1H-Pyrrolizine-5-acetic acid, 6-(4-chlorophenyl)-2,3-dihydro-2,2-dimethyl-7-phenyl-
| Title | Journal |
|---|---|
| Identification of potent Yes1 kinase inhibitors using a library screening approach. | Bioorganic & medicinal chemistry letters 20130801 |
| Licofelone inhibits interleukin-18-induced pro-inflammatory cytokine release and cellular proliferation in human mesangial cells. | Basic & clinical pharmacology & toxicology 20120901 |
| The decrease of cell membrane fluidity by the non-steroidal anti-inflammatory drug Licofelone inhibits epidermal growth factor receptor signalling and triggers apoptosis in HCA-7 colon cancer cells. | Cancer letters 20120828 |
| Ciliary beating is depressed in nasal cilia from chronic obstructive pulmonary disease subjects. | Respiratory medicine 20120801 |
| Efficient synthesis and 5-LOX/COX-inhibitory activity of some 3-hydroxybenzo[b]thiophene-2-carboxylic acid derivatives. | Bioorganic & medicinal chemistry letters 20120801 |
| Dynamic modeling of human 5-lipoxygenase-inhibitor interactions helps to discover novel inhibitors. | Journal of medicinal chemistry 20120322 |
| Targeting bone alleviates osteoarthritis in osteopenic mice and modulates cartilage catabolism. | PloS one 20120101 |
| Prostaglandins in cancer cell adhesion, migration, and invasion. | International journal of cell biology 20120101 |
| Anti-inflammatory drugs and prediction of new structures by comparative analysis. | Anti-inflammatory & anti-allergy agents in medicinal chemistry 20120101 |
| Chemoprevention of colon and small intestinal tumorigenesis in APC(Min/+) mice by licofelone, a novel dual 5-LOX/COX inhibitor: potential implications for human colon cancer prevention. | Cancer prevention research (Philadelphia, Pa.) 20111201 |
| Role of LOX/COX pathways in 3-nitropropionic acid-induced Huntington's disease-like symptoms in rats: protective effect of licofelone. | British journal of pharmacology 20110901 |
| Risk factors predictive of joint replacement in a 2-year multicentre clinical trial in knee osteoarthritis using MRI: results from over 6 years of observation. | Annals of the rheumatic diseases 20110801 |
| Chemopreventive efficacy and mechanism of licofelone in a mouse lung tumor model via aspiration. | Cancer prevention research (Philadelphia, Pa.) 20110801 |
| Licofelone-nitric oxide donors as anticancer agents. | Archiv der Pharmazie 20110801 |
| Chondroitin sulphate reduces both cartilage volume loss and bone marrow lesions in knee osteoarthritis patients starting as early as 6 months after initiation of therapy: a randomised, double-blind, placebo-controlled pilot study using MRI. | Annals of the rheumatic diseases 20110601 |
| Antibody-mediated 'universal' osteoclast targeting platform using calcitonin as a model drug. | Pharmaceutical research 20110501 |
| Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase. | Journal of medicinal chemistry 20110428 |
| Licofelone attenuates quinolinic acid induced Huntington like symptoms: possible behavioral, biochemical and cellular alterations. | Progress in neuro-psychopharmacology & biological psychiatry 20110330 |
| Investigations on cytotoxicity and anti-inflammatory potency of licofelone derivatives. | European journal of medicinal chemistry 20110301 |
| [Cyclooxygenases inhibitors and other compounds with antiinflammatory potential in osteoarthrosis--part I]. | Polski merkuriusz lekarski : organ Polskiego Towarzystwa Lekarskiego 20110101 |
| Tiludronate treatment improves structural changes and symptoms of osteoarthritis in the canine anterior cruciate ligament model. | Arthritis research & therapy 20110101 |
| The implications of relationships between human diseases and metabolic subpathways. | PloS one 20110101 |
