cyclooxygenase inhibitors

Summary

Summary: Compounds or agents that combine with cyclooxygenase (PROSTAGLANDIN-ENDOPEROXIDE SYNTHASES) and thereby prevent its substrate-enzyme combination with arachidonic acid and the formation of eicosanoids, prostaglandins, and thromboxanes.

Top Publications

  1. ncbi Identification of novel cyclooxygenase-2 selective inhibitors using pharmacophore models
    Albert Palomer
    R and D Department, Laboratorios Menarini S A, Alfonso XII 587, 08918 Badalona, Spain
    J Med Chem 45:1402-11. 2002
  2. ncbi Acetaminophen (paracetamol) is a selective cyclooxygenase-2 inhibitor in man
    Burkhard Hinz
    Institute of Toxicology and Pharmacology, University of Rostock, Schillingallee 70, D 18057 Rostock, Germany
    FASEB J 22:383-90. 2008
  3. ncbi Strategies to optimize treatment with NSAIDs in patients at risk for gastrointestinal and cardiovascular adverse events
    James M Scheiman
    Division of Gastroenterology, University of Michigan, Ann Arbor, Michigan, USA
    Clin Ther 32:667-77. 2010
  4. ncbi Cyclooxygenase-2 is instrumental in Parkinson's disease neurodegeneration
    Peter Teismann
    Neuroscience Research Laboratories of the Movement Disorder Division, Department of Neurology, Columbia University, New York, NY 10032, USA
    Proc Natl Acad Sci U S A 100:5473-8. 2003
  5. ncbi IL-17 in synovial fluids from patients with rheumatoid arthritis is a potent stimulator of osteoclastogenesis
    S Kotake
    The Institute of Rheumatology, Tokyo Women s Medical University, Tokyo 162 0054, Japan
    J Clin Invest 103:1345-52. 1999
  6. ncbi Cyclooxygenase-2 inhibition by celecoxib reduces proliferation and induces apoptosis in angiogenic endothelial cells in vivo
    Kathleen M Leahy
    Pharmacia, Mail Zone AA4C, 700 Chesterfield Parkway, Chesterfield, Missouri 63017, USA
    Cancer Res 62:625-31. 2002
  7. ncbi Effects of specific inhibition of cyclooxygenase-2 on sodium balance, hemodynamics, and vasoactive eicosanoids
    F Catella-Lawson
    University of Pennsylvania, School of Medicine, Philadelphia, Pennsylvania, USA
    J Pharmacol Exp Ther 289:735-41. 1999
  8. ncbi Isolation of linoleic and alpha-linolenic acids as COX-1 and -2 inhibitors in rose hip
    A K Jäger
    Department of Medicinal Chemistry, The Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, DK 2100 Copenhagen, Denmark
    Phytother Res 22:982-4. 2008
  9. ncbi The cyclooxygenase-2 inhibitor celecoxib has therapeutic effects in major depression: results of a double-blind, randomized, placebo controlled, add-on pilot study to reboxetine
    N Muller
    Hospital for Psychiatry and Psychotherapy, Ludwig Maximilians Universitat, Munchen, Germany
    Mol Psychiatry 11:680-4. 2006
  10. ncbi Screening of ubiquitous plant constituents for COX-2 inhibition with a scintillation proximity based assay
    U Huss
    Division of Pharmacognosy, Department of Medicinal Chemistry, Biomedical Centre, Uppsala University, Box 574, SE-751 23 Uppsala, Sweden
    J Nat Prod 65:1517-21. 2002

Research Grants

  1. FETAL REFLEX RESPONSES TO CEREBRAL HYPOPERFUSION
    Charles Wood; Fiscal Year: 1999
  2. NEURAL MECHANISMS OF PAIN AND HYPERALGESIA
    Jon Levine; Fiscal Year: 1993
  3. Use of Novel Cox-2 Inhibitors in Neurological Disorders
    STANLEY BELL; Fiscal Year: 2006
  4. Eicosanoids and Diabetic Retinopathy
    Rose Gubitosi Klug; Fiscal Year: 2007
  5. PROSTANOID BIOSYNTHESIS IN SYSTEMIC MASTOCYTOSIS
    John Oates; Fiscal Year: 2003
  6. IMAGING COX-2 GENE EXPRESSION IN INFLAMMATION AND TUMORS
    Harvey Herschman; Fiscal Year: 2009
  7. IMAGING COX-2 GENE EXPRESSION IN INFLAMMATION AND TUMORS
    Harvey Herschman; Fiscal Year: 2007

Detail Information

Publications300 found, 100 shown here

  1. ncbi Identification of novel cyclooxygenase-2 selective inhibitors using pharmacophore models
    Albert Palomer
    R and D Department, Laboratorios Menarini S A, Alfonso XII 587, 08918 Badalona, Spain
    J Med Chem 45:1402-11. 2002
    ..Compound 8a (LM-1685) was selected as a promising candidate for further pharmacological evaluation...
  2. ncbi Acetaminophen (paracetamol) is a selective cyclooxygenase-2 inhibitor in man
    Burkhard Hinz
    Institute of Toxicology and Pharmacology, University of Rostock, Schillingallee 70, D 18057 Rostock, Germany
    FASEB J 22:383-90. 2008
    ..In view of its substantial COX-2 inhibition, recently defined cardiovascular warnings for use of COX-2 inhibitors should also be considered for acetaminophen...
  3. ncbi Strategies to optimize treatment with NSAIDs in patients at risk for gastrointestinal and cardiovascular adverse events
    James M Scheiman
    Division of Gastroenterology, University of Michigan, Ann Arbor, Michigan, USA
    Clin Ther 32:667-77. 2010
    ..However, NSAIDs have been associated with gastrointestinal (GI) toxicity. The cardiovascular (CV) toxicity associated with COX-2 inhibitors and some other NSAIDs further complicates the choice of therapy...
  4. ncbi Cyclooxygenase-2 is instrumental in Parkinson's disease neurodegeneration
    Peter Teismann
    Neuroscience Research Laboratories of the Movement Disorder Division, Department of Neurology, Columbia University, New York, NY 10032, USA
    Proc Natl Acad Sci U S A 100:5473-8. 2003
    ..Because of the safety record of the COX-2 inhibitors, and their ability to penetrate the blood-brain barrier, these drugs may be therapies for PD...
