ISRAEL BARZILAY; Fiscal Year: 2010
    ..If effective, this treatment could reduce the risk of heart attacks and strokes that frequently occur in people with diabetes. ..
  12. Mechanistic study of CHD risk in subjects with high HDLC
    Marina Cuchel; Fiscal Year: 2008
    ....
  13. Oxidative Stress and Genetics of Prehypertension
    Shawna Nesbitt; Fiscal Year: 2004
    ..abstract_text> ..
  14. KIDNEY SPECIFIC GENE TRANSFER IN HYPERTENSION
    Theodore Kurtz; Fiscal Year: 2003
    ..Under this alternative hypothesis, the results of the cDNA microarray analysis will be used to identify potential downstream target genes whose expression is altered by the primary genetic defect on chromosome 1. ..
  15. DEVELOPMENT OF A LIVE ATTENUATED HSV-2 VACCINE
    Mark Prichard; Fiscal Year: 2002
    ..In addition further in vitro characterization will enable high quality clinical trial material to be produced for IND enabling primate studies and early Phase I human trials. PROPOSED COMMERCIAL APPLICATION: Not Available ..
  16. WHY DO METABOLIC RISK FACTORS CLUSTER WITH HYPERTENSION?
    Theodore Kurtz; Fiscal Year: 2003
    ....
  17. NICOTINIC RECEPTORS IN MAMMALIAN INTRACARDIAC NEURONS
    Javier Cuevas; Fiscal Year: 2001
    ..An understanding of the properties and physiological role of the receptors is necessary to comprehend neural control of the heart. ..
  18. Synthesis and Testing of Rigid CDK5 inhibitors
    Patrick Flaherty; Fiscal Year: 2008
    ..We hope that by preventing NFT formation, we can help America preserve its memory and recognize its future. [unreadable] [unreadable] [unreadable]..
  19. Angll and PPARy/LXR in Atherosclerosis
    Willa Hsueh; Fiscal Year: 2008
    ..4) Determine whether PPARgamma ligands or LXRaalpha ligands can induce regression of established atherosclerosis. ..
  20. Inflammation & Prognosis in Decompensated Heart Failure
    GARY FELKER; Fiscal Year: 2008
    ..Felker's development into an established independent clinical investigator with expertise in both complex clinical research methodology and the role of inflammation in the pathophysiology of heart failure. ..
  21. Role of Lamin B Receptor in Neutrophil Maturation and Functional Activation
    Peter Gaines; Fiscal Year: 2007
    ..The results may also offer important insight into the pathogenesis of potentially fatal hematologic disorders. [unreadable] [unreadable] [unreadable]..
  22. Characterization of the HCV NS5A Protein
    Timothy Tellinghuisen; Fiscal Year: 2007
    ..unreadable] ABSTRACT NOT PROVIDED[unreadable] [unreadable]..
  23. Brca1 Deletion in Murine Cells and Mammary Tissue
    MARCIA BROSE; Fiscal Year: 2007
    ..abstract_text> ..
  24. Identifying Genes Required for Prion Accumulation
    James Stanton; Fiscal Year: 2007
    ..The sponsor collaborates closely in research and has successfully mentored graduate students to research independence. ..
  25. Endoplasmic Reticulum Calcium Pools in Neuropathic Pain
    LAUREN TA; Fiscal Year: 2007
    ..3): To determine whether thapsigargin, an ER calcium pump inhibitor, can reverse nerve injury-induced neuropathic pain. ..
  26. HOOKWORM LARVAL INFECTIVITY AND DEVELOPMENT
    Peter Hotez; Fiscal Year: 2002
    ..The pharmacologic manipulation of parasite-derived protein kinases may offer a new approach to chemotherapy by taking larvae out of arrest. ..
  27. VASCULAR RESPONSES DURING CORTICAL SPREADING DEPRESSION
    David Busija; Fiscal Year: 2001
    ....