| Molecular changes in articular cartilage and subchondral bone in the rat anterior cruciate ligament transection and meniscectomized models of osteoarthritis. | BMC musculoskeletal disorders 20110101 |
| Sequential alterations in catabolic and anabolic gene expression parallel pathological changes during progression of monoiodoacetate-induced arthritis. | PloS one 20110101 |
| Quantitative cartilage imaging in knee osteoarthritis. | Arthritis 20110101 |
| Decrease in serum level of matrix metalloproteinases is predictive of the disease-modifying effect of osteoarthritis drugs assessed by quantitative MRI in patients with knee osteoarthritis. | Annals of the rheumatic diseases 20101201 |
| Relationship between bone marrow lesions, cartilage loss and pain in knee osteoarthritis: results from a randomised controlled clinical trial using MRI. | Annals of the rheumatic diseases 20101201 |
| Licofelone attenuates MPTP-induced neuronal toxicity: behavioral, biochemical and cellular evidence. | Inflammopharmacology 20101001 |
| Anti-atherogenic effect of BHB-TZD having inhibitory activities on cyclooxygenase and 5-lipoxygenase in hyperlipidemic mice. | Atherosclerosis 20100901 |
| Identification and characterisation of new inhibitors for the human hematopoietic prostaglandin D2 synthase. | European journal of medicinal chemistry 20100201 |
| Pharmacophore modeling and virtual screening for designing potential 5-lipoxygenase inhibitors. | Bioorganic & medicinal chemistry letters 20100201 |
| Regulation of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase-activating protein/5-lipoxygenase by 4-hydroxynonenal in human osteoarthritic chondrocytes. | Arthritis research & therapy 20100101 |
| High mobility group box 1 potentiates the pro-inflammatory effects of interleukin-1β in osteoarthritic synoviocytes. | Arthritis research & therapy 20100101 |
| Oestrogen is important for maintenance of cartilage and subchondral bone in a murine model of knee osteoarthritis. | Arthritis research & therapy 20100101 |
| Upregulation of MMP-13 and TIMP-1 expression in response to mechanical strain in MC3T3-E1 osteoblastic cells. | BMC research notes 20100101 |
| Investigational pharmacology for low back pain. | Journal of pain research 20100101 |
| 5-lipoxygenase: underappreciated role of a pro-inflammatory enzyme in tumorigenesis. | Frontiers in pharmacology 20100101 |
| Protective effects of licofelone, a 5-lipoxygenase and cyclo-oxygenase inhibitor, versus naproxen on cartilage loss in knee osteoarthritis: a first multicentre clinical trial using quantitative MRI. | Annals of the rheumatic diseases 20090601 |
| Systematic review of the management of canine osteoarthritis. | The Veterinary record 20090404 |
| Protective effects of total fraction of avocado/soybean unsaponifiables on the structural changes in experimental dog osteoarthritis: inhibition of nitric oxide synthase and matrix metalloproteinase-13. | Arthritis research & therapy 20090101 |
| An exploration of the ability of tepoxalin to ameliorate the degradation of articular cartilage in a canine in vitro model. | BMC veterinary research 20090101 |
| Treatment with ephrin B2 positively impacts the abnormal metabolism of human osteoarthritic chondrocytes. | Arthritis research & therapy 20090101 |
| The target of arachidonic acid pathway is a new anticancer strategy for human prostate cancer. | Biologics : targets & therapy 20081201 |
| Licofelone suppresses prostaglandin E2 formation by interference with the inducible microsomal prostaglandin E2 synthase-1. | The Journal of pharmacology and experimental therapeutics 20080901 |
| In vitro metabolism of 2-[6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl] acetic acid (licofelone, ML3000), an inhibitor of cyclooxygenase-1 and -2 and 5-lipoxygenase. | Drug metabolism and disposition: the biological fate of chemicals 20080501 |