  5. ncbi IL-17 in synovial fluids from patients with rheumatoid arthritis is a potent stimulator of osteoclastogenesis
    S Kotake
    The Institute of Rheumatology, Tokyo Women s Medical University, Tokyo 162 0054, Japan
    J Clin Invest 103:1345-52. 1999
    ....
  6. ncbi Cyclooxygenase-2 inhibition by celecoxib reduces proliferation and induces apoptosis in angiogenic endothelial cells in vivo
    Kathleen M Leahy
    Pharmacia, Mail Zone AA4C, 700 Chesterfield Parkway, Chesterfield, Missouri 63017, USA
    Cancer Res 62:625-31. 2002
    ..2-3.0-fold) in response to celecoxib. Thus, the antitumor activity of celecoxib may be attributable, at least in part, to a direct effect on host stromal elements, such as the angiogenic vasculature...
  7. ncbi Effects of specific inhibition of cyclooxygenase-2 on sodium balance, hemodynamics, and vasoactive eicosanoids
    F Catella-Lawson
    University of Pennsylvania, School of Medicine, Philadelphia, Pennsylvania, USA
    J Pharmacol Exp Ther 289:735-41. 1999
    ..Our data suggest that acute sodium retention by nonsteroidal anti-inflammatory drugs in healthy elderly subjects is mediated by the inhibition of Cox-2, whereas depression of GFR is due to inhibition of Cox-1...
  8. ncbi Isolation of linoleic and alpha-linolenic acids as COX-1 and -2 inhibitors in rose hip
    A K Jäger
    Department of Medicinal Chemistry, The Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, DK 2100 Copenhagen, Denmark
    Phytother Res 22:982-4. 2008
    ..The COX-2/COX-1 ratio was 0.007 for linoleic acid and 0.2 for alpha-linolenic acid. Linoleic acid and alpha-linolenic acid contribute to the COX-1 and -2 inhibitory activity of rose hip...
  9. ncbi The cyclooxygenase-2 inhibitor celecoxib has therapeutic effects in major depression: results of a double-blind, randomized, placebo controlled, add-on pilot study to reboxetine
    N Muller
    Hospital for Psychiatry and Psychotherapy, Ludwig Maximilians Universitat, Munchen, Germany
    Mol Psychiatry 11:680-4. 2006
    ..Moreover, the fact that treatment with an anti-inflammatory drug showed beneficial effects on MD indicates that inflammation is related to the pathomechanism of the disorder, although the exact mechanisms remain to become elucidated...
  10. ncbi Screening of ubiquitous plant constituents for COX-2 inhibition with a scintillation proximity based assay
    U Huss
    Division of Pharmacognosy, Department of Medicinal Chemistry, Biomedical Centre, Uppsala University, Box 574, SE-751 23 Uppsala, Sweden
    J Nat Prod 65:1517-21. 2002
    ..This study showed that a COX-2-catalyzed PGE(2) assay using SPA is suitable for screening natural compounds with respect to COX-2 inhibition...
  11. ncbi Potential involvement of the cyclooxygenase-2 pathway in the regulation of tumor-associated angiogenesis and growth in pancreatic cancer
    Jingsong Chu
    Signal Transduction Laboratory, Methodist Research Institute, Indianapolis, Indiana 46202, USA
    Mol Cancer Ther 2:1-7. 2003
    ....
  12. ncbi Cardiovascular risk of celecoxib in 6 randomized placebo-controlled trials: the cross trial safety analysis
    Scott D Solomon
    Cardiovascular Division, Brigham and Women s Hospital, 75 Francis St, Boston, MA 02115, USA
    Circulation 117:2104-13. 2008
    ..Our aim was to assess the cardiovascular risk associated with celecoxib in 3 dose regimens and to assess the relationship between baseline cardiovascular risk and effect of celecoxib on cardiovascular events...
  13. ncbi Cardiovascular risk and inhibition of cyclooxygenase: a systematic review of the observational studies of selective and nonselective inhibitors of cyclooxygenase 2
    Patricia McGettigan
    Discipline of Clinical Pharmacology, School of Medicine and Public Health, The University of Newcastle, New South Wales, Australia
    JAMA 296:1633-44. 2006
    ....
  14. ncbi Breast-cancer-associated metastasis is significantly increased in a model of autoimmune arthritis
    Lopamudra Das Roy
    Department of Immunology, Mayo Clinic School of Medicine, 13400 E, Shea Blvd, Scottsdale, Arizona 85259, USA
    Breast Cancer Res 11:R56. 2009
    ....
  15. ncbi Effects of eicosapentaenoic and docosahexaenoic n-3 fatty acids from fish oil and preferential Cox-2 inhibition on systemic syndromes in patients with advanced lung cancer
    Leandro C A Cerchietti
    Translational Research Unit, Angel H Roffo Cancer Institute, Universidad de Buenos Aires, Buenos Aires, Argentina
    Nutr Cancer 59:14-20. 2007
    ..This study shows that by modulating the eicosanoid metabolism using a combination of n-3 fatty acids and cyclooxygenase-2 inhibitor, some of the signs and symptoms associated with a SIMS could be ameliorated...
  16. ncbi Celecoxib-loaded poly(D,L-lactide-co-glycolide) nanoparticles prepared using a novel and controllable combination of diffusion and emulsification steps as part of the salting-out procedure
    Paul A McCarron
    School of Pharmacy, Queens University Belfast, Medical Biology Centre, Belfast, UK
    J Microencapsul 23:480-98. 2006
    ....
  17. ncbi Inflammation in lung carcinogenesis: new targets for lung cancer chemoprevention and treatment
    Jay M Lee
    Division of Cardiothoracic Surgery, Department of Surgery, UCLA Lung Cancer Research Program, Jonsson Comprehensive Cancer Center, David Geffen School of Medicine at UCLA, Los Angeles, CA 90095, USA
    Crit Rev Oncol Hematol 66:208-17. 2008
    ..The understanding of molecular mechanisms involved in inflammation and lung carcinogenesis provide insight for new drug development that target reversible, non-mutational events in the chemoprevention and treatment of lung cancer...
  18. ncbi Phase II nonrandomized study of the efficacy and safety of COX-2 inhibitor celecoxib on patients with cancer cachexia
    Giovanni Mantovani
    Department of Medical Oncology, University of Cagliari, Cagliari, Italy
    J Mol Med (Berl) 88:85-92. 2010
    ..Therefore, phase III clinical trials are warranted to test the efficacy and safety of celecoxib...