  28. Molecular Basis Of Renal Cell Carcinoma Response to SU11428
    Robert J Motzer; Fiscal Year: 2011
    ..These tumor and cell line-based studies lay a foundation for further molecular studies aimed at understanding the sensitivity/resistance of RCC to SU11248. ..
  29. Development of cAMP Biosensor, High Content Imaging, and Functional GLP-1R aSSAYS
    Philip LoGrasso; Fiscal Year: 2010
    ....
  30. Genetics of Microangiopathic Brain Injury
    Stephen T Turner; Fiscal Year: 2010
    ..abstract_text> ..
  31. GENETIC EPIDEMIOLOGY OF RESPONSES TO ANTIHYPERTENSIVES
    Stephen Turner; Fiscal Year: 2006
    ....
  32. Hsp90, NOS3 and Cardioprotection
    Yang Shi; Fiscal Year: 2009
    ..abstract_text> ..
  33. Agilent 5973 GC/MS System
    GARY MOLANDER; Fiscal Year: 2002
    ..Our current lack of such instrumentation negatively affects the ability to carry out many of these studies. This critical capability, in the form of an instrument for everyday analysis, is urgently needed. ..
  34. Genetics of Chronic Kidney Disease
    Stephen T Turner; Fiscal Year: 2010
    ..abstract_text> ..
  35. Evaluation in Primates of Cocaine Esterase for the Treatment of Cocaine Toxicity
    Mei Chuan Ko; Fiscal Year: 2010
    ..Dose-response functions for each enzyme will be obtained repeatedly and blood samples analyzed for titer development so that tolerance to the effects of CocE can be monitored. ..
  36. MOLECULAR STRUCTURE OF THE PHAGOCYTE NADPH OXIDASE
    Mark Quinn; Fiscal Year: 2007
    ..The results of these studies will further our understanding of how distinct levels of regulatory input are integrated to facilitate functional assembly and activation of the phagocyte NADPH oxidase. ..
  37. The significance of racial segregation for CV disease
    Mary Vaughan Sarrazin; Fiscal Year: 2007
    ..The knowledge gained from this study about the significance of segregation as a determinant of racial disparity will be essential for designing effective strategies for eliminating disparities. [unreadable] [unreadable] [unreadable]..
  38. ANGIOTENSIN II AND MITOGEN ACTIVATED PROTEIN KINASE
    Willa Hsueh; Fiscal Year: 2003
    ..5) Investigate the mechanism of transcription at regulation of PAI-1 by hyperglycemia AngII, insulin and the MAPK inhibitor in cultured rat cardiac fibroblasts. ..
  39. MODULATION OF NEUTROPHIL FUNCTION BY PEROXYNITRITE
    Mark Quinn; Fiscal Year: 2003
    ....
  40. Pharmacogenetics and Antithrombotic Therapy
    Brian Gage; Fiscal Year: 2003
    ..Using high performance liquid chromatography, we will measure the levels of the 2 enantiomers of warfarin and test Hypothesis 4: Clearance of S-warfarin will be significantly decreased in the presence of 2C9 SNPs. ..
  41. Characterization of the Hepatitis C NS5a Kinase Complex
    Timothy Tellinghuisen; Fiscal Year: 2004
    ..abstract_text> ..
  42. Human Subjects Research Enhancements Program
    Frederick Samaha; Fiscal Year: 2003
    ..The sharing of electronic systems will allow Tri-Health to upgrade their research compliance program. ..
  43. Cerebrovascular Dysfunction in Insulin Resistance
    David Busija; Fiscal Year: 2004
    ..We believe that our studies will result in new and important findings that will lead to improved therapies to reduce morbidity and mortality in IR individuals. ..
  44. Catalytic Processes for Selective Organic Synthesis
    GARY MOLANDER; Fiscal Year: 2005
    ..4) Carbometalation/cyclization reactions will be explored utilizing organochromium species. 5) Ligands and catalytic systems designed for asymmetric synthesis will be explored. ..
  45. CLINICAL TRIALS AND MENTORING IN ONCOLOGY RESEARCH
    Robert Motzer; Fiscal Year: 2003
    ..One recently joined staff at MSKCC in the Genito-urinary Section. Mentoring of clinical trials is extended beyond fellowship to junior faculty members. ..