| The dual inhibitor of lipoxygenase and cyclooxygenase ML3000 decreases the expression of CXCR3 ligands. | Annals of the rheumatic diseases 20080401 |
| Gateways to clinical trials. | Methods and findings in experimental and clinical pharmacology 20080301 |
| Licofelone, a dual COX/5-LOX inhibitor, induces apoptosis in HCA-7 colon cancer cells through the mitochondrial pathway independently from its ability to affect the arachidonic acid cascade. | Carcinogenesis 20080201 |
| Cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) selectivity of COX inhibitors. | Prostaglandins, leukotrienes, and essential fatty acids 20080201 |
| A role for subchondral bone changes in the process of osteoarthritis; a micro-CT study of two canine models. | BMC musculoskeletal disorders 20080101 |
| Gateways to clinical trials. | Methods and findings in experimental and clinical pharmacology 20080101 |
| Licofelone: the answer to unmet needs in osteoarthritis therapy? | Current rheumatology reports 20080101 |
| Is collagenase-3 (MMP-13) expression in chondrosarcoma of the jaws a true marker for tumor aggressiveness? | Diagnostic pathology 20080101 |
| Diacerein inhibits the synthesis of resorptive enzymes and reduces osteoclastic differentiation/survival in osteoarthritic subchondral bone: a possible mechanism for a protective effect against subchondral bone remodelling. | Arthritis research & therapy 20080101 |
| Finding multiple target optimal intervention in disease-related molecular network. | Molecular systems biology 20080101 |
| Analysis of the precision and sensitivity to change of different approaches to assess cartilage loss by quantitative MRI in a longitudinal multicentre clinical trial in patients with knee osteoarthritis. | Arthritis research & therapy 20080101 |
| Combination Therapy of PPARgamma Ligands and Inhibitors of Arachidonic Acid in Lung Cancer. | PPAR research 20080101 |
| Comparative protection against liver inflammation and fibrosis by a selective cyclooxygenase-2 inhibitor and a nonredox-type 5-lipoxygenase inhibitor. | The Journal of pharmacology and experimental therapeutics 20071201 |
| The molecular mechanism of the inhibition by licofelone of the biosynthesis of 5-lipoxygenase products. | British journal of pharmacology 20071001 |
| Gastrointestinal safety of novel nonsteroidal antiinflammatory drugs: selective COX-2 inhibitors and beyond. | Acta bio-medica : Atenei Parmensis 20070801 |
| Efficacy of licofelone in dogs with clinical osteoarthritis. | The Veterinary record 20070428 |
| Dynamic simulations on the arachidonic acid metabolic network. | PLoS computational biology 20070301 |
| Activity and potential role of licofelone in the management of osteoarthritis. | Clinical interventions in aging 20070301 |
| Arthritis clinical trial results revealed. | JAMA 20070103 |
| Licofelone, a balanced inhibitor of cyclooxygenase and 5-lipoxygenase, reduces inflammation in a rabbit model of atherosclerosis. | The Journal of pharmacology and experimental therapeutics 20070101 |
| Licofelone--a novel analgesic and anti-inflammatory agent. | Current topics in medicinal chemistry 20070101 |
| Selection of reliable reference genes for qPCR studies on chondroprotective action. | BMC molecular biology 20070101 |
| Extracellular localization of galectin-3 has a deleterious role in joint tissues. | Arthritis research & therapy 20070101 |
| Anticancer effects of licofelone (ML-3000) in prostate cancer cells. | Anticancer research 20070101 |
| DMOAD developments: present and future. | Bulletin of the NYU hospital for joint diseases 20070101 |
| Activation of proteinase-activated receptor 2 in human osteoarthritic cartilage upregulates catabolic and proinflammatory pathways capable of inducing cartilage degradation: a basic science study. | Arthritis research & therapy 20070101 |