  19. ncbi Ibuprofen in very preterm infants impairs renal function for the first month of life
    Rachel Vieux
    Maternite Regionale, Neonatal Department, Nancy University, Nancy, France
    Pediatr Nephrol 25:267-74. 2010
    ..Renal function of infants receiving ibuprofen should be carefully monitored and drugs that are eliminated by glomerular filtration handled cautiously during this period...
  20. ncbi Cyclooxygenase-2-dependent and -independent inhibition of proliferation of colon cancer cells by 5-aminosalicylic acid
    Carmine Stolfi
    Dipartimento di Medicina Interna, Universita Tor Vergata, Via Montpellier, 1 00133 Rome, Italy
    Biochem Pharmacol 75:668-76. 2008
    ..Taken together our data indicate that 5-ASA causes both a COX-2-dependent and -independent inhibition of CRC cell growth...
  21. ncbi Cardiovascular effects of the cyclooxygenase inhibitors
    William B White
    Division of Hypertension and Clinical Pharmacology, Pat and Jim Calhoun Cardiology Center, University of Connecticut School of Medicine, Farmington, CT 06030-3940, USA
    Hypertension 49:408-18. 2007
  22. ncbi Celecoxib and curcumin synergistically inhibit the growth of colorectal cancer cells
    Shahar Lev-Ari
    Department of Cancer Prevention, Tel Aviv Medical Center, Israel
    Clin Cancer Res 11:6738-44. 2005
    ..This synergistic effect is clinically important because it can be achieved in the serum of patients receiving standard anti-inflammatory or antineoplastic dosages of celecoxib...
  23. ncbi Selective cyclooxygenase-2 inhibitors inhibit growth and induce apoptosis of bladder cancer
    Jason Gee
    Department of Urology, The University of Texas M D Anderson Cancer Center, Houston, TX 77030, USA
    Oncol Rep 15:471-7. 2006
    ..Induction of apoptosis in all three cell lines by celecoxib was associated with downregulation of Bcl-2. These changes occur independently of COX-2 expression levels suggesting the presence of a COX-2 independent pathway...
  24. ncbi Selective inhibition of interleukin-8-induced neutrophil chemotaxis by ketoprofen isomers
    C Bizzarri
    Consorzio Biolaq, L'Aquila, Italy
    Biochem Pharmacol 61:1429-37. 2001
    ..It is concluded that inhibition of IL-8 chemotaxis could represent a new clinical target for ketoprofen isomers and, in fact, contribute to the anti-inflammatory activity of NSAIDs...
  25. ncbi Nimesulide inhibits proliferation via induction of apoptosis and cell cycle arrest in human gastric adenocarcinoma cell line
    Jian Ying Li
    Department of Gastroenterology, Affiliated Union Hospital, Fujian Medical University, Fuzhou 350001, China
    World J Gastroenterol 9:915-20. 2003
    ..To evaluate the potential role of Nimesulide, a selective COX-2 inhibitor, in proliferation and apoptosis of gastric adenocarcinoma cells SGC7901...
  26. ncbi Amelioration of hippocampal neuronal damage after transient forebrain ischemia in cyclooxygenase-2-deficient mice
    Tsutomu Sasaki
    Department of Internal Medicine and Therapeutics, Osaka University Graduate School of Medicine, Suita City, Osaka, Japan
    J Cereb Blood Flow Metab 24:107-13. 2004
    ..These results of genetic disruption and chemical inhibition of cyclooxygenase-2 show that inhibition of COX-2 ameliorates selective neuronal death after transient forebrain ischemia in mice...
  27. ncbi Prophylactic ibuprofen versus placebo in very premature infants: a randomised, double-blind, placebo-controlled trial
    V Gournay
    Service de réanimation pédiatrique et néonatale, hôpital de la Mère et de l Enfant, Centre Hospitalier Universitaire CHU de Nantes, quai Moncousu, 44000 Nantes, France
    Lancet 364:1939-44. 2004
    ..We aimed to compare prophylactic and curative ibuprofen in the treatment of this abnormality in very premature infants...
  28. ncbi Multifaceted roles of cyclooxygenase-2 in lung cancer
    Karen Riedl
    UCLA Lung Cancer Research Program, Department of Medicine, 37-131 CHS, David Geffen School of Medicine at UCLA, 10833 LeConte Avenue, Los Angeles, CA 90095-1690, USA
    Drug Resist Updat 7:169-84. 2004
    ..In addition, delineation of how COX-2-dependent genes modulate the malignant phenotype will provide novel insights in lung cancer pathogenesis...
  29. ncbi Hyperinduction of cyclooxygenase-2-mediated proinflammatory cascade: a mechanism for the pathogenesis of avian influenza H5N1 infection
    Suki M Y Lee
    Department of Microbiology, Siriraj Hospital, Bangkok, Thailand
    J Infect Dis 198:525-35. 2008
    ..These data provide a basis for the possible development of novel therapeutic interventions for the treatment of H5N1 disease, as adjuncts to antiviral drugs...
  30. ncbi Cyclooxygenase inhibitors induce the expression of the tumor suppressor gene EGR-1, which results in the up-regulation of NAG-1, an antitumorigenic protein
    Seung Joon Baek
    Laboratory of Molecular Carcinogenesis, 111 TW Alexander Drive, Research Triangle Park, NC 27709, USA
    Mol Pharmacol 67:356-64. 2005
    ..NAG-1 seems to be an important downstream target protein of this transcription factor, EGR-1, and may mediate the chemopreventive activity of some NSAIDs...
  31. ncbi The cyclooxygenase inhibitor ibuprofen and the FLAP inhibitor MK886 inhibit pancreatic carcinogenesis induced in hamsters by transplacental exposure to ethanol and the tobacco carcinogen NNK
    H M Schuller
    Experimental Oncology Laboratory, College of Veterinary Medicine, University of Tennessee, 2407 River Drive, Knoxville, TN 37996, USA
    J Cancer Res Clin Oncol 128:525-32. 2002
    ....