  46. Chondroleukin and Articular Cartilage
    A Reddi; Fiscal Year: 2005
    ..Aim 2A. To identify the cognate receptors of lL-17B in articular chondrocytes. Aim 2B. To examine the hypothesis that the novel lL-17 receptor-like molecule (IL-1 7RL) is a functional receptor in articular cartilage. ..
  47. IMPAIRED CORONARY ARTERY FUNCTION IN INSULIN RESISTANCE
    David Busija; Fiscal Year: 2003
    ..Findings from this project may provide important information that can be used in future studies to design treatments to prevent or abort the cardiovascular complications of insulin resistance. ..
  48. Novel Therapeutics for Bacillus anthracis
    Michael Johnson; Fiscal Year: 2007
    ..A bioassay core will provide a variety of assays for identifying and evaluating lead therapeutic agents. An administrative core will provide fiscal management and administrative support. ..
  49. A NEURAL TRANSCRIPTION FACTOR IN LUNG CANCER EVOLUTION
    Douglas Ball; Fiscal Year: 2006
    ..The proposed studies should provide novel insights in SCLC biology and a firm basis for determining whether hASH1, and hASHl-regulated growth mechanisms, should be intensively pursued as therapeutic targets for SCLC. ..
  50. Anthipertensive PharmacoGenomics
    Stephen Turner; Fiscal Year: 2006
    ..abstract_text> ..
  51. Mechanisms of CVD and Endothelial Dysfunction in Obesity
    Willa Hsueh; Fiscal Year: 2006
    ..Early intervention is critical if we are to prevent these two major diseases, which may, indeed, be the same disease. ..
  52. PPARGAMMA AND AII IN GLOMERULOSCLEROSIS
    Willa Hsueh; Fiscal Year: 2002
    ..abstract_text> ..
  53. Chronic Thromboembolic Pulmonary Hypertension
    TIMOTHY MORRIS; Fiscal Year: 2006
    ..The fragments will be subjected to liquid chromatography-mass spectroscopy with data-dependent MS-2 data acquisition, followed by computer-assisted sequence analysis. ..
  54. Impact of Certificate of Need on the Use of Revascularization for AMI
    Mary Vaughan Sarrazin; Fiscal Year: 2006
    ..g., revascularization, mortality) and Cox regression with stratification for time-to-event outcomes (e.g., time to readmission). [unreadable] [unreadable]..
  55. Intrathecal Opioid-Induced Pruritus
    Mei Chuan Ko; Fiscal Year: 2003
    ..These studies would provide a systematic understanding of the pharmacology of intrathecal morphine-induced pruritus in primates and establish the basis for identifying potential therapeutically effective antipruritics. ..
  56. Sir2 regulation and chemical modulation
    Anthony A Sauve; Fiscal Year: 2010
    ..abstract_text> ..
  57. Altered Accumbens Signaling Following Ethanol Exposure
    FREDERIC WOODWARD HOPF; Fiscal Year: 2010
    ..Altered spike firing and dopamine signaling in the NAcb could significantly influence the behavioral contribution of the NAcb, and in this way facilitate the onset of relapse. ..
  58. REGULATION OF RENAL FUNCTION AND BP BY THROMBOXANE
    CHRISTOPHER WILCOX; Fiscal Year: 2002
    ....
  59. Phase I/II Study of MS-275 and 5-Azacytidine in Patients with Advanced Non-Small
    CHARLES RUDIN; Fiscal Year: 2008
    ..If successful, this approach could alter the poor prognosis of individuals with this disease. [unreadable] [unreadable] [unreadable]..
  60. A pharmacogenetic and pharmacodynamic study of erlotinib
    CHARLES RUDIN; Fiscal Year: 2004
    ..Defining the basis of this toxicity could also promote the development of EGFR-directed agents that may avoid such toxicity or that may be effective in a broader spectrum of cancer patients. ..