| Effects on primary haemostasis of an anti-inflammatory agent with 5-lipoxygenase and cyclooxygenase inhibitory activity. | Journal of cardiovascular medicine (Hagerstown, Md.) 20061201 |
| The lipoxygenase-cyclooxygenase inhibitor licofelone prevents thromboxane A2-mediated cardiovascular derangement triggered by the inflammatory peptide fMLP in the rabbit. | European journal of pharmacology 20060928 |
| Licofelone reduces progression of structural changes in a canine model of osteoarthritis under curative conditions: effect on protease expression and activity. | The Journal of rheumatology 20060601 |
| Anti-inflammatory effect of licofelone against various inflammatory challenges. | Fundamental & clinical pharmacology 20060201 |
| Most recent developments in strategies to reduce the progression of structural changes in osteoarthritis: today and tomorrow. | Arthritis research & therapy 20060101 |
| Licofelone, a novel 5-LOX/COX-inhibitor, attenuates leukocyte rolling and adhesion on endothelium under flow. | Biochemical pharmacology 20050701 |
| The regulation of human MMP-13 by licofelone, an inhibitor of cyclo-oxygenases and 5-lipoxygenase, in human osteoarthritic chondrocytes is mediated by the inhibition of the p38 MAP kinase signalling pathway. | Annals of the rheumatic diseases 20050601 |
| Eicosanoids, osteoarthritis, and crystal deposition diseases. | Current opinion in rheumatology 20050501 |
| Dual inhibition of cyclo-oxygenases and 5-lipoxygenase: a novel therapeutic approach to inflammation? | Joint, bone, spine : revue du rhumatisme 20050501 |
| Leukotriene and prostaglandin synthesis pathways in osteoarthritic synovial membranes: regulating factors for interleukin 1beta synthesis. | The Journal of rheumatology 20050401 |
| Effect of licofelone against NSAIDs-induced gastrointestinal ulceration and inflammation. | Indian journal of experimental biology 20050301 |
| Superiority of the gastroduodenal safety profile of licofelone over rofecoxib, a COX-2 selective inhibitor, in dogs. | Journal of veterinary pharmacology and therapeutics 20050201 |
| Combined lipoxygenase/cyclo-oxygenase inhibition in the elderly: the example of licofelone. | Drugs & aging 20050101 |
| Effect of licofelone against mechanical hyperalgesia and cold allodynia in the rat model of incisional pain. | Pharmacological reports : PR 20050101 |
| The protective effect of licofelone on experimental osteoarthritis is correlated with the downregulation of gene expression and protein synthesis of several major cartilage catabolic factors: MMP-13, cathepsin K and aggrecanases. | Arthritis research & therapy 20050101 |
| Regulation of the expression of 5-lipoxygenase-activating protein/5-lipoxygenase and the synthesis of leukotriene B(4) in osteoarthritic chondrocytes: role of transforming growth factor beta and eicosanoids. | Arthritis and rheumatism 20041201 |
| Pain and osteoarthritis: new drugs and mechanisms. | Current opinion in rheumatology 20040901 |
| Gateways to clinical trials. | Methods and findings in experimental and clinical pharmacology 20040901 |
| The gastrointestinal tolerability of the LOX/COX inhibitor, licofelone, is similar to placebo and superior to naproxen therapy in healthy volunteers: results from a randomized, controlled trial. | The American journal of gastroenterology 20040401 |
| Licofelone, an inhibitor of cyclooxygenase and 5-lipoxygenase, specifically inhibits cyclooxygenase-1-dependent platelet activation. | European journal of pharmacology 20040319 |
| The inhibition of subchondral bone resorption in the early phase of experimental dog osteoarthritis by licofelone is associated with a reduction in the synthesis of MMP-13 and cathepsin K. | Bone 20040301 |