  32. ncbi Induction of cyclooxygenase-2 accounts for restraint stress-induced oxidative status in rat brain
    Jose L M Madrigal
    Department of Pharmacology, Faculty of Medicine, University of Complutense, 28040 Madrid, Spain
    Neuropsychopharmacology 28:1579-88. 2003
    ..These findings are discussed as possible damaging and/or adaptive roles for stress-induced COX-2 in the brain...
  33. ncbi Effects of celecoxib and rofecoxib on blood pressure and edema in patients > or =65 years of age with systemic hypertension and osteoarthritis
    Andrew Whelton
    Universal Clinical Research Center, Inc, and The Johns Hopkins University School of Medicine, Baltimore, Maryland 21030 1603, USA
    Am J Cardiol 90:959-63. 2002
    ..7%) compared with the celecoxib group (4.7%) (p <0.05). Thus, in patients with controlled hypertension on a fixed antihypertensive regimen, careful monitoring of BP is warranted after the initiation of celecoxib or rofecoxib therapy...
  34. ncbi Role of COX-2 in epithelial-stromal cell interactions and progression of ductal carcinoma in situ of the breast
    Min Hu
    Department of Medical Oncology, Dana Farber Cancer Institute, Boston, MA 02115, USA
    Proc Natl Acad Sci U S A 106:3372-7. 2009
    ....
  35. ncbi Cyclooxygenase-2--10 years later
    Burkhard Hinz
    Department of Experimental and Clinical Pharmacology and Toxicology, Friedrich Alexander University Erlangen Nurnberg, Erlangen, Germany
    J Pharmacol Exp Ther 300:367-75. 2002
    ..The present review assesses recent advances in COX-2 research, with particular emphasis on new insights into pathophysiological and physiological functions of this isoenzyme...
  36. ncbi Prevention and 18-month outcomes of serious pulmonary hemorrhage in extremely low birth weight infants: results from the trial of indomethacin prophylaxis in preterms
    Khalid Alfaleh
    Department of Pediatrics, McMaster University, Hamilton, Ontario, Canada
    Pediatrics 121:e233-8. 2008
    ..We also compared the 18-month outcomes of infants with and without a serious pulmonary bleed...
  37. ncbi Expression of cyclooxygenase 2 in human malignant melanoma
    C Denkert
    Institute of Pathology, , Berlin, Germany
    Cancer Res 61:303-8. 2001
    ..It remains to be investigated whether selective inhibitors of COX-2 might be useful for prevention or treatment of malignant melanoma...
  38. ncbi Inhibition of delayed rectifier potassium channels and induction of arrhythmia: a novel effect of celecoxib and the mechanism underlying it
    Roman V Frolov
    Department of Pharmacology and Toxicology, State University of New York, Buffalo, NY 14214, USA
    J Biol Chem 283:1518-24. 2008
    ..These observations reveal an unanticipated effect of celecoxib on Drosophila hearts and on heart cells from rats, implicating the inhibition of Kv2 channels as the mechanism underlying this effect...
  39. ncbi Targeting cyclooxygenase-2 in hematological malignancies: rationale and promise
    M P Bernard
    Department of Microbiology and Immunology, University of Rochester School of Medicine and Dentistry, Rochester, NY 14642, USA
    Curr Pharm Des 14:2051-60. 2008
    ..Therefore, Cox-2 selective inhibitors have promising therapeutic potential in patients suffering from certain hematological malignancies...
  40. ncbi MR monitoring of cyclooxygenase-2 inhibition of angiogenesis in a human breast cancer model in rats
    Laure S Fournier
    Center for Pharmaceutical and Molecular Imaging, University of California, San Francisco, USA
    Radiology 243:105-11. 2007
    ....
  41. ncbi NSAIDs and apoptosis
    N R Jana
    Cellular and Molecular Neuroscience Laboratory, National Brain Research Centre, Manesar, Gurgaon, India
    Cell Mol Life Sci 65:1295-301. 2008
    ..Both COX-2-dependent and COX-2-independent mechanisms are involved in NSAIDs-induced neoplastic growth. This article reviews the recent literature that has revealed various important mechanisms of NSAIDs-induced apoptosis...
  42. ncbi Gastrointestinal effects of nonsteroidal anti-inflammatory drugs
    Brendan J R Whittle
    William Harvey Research Institute, St Bartholomew s and the Royal London School of Medicine and Dentistry, Charterhouse Square, London EC1M 6BQ, UK
    Fundam Clin Pharmacol 17:301-13. 2003
    ..The clinical outcome of the use of the second generation of coxibs, and the newer NO NSAIDs is now awaited...
  43. ncbi Structural and functional basis of cyclooxygenase inhibition
    Anna L Blobaum
    A. B. Hancock Jr. Memorial Laboratory for Cancer Research, Department of Biochemistry, Vanderbilt Institute for Chemical Biology and Center in Molecular Toxicology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, USA
    J Med Chem 50:1425-41. 2007
  44. ncbi Cyclooxygenase-2 expression is induced in rat brain after kainate-induced seizures and promotes neuronal death in CA3 hippocampus
    Kenji Kawaguchi
    Department of Neurology, University of Pittsburgh, PA 15260, USA
    Brain Res 1050:130-7. 2005
    ..These results suggest that COX-2 activity can contribute to epileptic neuronal injury and that selective COX-2 inhibitors are neuroprotective...
  45. ncbi Clinical pharmacokinetics and pharmacodynamics of celecoxib: a selective cyclo-oxygenase-2 inhibitor
    N M Davies
    Faculty of Pharmacy, University of Sydney, New South Wales, Australia
    Clin Pharmacokinet 38:225-42. 2000
    ..As celecoxib is metabolised by CYP2C9, increased clinical vigilance is required during the coadministration of other substrates or inhibitors of this enzyme...
  46. ncbi Role of combination therapy with aromatase and cyclooxygenase-2 inhibitors in patients with metastatic breast cancer
    C Falandry
    Department of Medical Oncology, Centre Hospitalier Lyon Sud, Pierre Benite, France
    Ann Oncol 20:615-20. 2009
    ..Careful monitoring during future trials will be necessary to accurately assess the risk-benefit ratio of combination therapy...
  47. ncbi Cyclooxygenases: structural, cellular, and molecular biology
    W L Smith
    Department of Biochemistry, Michigan State University, East Lansing, MI 48824, USA
    Annu Rev Biochem 69:145-82. 2000
    ..We further examine the evidence for independent signaling by PGHS-1 and PGHS-2, and the complex mechanisms for regulation of PGHS-2 gene expression...
