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  • inhibition
  • However, with regard to this drug's promise for the therapy of advanced cancers, it is unclear whether the inhibition of COX-2 plays a dominant role, and this has become a controversial and intensely researched issue. (wikipedia.org)
  • Like its ability to control pain, aspirin's ability to control fever is due to its action on the prostaglandin system through its irreversible inhibition of COX. (wikipedia.org)
  • analgesic
  • COX-2 inhibitors are important drugs with analgesic and anti-inflammatory effects. (booktopia.com.au)
  • Hemicrania was mentioned in 1881 in The Therapeutic Gazette Vol. 2, by G.S.Davis, and the incident has been cited in King's American Dispensatory (1898 and later editions) in the description of the strong analgesic Jamaican Dogwood, a relatively low dose of which reportedly produced convulsions and prolonged respiratory depression over six hours in an elderly woman with this condition. (wikipedia.org)
  • potent
  • The researchers were able to achieve similar heart-stopping results in rat cardiac cells, whereas aspirin, another potent COX-2 inhibitor, had no effect, confirming that another mechanism is at work. (newsinferno.com)
  • Bextra
  • LOS ANGELES (CBS.MW) -- The U.S. Food and Drug Administration has called for evaluation of Cox-2 inhibitors such as Celebrex and Bextra, the agency said Thursday. (marketwatch.com)
  • On September 2, 2009, the United States Department of Justice fined Pfizer $2.3 billion after one of its subsidiaries, Pharmacia & UpJohn Company, pleaded guilty to marketing four drugs including Bextra "with the intent to defraud or mislead. (wikipedia.org)
  • prevention
  • The study, published in the August 1 issue of Cancer Research, a journal of the American Association for Cancer Research, suggests a potential role for COX-2 inhibitors in pancreatic cancer prevention among high-risk patients. (innovations-report.com)
  • COX-2 Inhibitors for Cancer Prevention & Treatment: Research. (lww.com)
  • So said Andrew J. Dannenberg, MD, Director of Cancer Prevention at New York Weill Cornell Medical Center, speaking at a news briefing here called "From Arthritis to Cancer-A New View of COX-2. (lww.com)
  • tumors
  • Studies of breast, colon, and pancreatic cancers have led researchers to believe COX-2 plays a key role in the development and growth of tumors. (innovations-report.com)
  • COX-2 cannot be detected in most normal tissues, but is induced by oncogenes and overexpressed in premalignant and malignant tumors, Dr. Dannenberg said. (lww.com)
  • The antiangiogenic properties of COX-2 inhibitors may be independent of COX-2 expression in tumors, Dr. Li added. (lww.com)
  • Because virtually all tumors undergo infiltration by inflammatory cells such as monocytes and macrophages, COX-2 inhibitors could help to suppress the angiogenesis promulgated by these pre-tumoral cell elements. (lww.com)
  • clinical trials
  • After several COX-2 inhibiting drugs were approved for marketing, data from clinical trials revealed that COX-2 inhibitors caused a significant increase in heart attacks and strokes, with some drugs in the class having worse risks than others. (wikipedia.org)
  • novel
  • In 1991, during the investigation of the expression of early-response genes in fibroblasts transformed with Rous sarcoma virus, a novel mRNA transcript that was similar, but not identical, to the seminal COX enzyme was identified. (wikipedia.org)
  • Another group discovered a novel cDNA species encoding a protein with similar structure to COX-1 while studying phorbol-ester-induced genes in Swiss 3T3 cells. (wikipedia.org)
  • The same laboratory showed that this gene truly expressed a novel COX enzyme. (wikipedia.org)
  • effects
  • See 'COX-2 selective inhibitors: Adverse cardiovascular effects' . (uptodate.com)
  • To study the effects of COX-2 on PanIN progression, Dr. Eibl and colleagues focused on the KrasG12D mouse, an animal model that mimics the early stages of pancreatic cancer. (innovations-report.com)
  • In the future, Dr. Eibl and others plan to study the long-term effects of nimesulide and additional COX-2 inhibitors on the onset and progression of pancreatic cancer. (innovations-report.com)
  • They also stress it is too early to speculate on human effects, although their results suggest Drosophilaâ€"one of the most valuable of organisms in biological research and has been used as a model research organism for almost a centuryâ€"are a valuable tool to investigate other COX-2 drugs. (newsinferno.com)
  • Inc. (Novartis) to remove (recall) all lumiracoxib from local drug stores in 2 weeks due to the harmful effects of the drug (potential serious liver-related side effects, hepatotoxicity or malfunction of the lungs). (wikipedia.org)
  • Tramadol is structurally closer to venlafaxine than to codeine and delivers analgesia by not only delivering "opioid-like" effects (through mild agonism of the mu receptor) but also by acting as a weak but fast-acting serotonin releasing agent and norepinephrine reuptake inhibitor. (wikipedia.org)
  • pathways
  • COX-2 inhibitors have been found to be effective in suppressing inflammatory neurodegenerative pathways in mental illness, with beneficial results in trials for major depressive disorder as well as schizophrenia . (wikipedia.org)
  • The COX-2 system appears to play a role in a number of pathways to cancer, another expert, David Weinberg, MD, Director of Gastroenterology at Fox Chase Cancer Center in Philadelphia, noted in an interview. (lww.com)
  • Hence, COX-2 is targeted in the sense that it preferentially affects the bad pathways while sparing the good. (lww.com)
  • disorders