| Is licofelone, a dual inhibitor of cyclo-oxygenase and 5-lipoxygenase, a promising alternative in anti-inflammatory therapy? | Fundamental & clinical pharmacology 20040201 |
| Osteoarthritis therapy--are there still unmet needs? | Rheumatology (Oxford, England) 20040201 |
| Safety of anti-inflammatory treatment--new ways of thinking. | Rheumatology (Oxford, England) 20040201 |
| Licofelone--clinical update on a novel LOX/COX inhibitor for the treatment of osteoarthritis. | Rheumatology (Oxford, England) 20040201 |
| Treatment with licofelone prevents abnormal subchondral bone cell metabolism in experimental dog osteoarthritis. | Annals of the rheumatic diseases 20040101 |
| Gateways to clinical trials. | Methods and findings in experimental and clinical pharmacology 20040101 |
| Inhibition of gastric H,K-ATPase activity and gastric epithelial cell IL-8 secretion by the pyrrolizine derivative ML 3000. | BMC gastroenterology 20040101 |
| Gateways to clinical trials. | Methods and findings in experimental and clinical pharmacology 20031201 |
| Evidence that 5-lipoxygenase and acetylated cyclooxygenase 2-derived eicosanoids regulate leukocyte-endothelial adherence in response to aspirin. | British journal of pharmacology 20030801 |
| Licofelone (Merckle). | IDrugs : the investigational drugs journal 20030801 |
| International Conference on Inflammopharmacology -- VIII Side-Effects of Anti-inflammatory Drugs Symposium. | Expert opinion on investigational drugs 20030701 |
| The metabolic effects of inhibitors of 5-lipoxygenase and of cyclooxygenase 1 and 2 are an advancement in the efficacy and safety of anti-inflammatory therapy. | Prostaglandins & other lipid mediators 20030701 |
| Relative contribution of acetylated cyclo-oxygenase (COX)-2 and 5-lipooxygenase (LOX) in regulating gastric mucosal integrity and adaptation to aspirin. | FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20030601 |
| Anti arthritic drugs--SMi conference: dual inhibitors. 28-29 April 2003, London, UK. | IDrugs : the investigational drugs journal 20030601 |
| COX-LOX inhibition: current evidence for an emerging new therapy. | International journal of clinical practice 20030501 |
| Licofelone, a dual lipoxygenase-cyclooxygenase inhibitor, downregulates polymorphonuclear leukocyte and platelet function. | European journal of pharmacology 20021018 |
| Gateways to clinical trials. | Methods and findings in experimental and clinical pharmacology 20021001 |
| Study of the role of leukotriene B()4 in abnormal function of human subchondral osteoarthritis osteoblasts: effects of cyclooxygenase and/or 5-lipoxygenase inhibition. | Arthritis and rheumatism 20020701 |
| Licofelone (ML-3000), a dual inhibitor of 5-lipoxygenase and cyclooxygenase, reduces the level of cartilage chondrocyte death in vivo in experimental dog osteoarthritis: inhibition of pro-apoptotic factors. | The Journal of rheumatology 20020701 |
| Antithrombotic and platelet function inhibiting effects of ML3000, a new antiinflammatory drug with Cox/5-LOX inhibitory activity. | Inflammation research : official journal of the European Histamine Research Society ... [et al.] 20020301 |
| The mechanism of action of the new antiinflammatory compound ML3000: inhibition of 5-LOX and COX-1/2. | Inflammation research : official journal of the European Histamine Research Society ... [et al.] 20020301 |
| In vivo dual inhibition of cyclooxygenase and lipoxygenase by ML-3000 reduces the progression of experimental osteoarthritis: suppression of collagenase 1 and interleukin-1beta synthesis. | Arthritis and rheumatism 20011001 |
| [Double blockade should protect the stomach. New approach to rheumatism]. | MMW Fortschritte der Medizin 20010920 |
| Dual inhibition of 5-lipoxygenase and cyclooxygenases 1 and 2 by ML3000 reduces joint destruction in adjuvant arthritis. | The Journal of rheumatology 20010901 |