  48. ncbi Molecular cloning of human prostaglandin endoperoxide synthase type II and demonstration of expression in response to cytokines
    D A Jones
    Department of Internal Medicine, University of Utah, Salt Lake City 84112
    J Biol Chem 268:9049-54. 1993
    ..3-kb message is required for increased prostacyclin biosynthesis. We conclude that expression of PHS II may have important pathophysiological effects in the vasculature...
  49. ncbi Cyclooxygenase-2 inhibitor enhances the efficacy of a breast cancer vaccine: role of IDO
    Gargi D Basu
    Mayo Clinic College of Medicine, and Mayo Clinic Arizona, 13400 East Shea Boulevard, Scottsdale, AZ 85259, USA
    J Immunol 177:2391-402. 2006
    ..Thus, a novel mechanism of COX-2-induced immunosuppression via regulation of IDO has emerged that may have implications in designing future cancer vaccines...
  50. ncbi Changes in physicians' practice of prescribing cyclooxygenase-2 inhibitor after market withdrawal of rofecoxib: a retrospective study of physician-patient pairs in Taiwan
    Fei Yuan Hsiao
    Institute of Health and Welfare Policy, National Yang Ming University, Taipei, Taiwan
    Clin Ther 31:2618-27. 2009
    ..Safety concerns regarding severe cardiovascular events associated with the use of selective cyclooxygenase-2 (COX-2) inhibitors resulted in the market withdrawal of rofecoxib in September 2004...
  51. ncbi Predictors of failed closure of patent ductus arteriosus with indomethacin
    N Y Boo
    Department of Paediatrics, Faculty of Medicine, Hospital Universiti Kebangsaan Malaysia, Jalan Yaacob Latif, Cheras, Kuala Lumpur 56000, Malaysia
    Singapore Med J 47:763-8. 2006
    ..The aim of this study was to determine predictors of failed closure of patent ductus arteriosus (PDA) following a single course of indomethacin in symptomatic preterm infants...
  52. ncbi Furosemide in preterm infants treated with indomethacin for patent ductus arteriosus
    Peter Andriessen
    Department of Neonatology, Maxima Medical Centre, Veldhoven, The Netherlands
    Acta Paediatr 98:797-803. 2009
    ..To evaluate the effect of furosemide on renal function and water balance in preterm infants treated with indomethacin (3 x 0.2 mg/kg at 12-h intervals) for symptomatic patent ductus arteriosus. Patients and..
  53. ncbi Ibuprofen treatment for closure of patent ductus arteriosus is not associated with increased risk of neuropathology
    Michelle Loeliger
    Department of Anatomy and Cell Biology, University of Melbourne, Melbourne, Victoria 3010, Australia
    Pediatr Res 68:298-302. 2010
    ..No overt cerebellar alterations were observed in either group. Ibuprofen treatment for PDA closure in the preterm baboon neonate is not associated with any increased risk of neuropathology or alterations to brain growth and development...
  54. ncbi Mechanisms of Kv2.1 channel inhibition by celecoxib--modification of gating and channel block
    R V Frolov
    Department of Pharmacology and Toxicology, State University of New York, Buffalo, New York 14214 3000, USA
    Br J Pharmacol 159:405-18. 2010
    ..1 and other ion channels. In this study, we investigated the mechanism of the action of celecoxib on K(v)2.1 channels...
  55. ncbi COX-2 inhibition improves immune system homeostasis and decreases liver damage in septic rats
    Bin Li
    Department of General Surgery, the First Hospital of Lanzhou University, Gansu, China
    J Surg Res 157:43-7. 2009
    ..To evaluate cyclooxygenase-2 (COX-2) inhibition by NS-398 in septic rats with respect to immunologic derangements and hepatic damage...
  56. ncbi Celecoxib shown effective in preventing colon polyps
    Nancy J Nelson
    J Natl Cancer Inst 98:665-7. 2006
  57. ncbi Potential cancer chemopreventive agents from Arbutus unedo
    Esperanza J Carcache-Blanco
    Program for Collaborative Research in the Pharmaceutical Sciences and Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, Chicago, IL 60612, USA
    Nat Prod Res 20:327-34. 2006
    ..Activity in the JB6 cell transformation assay was found for pomolic acid 3-acetate (4). All isolates obtained were evaluated in a cyclooxygenase-2 (COX-2) inhibition assay...
  58. ncbi Biochemistry of cyclooxygenase (COX)-2 inhibitors and molecular pathology of COX-2 in neoplasia
    E Fosslien
    Department of Pathology, College of Medicine, University of Illinois at Chicago, 60612, USA
    Crit Rev Clin Lab Sci 37:431-502. 2000
    ..These findings might somewhat limit the use of presently available selective COX-2 inhibitors in cancer prevention but will probably not deter their successful application for the treatment of human cancers...
  59. ncbi Flavocoxid, a dual inhibitor of cyclooxygenase and 5-lipoxygenase, blunts pro-inflammatory phenotype activation in endotoxin-stimulated macrophages
    D Altavilla
    Department of Clinical and Experimental Medicine and Pharmacology, University of Messina, Messina, Italy
    Br J Pharmacol 157:1410-8. 2009
    ..The anti-inflammatory activity, measured by protein and gene expression of inflammatory markers, of flavocoxid in rat peritoneal macrophages stimulated with Salmonella enteritidis lipopolysaccharide (LPS) was investigated...
  60. ncbi The additive antinociceptive interaction between WIN 55,212-2, a cannabinoid agonist, and ketorolac
    Ahmet Ulugol
    Department of Pharmacology, Trakya University, Edirne, Turkey
    Anesth Analg 102:443-7. 2006
    ..This study demonstrated an additive antinociceptive interaction between WIN 55,212-2 and ketorolac in an inflammatory visceral pain model. The combination of cannabinoids and NSAIDs may have utility in the pharmacotherapy of pain...
  61. ncbi Discovery of cyclooxygenase inhibitors from medicinal plants used to treat inflammation
    Hongmei Cao
    Department of Medicinal Chemistry and Pharmacognosy, University of Illinois College of Pharmacy, 833 S Wood Street, Chicago, IL, USA
    Pharmacol Res 61:519-24. 2010
    ..Roburic acid and phenethyl-trans-ferulate inhibited COX-1 and COX-2 equally. COX inhibition and the IC(50) values of most of these natural product ligands have not been reported previously...