  • Mark Thompson, "Hemicrania Continua" "The International Classification of Headache Disorders 2nd Edition (ICHD-2)" (PDF). (wikipedia.org)
  • kidney
  • A new study tests the hypothesis that altered kidney regulation of COX-2 occurs at a very early stage in the progression of kidney disease. (innovations-report.com)
  • increased COX-2 protein expression was observed in the kidney cortex and microvessels of the Obese Zucker rats at 10-12 and 20-21 weeks of age. (innovations-report.com)
  • pain
  • It treats pain mainly by blocking COX-2 mostly in the central nervous system, but not much in the rest of the body. (wikipedia.org)
  • analogue
  • Reaction of the imine with TosMIC in the presence of potassium carbonate leads to what may be viewed as 2+3 cycloaddition of the nitrogen analogue of a ketene to form the imidazole ring. (wikipedia.org)
  • enzyme
  • Since COX-1 prostaglandins are stomach-protective, blocking this enzyme is associated with gastrointestinal toxicity, a known side effect of these drugs. (oakhillhospital.com)
  • Each monomer of the enzyme has a peroxidase and a PTGS (COX) active site. (wikipedia.org)
  • Researchers from the Wellcome Trust Sanger Institute reported that the mutation of CUX1 reduces the inhibitory effects of a biological inhibitor, PIK3IP1 (phosphoinositide-3-kinase interacting protein 1), resulted in higher activity of the growth promoting enzyme, phosphoinositide 3-kinase (PI3K) which leads to tumor progression. (wikipedia.org)
  • Squalene monooxygenase (also called squalene epoxidase) is an enzyme that uses NADPH and molecular oxygen to oxidize squalene to 2,3-oxidosqualene (squalene epoxide). (wikipedia.org)
  • Inhibitors of squalene epoxidase have found application mainly as antifungal drugs: butenafine naftifine terbinafine Since squalene epoxidase is on the biosynthetic pathway leading to cholesterol, inhibitors of this enzyme may also find application in treatment of hypercholesterolemia. (wikipedia.org)
  • substrates
  • COX-2 is naturally inhibited by Calcitriol (the active form of Vitamin D). Both the peroxidase and PTGS activities are inactivated during catalysis by mechanism-based, first-order processes, which means that PGHS-2 peroxidase or PTGS activities fall to zero within 1-2 minutes, even in the presence of sufficient substrates. (wikipedia.org)
  • Following is a table of selected substrates, inducers and inhibitors of CYP2B6. (wikipedia.org)
  • Drugs
  • For patients at low risk of gastrointestinal complications, nonsteroidal anti-inflammatory drugs may be used, whereas cotherapy with a proton pump inhibitor or misoprostol (Cytotec) is recommended for patients with moderate risk of ulcer, and they should be avoided in those with a high risk of ulcer. (aafp.org)
  • Vildagliptin (previously LAF237, trade names Galvus, Zomelis,) is an oral anti-hyperglycemic agent (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. (wikipedia.org)
  • protein
  • An ESR of more than 37.5 mm/hour was found to be the optimal threshold value for predicting prognosis.RESULTS: ESR was associated with more frequent advanced Ann Arbor stage, poorer performance status, elevated lactate dehydrogenase level, the presence of B symptoms, high-risk International Prognostic Index (IPI 3-5), more extranodal involvement (ENI ≥2), non-germinal-center B-cell (non-GCB) subtypes, and more frequent Myc protein positivity. (slesystems.com)
  • Cux1 DNA binding is stimulated by activation of the PAR2/F2RL1 cell-surface G-protein-coupled receptor in fibroblasts and breast-cancer epithelial cells to regulate Matrix metalloproteinase 10, Interleukin1-alpha, and Cyclo-oxygenase 2 (COX2) genes. (wikipedia.org)
  • activity
  • The ADD domain serves as an inhibitor of the methyltransferase domain until DNMT3A binds to the unmodified lysine 4 of histone 3 (H3K4me0) for its de novo methylating activity. (wikipedia.org)
  • Causes
  • Inhibitors of CYP2B6 can be classified by their potency, such as: Strong inhibitor being one that causes at least a 5-fold increase in the plasma AUC values, or more than 80% decrease in clearance. (wikipedia.org)
  • found
  • Another study found that a different Tph1-inhibitor decreased serotonin levels in the blood and intestine, but did not affect bone mass or markers of bone formation. (wikipedia.org)
  • group
  • A group at UCLA reported increased pre-cancerous pancreatic changes in rats and in human organ donors who had been treated with DPP-IV inhibitors. (wikipedia.org)
  • Development of dipeptidyl peptidase-4 inhibitors Dipeptidyl peptidase-4 (CD26) WHO International Working Group for Drug Statistics Methodology (August 27, 2008). (wikipedia.org)
  • data
  • In response to these reports, the United States FDA and the European Medicines Agency each undertook independent reviews of all clinical and preclinical data related to the possible association of DPP-IV inhibitors with pancreatic cancer. (wikipedia.org)
  • market
  • However, this is not proven, and some COX-2s have been taken off the market due to excess risk of heart attacks attributable to their use. (oakhillhospital.com)
  • days
  • Early infection consists of stage 1 (localized skin infection), followed within days to weeks by stage 2 (disseminated infection). (asmscience.org)
  • either
  • In the first double-blind, placebo-controlled study, 103 people with BPH were assigned to take either placebo or 2 capsules of a standardized grass pollen extract 3 times daily for a period of 12 weeks. (sahealth.com)
  • type
  • Vildagliptin has been shown to reduce hyperglycemia in type 2 diabetes mellitus. (wikipedia.org)
  • stage
  • A stage 2 clinical trial investigating the efficacy and security of While602801, a recently developed JNK inhibitor, in the treating inflammatory endometriosis is complete. (biomasswars.com)