  62. ncbi A review of the gastrointestinal safety data--a gastroenterologist's perspective
    Angel Lanas
    Servicio de Aparato Digestivo, Hospital Clinico Universitario, C San Juan Bosco 15, 50009 Zaragoza, Spain
    Rheumatology (Oxford) 49:ii3-10. 2010
    ..To facilitate such studies a new endpoint, Clinically Significant Upper or Lower GI Events, has been introduced that captures both upper and lower GI events...
  63. ncbi Eudragit S-100 entrapped chitosan microspheres of valdecoxib for colon cancer
    Naveen K Thakral
    Centre for Biomedical Engineering, Indian Institute of Technology Delhi, Hauz Khas, New Delhi, 110016, India
    J Mater Sci Mater Med 21:2691-9. 2010
    ..4 for 30 min, when applied to mucosal surface of freshly excised goat colon, showed good mucoadhesion. The drug release at pH 7.4 and good mucoadhesive property of the microspheres make the system ideal for colonic delivery...
  64. ncbi Efficacy and safety of flavocoxid, a novel therapeutic, compared with naproxen: a randomized multicenter controlled trial in subjects with osteoarthritis of the knee
    Robert M Levy
    Primus Pharmaceuticals, Inc, Scottsdale, AZ 85251, USA
    Adv Ther 27:731-42. 2010
    ..This study was designed to compare the effectiveness and safety of flavocoxid to naproxen in subjects with moderate to severe osteoarthritis (OA) of the knee...
  65. ncbi Flavocoxid, a dual inhibitor of cyclooxygenase-2 and 5-lipoxygenase, reduces pancreatic damage in an experimental model of acute pancreatitis
    F Polito
    Department of Clinical and Experimental Medicine and Pharmacology, Section of Pharmacology, University of Messina, Messina, Italy
    Br J Pharmacol 161:1002-11. 2010
    ..We studied the effects of flavocoxid, a plant-derived dual inhibitor of COX-2 and 5-LOX, in a model of caerulein (CER)-induced acute pancreatitis...
  66. ncbi Low-dose aspirin, coxibs, and other NSAIDS: a clinical mosaic emerges
    Carlo Patrono
    Department of Pharmacology, Catholic University School of Medicine, Rome, Italy
    Mol Interv 9:31-9. 2009
    ..In this Review, the authors offer an assessment of drug pharmacokinetics and enzyme physiology that reconciles cardiovascular appraisals from a wide array of clinical data...
  67. ncbi Cyclooxygenase-inhibiting nitric oxide donators for osteoarthritis
    John L Wallace
    Farncombe Family Digestive Health Research Institute, McMaster University, Hamilton, Ontario, L8N 3Z5, Canada
    Trends Pharmacol Sci 30:112-7. 2009
    ..We provide an outline of the rationale for CINODs and their activity, in addition to an overview of the pre-clinical and clinical profile of the most advanced CINOD, naproxcinod...
  68. ncbi Cyclooxygenase inhibitors block uterine tumorigenesis in HMGA1a transgenic mice and human xenografts
    Francescopaolo Di Cello
    Hematology Division, The Johns Hopkins University School of Medicine, Baltimore, MD 21205, USA
    Mol Cancer Ther 7:2090-5. 2008
    ..Importantly, these drugs have lower toxicity than chemotherapeutic agents used to treat advanced-stage uterine cancers...
  69. ncbi Cyclooxygenase-2 selective non-steroidal anti-inflammatory drugs (etodolac, meloxicam, celecoxib, rofecoxib, etoricoxib, valdecoxib and lumiracoxib) for osteoarthritis and rheumatoid arthritis: a systematic review and economic evaluation
    Y F Chen
    Department of Public Health and Epidemiology, University of Birmingham, UK
    Health Technol Assess 12:1-278, iii. 2008
    ....
  70. ncbi Synergy between enzyme inhibitors of fatty acid amide hydrolase and cyclooxygenase in visceral nociception
    Pattipati S Naidu
    Department of Pharmacology and Toxicology, Medical College of Virginia Campus, Virginia Commonwealth University, Richmond, Virginia 23298 0613, USA
    J Pharmacol Exp Ther 329:48-56. 2009
    ....
  71. ncbi Oxidative stress mediates chemical hypoxia-induced injury and inflammation by activating NF-κb-COX-2 pathway in HaCaT cells
    Chuntao Yang
    Department of Physiology, Zhongshan School of Medicine, Sun Yat Sen University, Guangdong, People s Republic of China
    Mol Cells 31:531-8. 2011
    ..In conclusion, our results demonstrated that oxidative stress mediates chemical hypoxia-induced injury and inflammatory response through activation of NF-κB-COX-2 pathway in HaCaT cells...
  72. ncbi Effects of cyclooxygenase inhibitors on parasite burden, anemia and oxidative stress in murine Trypanosoma cruzi infection
    Vera L Hideko Tatakihara
    Departamento de Ciências Patológicas, Centro de Ciencias Biologicas, Universidade Estadual de Londrina, Parana, Brazil
    FEMS Immunol Med Microbiol 52:47-58. 2008
    ....
  73. ncbi Cyclooxygenase-2 inhibitors in colorectal cancer prevention: point
    Nadir Arber
    Integrated Cancer Prevention Center, Tel Aviv Sourasky Medical Center and Sackler Faculty of Medicine, 6 Weizmann Street, Tel Aviv 64239, Israel
    Cancer Epidemiol Biomarkers Prev 17:1852-7. 2008
    ..Better patient selection and more effective and safer drugs are needed. Celecoxib is probably best used in a subset of individuals at moderate to high colorectal cancer risk and low risk of cardiovascular disease...
  74. ncbi Non-steroidal anti-inflammatory drugs, Cyclooxygenase-2 inhibitors and paracetamol use in Queensland and in the whole of Australia
    Nadia Barozzi
    School of Pharmacy, University of Queensland, Steele Building, Brisbane, QLD 4072, Australia
    BMC Health Serv Res 8:196. 2008
    ..The aim of this study was to compare the utilization of non selective NSAID, COX-2 inhibitors and paracetamol between Queensland and Australia...
  75. ncbi A cyclooxygenase-2 (COX-2) inhibitor compared with dexamethasone in a survival study of rats with intracerebral 9L gliosarcomas
    Jana Portnow
    The Johns Hopkins Oncology Center, Baltimore, MD 21231-1000, USA
    Neuro Oncol 4:22-5. 2002
    ..2). These results suggest that a selective COX-2 inhibitor appears to be as effective as dexamethasone in prolonging survival in a rat brain tumor model...
  76. ncbi Mechanisms of anti-proliferative effect of JTE-522, a selective cyclooxygenase-2 inhibitor, on human liver cancer cells
    Takakazu Nagahara
    Second Department of Internal Medicine, Tottori University School of Medicine, 36 1 Nishi cho, Yonago, Tottori 683 8504, Japan
    Oncol Rep 18:1281-90. 2007
    ..Our data demonstrate that JTE-522 inhibited the growth of HCC cells in a COX-2-independent manner, and that the growth inhibition was in part mediated by the cell cycle arrest and the upregulation of PPAR-gamma protein...
  77. ncbi Inhibition of cyclooxygenases by dipyrone
    S C Pierre
    Pharmazentrum Frankfurt, ZAFES, Klinikum der Johann Wolfgang Goethe Universitat Frankfurt, Frankfurt, Germany
    Br J Pharmacol 151:494-503. 2007
    ..Here, we aimed to investigate the effects of dipyrone on COX...
  78. ncbi Cancer preventive phytochemicals as speed breakers in inflammatory signaling involved in aberrant COX-2 expression
    Young Joon Surh
    Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul, South Korea
    Curr Cancer Drug Targets 7:447-58. 2007
    ....
  79. ncbi Anti-apoptotic effects of arachidonic acid and prostaglandin E2 in pancreatic beta-cells
    Alexandros Papadimitriou
    Beta Cell Development and Function Group, School of Biomedical and Health Sciences, King s College London, London, UK
    Cell Physiol Biochem 20:607-16. 2007
    ..We have now investigated the anti-apoptotic effects of AA and its metabolite, PGE(2), in the MIN6 mouse insulin-secreting beta-cell line and mouse islets...
  80. ncbi Cyclooxygenase inhibitors: a novel direction for Alzheimer's management
    Manish Nivsarkar
    Department of Pharmacology and Toxicology, B V Patel Pharmaceutical Education and Research Development PERD Center, SG Highway, Thaltej, Ahmedabad 380 054, Gujarat, India
    Pharmacol Rep 60:692-8. 2008
    ..Further experimental work towards identifying the most efficacious COX-2 inhibitors, as well as the mechanism of action and the optimal dosage regimen should be executed...
  81. ncbi Role of coxibs in the strategies for gastrointestinal protection in patients requiring chronic non-steroidal anti-inflammatory therapy
    Corrado Blandizzi
    Division of Pharmacology and Chemotherapy, Department of Internal Medicine, University of Pisa, Via Roma 55, Pisa 56126, Italy
    Pharmacol Res 59:90-100. 2009
    ....
  82. ncbi Cyclooxygenase-2 inhibitors, nonsteroidal anti-inflammatory drugs, and cardiovascular risk
    Orly Vardeny
    School of Pharmacy, University of Wisconsin, 777 Highland Avenue, Madison, WI 53705 2222, USA
    Cardiol Clin 26:589-601. 2008
    ....
  83. ncbi Cyclooxygenase-2 mediates the delayed cardioprotection induced by hydrogen sulfide preconditioning in isolated rat cardiomyocytes
    Li Fang Hu
    Cardiovascular Biology Research Group, Department of Pharmacology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, Singapore
    Pflugers Arch 455:971-8. 2008
    ..In conclusion, we provided the first evidence that SP may produce delayed cardioprotection via K(ATP)/PKC dependent induction of COX-2 expression and via nitric oxide-induced COX-2 activation...
  84. ncbi NSAID use in individuals at risk of renal adverse events: an observational study to investigate trends in Australian veterans
    Elizabeth E Roughead
    Quality Use of Medicines and Pharmacy Research Centre, Sansom Institute, University of South Australia, Adelaide, South Australia 5001, Australia
    Drug Saf 31:997-1003. 2008
    ..Randomized clinical trials had demonstrated fewer adverse gastrointestinal events with COX-2 inhibitors, but no difference with other adverse events, including adverse renal events. There was a rapid uptake of these medicines...
  85. ncbi NSAIDs: gastroprotection or selective COX-2 inhibitor?
    Andrew Dickman
    Marie Curie Centre, Woolton, Liverpool, UK
    Palliat Med 18:275-86. 2004
    ..This review discusses the merits of both options and devises a treatment strategy for the safe and cost-effective use of these drugs in the palliative care population...
  86. ncbi Changes in osteoarthritis management by general practitioners in the COX2-inhibitor era-concomitant gastroprotective therapy
    Stéphane Bouée
    Cemka Eval, 43, boulevard du Maréchal Joffre, 92340 Bourg la Reine, France
    Joint Bone Spine 71:214-20. 2004
    ..We evaluated their use in the treatment of osteoarthritis by general practitioners, with special attention to concomitant prescription of gastroprotective agents...
  87. ncbi Multiple roles of COX-2 in tumor angiogenesis: a target for antiangiogenic therapy
    Stephen Gately
    Department of Translational Medicine, NeoPharm Inc, 150 Field Drive, Suite 195, Lake Forest, IL 60045, USA
    Semin Oncol 31:2-11. 2004
    ....
  88. ncbi Cyclooxygenase involvement in thromboxane-dependent contraction in rat mesenteric resistance arteries
    Manlio Bolla
    , Paris, France
    Hypertension 43:1264-9. 2004
    ..Inhibition by 3 chemically different cyclooxygenase inhibitors (ie, flurbiprofen, indomethacin, and aspirin) potently reduced the contraction to 27%, 25%, and 6% of ..
  89. ncbi Pathophysiology of vascular dysfunction in a rat model of chronic joint inflammation
    Colin G Egan
    Biological Sciences, University of Paisley, Paisley PA1 2BE, UK
    J Physiol 557:635-43. 2004
    ....
  90. ncbi Selective inhibitors of cyclooxygenase-2: a growing class of anti-inflammatory drugs
    I A Mardini
    Center for Experimental Therapeutics and Department of Anesthesia, University of Pennsylvania, Philadelphia, USA
    Mol Interv 1:30-8. 2001
    ....
  91. ncbi [Clinical pharmacology of selective inhibitors of cyclooxygenase-2]
    P Patrignani
    Dipartimento di Medicina e Centro di Eccellenza sull'Invecchiamento, , Chieti
    Acta Otorhinolaryngol Ital 23:13-8, 37-40. 2003
  92. ncbi [Safety of selective inhibitors of inducible cyclooxygenase-2 taken for a long period]
    Dominique Lamarque
    Unité d hépato gastroentérologie et service de chirurgie générale, Hotel Dieu, 1 place du parvis de Notre Dame, 75004 Paris
    Bull Cancer 91:S117-24. 2004
    ..The selective inhibitors may reduce the renal sodium excretion and increase the blood pressure, particularly in hypertensive patients whose the blood pressure has to be regularly checked...
  93. ncbi [Analgesic effects of cyclooxygenase 2 inhibitors]
    Christian Jayr
    DAAR Institut Gustave Roussy 39, rue Camille Desmoulins, 94805 Villejuif
    Bull Cancer 91:S125-31. 2004
    ....
  94. ncbi Docking studies on NSAID/COX-2 isozyme complexes using contact statistics analysis
    Giuseppe Ermondi
    Dipartimento di Scienza e Tecnologia del Farmaco, V P Giuria 9, 1 10125 Torino, Italy
    J Comput Aided Mol Des 18:683-96. 2004
    ..We use a combination of a traditional docking procedure with a new computational tool (Contact Statistics analysis) that identifies the best orientation among a number of solutions to shed some light on this topic...
  95. ncbi Interactions between aspirin and COX-2 inhibitors or NSAIDs in a rat thrombosis model
    Anwar Umar
    Department of Pharmacology, , 33076 Bordeaux, France
    Fundam Clin Pharmacol 18:559-63. 2004
    ..The interactions with aspirin do not seem to affect all NSAIDs to equal levels. The clinical impact of this needs to be confirmed in adequately powered clinical trials or pharmaco-epidemiological studies...
  96. ncbi Role of cyclooxygenase-2 in cytokine-induced beta-cell dysfunction and damage by isolated rat and human islets
    Monique R Heitmeier
    Department of Cardiovascular, Pfizer Global Research and Development, 700 Chesterfield Pkwy, West, Mail Code T2C, St Louis, MO 63017, USA
    J Biol Chem 279:53145-51. 2004
    ....
  97. ncbi Coxibs and cardiovascular disease
    Garret A Fitzgerald
    Institute for Translational Medicine and Therapeutics, University of Pennsylvania, Philadelphia, USA
    N Engl J Med 351:1709-11. 2004
  98. ncbi [Coxibs, which real therapeutic advance?: Recent pharmacoepidemiological data]
    Jean Louis Montastruc
    Service de Pharmacologie Clinique du Centre Hospitalier Universitaire de Toulouse, France
    Therapie 59:201-5. 2004
    ..Currently marketed coxibs do not appear to meet the previously defined criteria for therapeutic advance...
  99. ncbi [Therapeutic advances with coxibs: few certainties and a lot of doubts]
    Jean-Yves Jouzeau
    Laboratoire de Pharmacologie et UMR 7561 CNRS-UHP, , , France
    Therapie 59:207-11. 2004
  100. ncbi Tolerability of three selective cyclo-oxygenase-2 inhibitors, meloxicam, celecoxib and rofecoxib in NSAID-sensitive patients
    G Senna
    , Ospedale Civile Maggiore di Verona, Verona, Italy
    Allerg Immunol (Paris) 36:215-8. 2004
    ..However for this reason a controlled oral challenge with these drugs is useful for the proper management of patients sensitive to classic NSAIDs...
  101. ncbi Longer use of COX-2-specific inhibitors compared to nonspecific nonsteroidal antiinflammatory drugs: a longitudinal study of 3639 patients in community practice
    Frederick Wolfe
    National Data Bank for Rheumatic Diseases Arthritis Research Center Foundation, Wichita, Kansas 67214, USA
    J Rheumatol 31:355-8. 2004
    ..To compare COX-2-specific inhibitor therapy with conventional nonspecific nonsteroidal antiinflammatory drugs (NS NSAID), and investigate the effect of demographic and disease factors on NSAID duration of use...

Research Grants66

  1. FETAL REFLEX RESPONSES TO CEREBRAL HYPOPERFUSION
    Charles Wood; Fiscal Year: 1999
    ..Improvement of our knowledge of the rnle of prostanoids in the control of fetal blood pressure is also quite important in light of the use of prostaglandin synthase inhibitors clinically for various reasons, including tocolysis. ..
  2. NEURAL MECHANISMS OF PAIN AND HYPERALGESIA
    Jon Levine; Fiscal Year: 1993
    ..of leukotrienes (LTs), a newly discovered class of AA metabolites whose synthesis is not blocked by cyclooxygenase inhibitors. We showed that leukotriene B4 (LTB4), a product of the 5-lipoxygenase pathway of AA metabolism, reduced ..
  3. Use of Novel Cox-2 Inhibitors in Neurological Disorders
    STANLEY BELL; Fiscal Year: 2006
    ....
  4. Eicosanoids and Diabetic Retinopathy
    Rose Gubitosi Klug; Fiscal Year: 2007
    ..The candidate's preliminary data suggest that both lipoxygenase and cyclooxygenase inhibitors can ameliorate the high glucose-induced cell death seen in cultured retinal endothelial cells...
  5. PROSTANOID BIOSYNTHESIS IN SYSTEMIC MASTOCYTOSIS
    John Oates; Fiscal Year: 2003
    ..Inhibition of PGD2 biosynthesis with nonselective cyclooxygenase inhibitors (the nonsteroidal anti- inflammatory drugs) has been employed in the treatment of this disorder, but ..
  6. IMAGING COX-2 GENE EXPRESSION IN INFLAMMATION AND TUMORS
    Harvey Herschman; Fiscal Year: 2009
    ..Studies with this mouse will correlate optical and microPET imaging technologies. ..
  7. IMAGING COX-2 GENE EXPRESSION IN INFLAMMATION AND TUMORS
    Harvey Herschman; Fiscal Year: 2007
    ..Studies with this mouse will correlate optical and microPET imaging technologies. ..