Search Results - "de Leval, Xavier"
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1
Regulation of HER-2 oncogene expression by cyclooxygenase-2 and prostaglandin E2
Published in Oncogene (26-02-2004)“…The oncoprotein HER-2/neu is a prosurvival factor and its overexpression has been correlated with adverse prognosis in breast cancers. High levels of the…”
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2
Therapeutic potential of thromboxane inhibitors in asthma
Published in Expert opinion on investigational drugs (01-02-2002)“…This paper reviews the role of thromboxane A(2) (TXA(2)) in the pathogenesis of pulmonary allergies, particularly asthma. The potential of TXA(2) modifiers in…”
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3
New trends in dual 5-LOX/COX inhibition
Published in Current medicinal chemistry (01-05-2002)“…Dual inhibitors are drugs able to block both the COX and the 5-LOX metabolic pathways. The interest of developing such compounds is supported by a large number…”
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4
Evaluation of original dual thromboxane A2 modulators as antiangiogenic agents
Published in The Journal of pharmacology and experimental therapeutics (01-09-2006)“…Angiogenesis is a promising target for the therapy of several diseases including cancer. This study was undertaken to characterize the antiangiogenic…”
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5
Recent advances in inducible cyclooxygenase (COX-2) inhibition
Published in Current medicinal chemistry (01-10-2000)“…Cyclooxygenase is the key enzyme in the biosynthesis of prostanoids, biologically active substances that are involved in several physiological processes but…”
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6
New trends in thromboxane and prostacyclin modulators
Published in Current medicinal chemistry (01-06-2000)“…Thromboxane A2 (TXA2) and prostacyclin (PGI2) are two labile products formed from arachidonic acid by the way of cyclooxygenase. An overproduction of…”
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7
Carbonic Anhydrase Inhibitors: Synthesis and Topical Intraocular Pressure Lowering Effects of Fluorine-Containing Inhibitors Devoid of Enhanced Reactivity
Published in Journal of medicinal chemistry (20-05-2004)“…Polyfluorinated carbonic anhydrase inhibitors (CAIs) show very good inhibitory properties against carbonic anhydrase (CA) and excellent in vivo antiglaucoma…”
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8
N-(3-Arylaminopyridin-4-yl)alkanesulfonamides as pyridine analogs of nimesulide: Cyclooxygenases inhibition, anti-inflammatory studies and insight on metabolism
Published in European journal of medicinal chemistry (03-03-2014)“…Nimesulide, a COX-2 preferential inhibitor with a favorable gastric and cardiovascular safety profile, was responsible for some cases of acute liver failure…”
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Pyridine Analogues of Nimesulide: Design, Synthesis, and in Vitro and in Vivo Pharmacological Evaluation as Promising Cyclooxygenase 1 and 2 Inhibitors
Published in Journal of medicinal chemistry (08-10-2009)“…Nonsteroidal anti-inflammatory drugs (NSAIDs) represent one of the most prescribed medications, although the chronic use of such pharmacological agents is…”
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10
Activation of the thromboxane A2 pathway in human prostate cancer correlates with tumor Gleason score and pathologic stage
Published in European urology (01-11-2006)“…We investigated the potential involvement of the thromboxane A(2) (TXA(2)) pathway in human prostate cancer (PCa). Expression of cyclooxygenase-2 (COX-2),…”
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Structure-based pharmacophore of COX-2 selective inhibitors and identification of original lead compounds from 3D database searching method
Published in European journal of medicinal chemistry (01-12-2006)“…A four-point pharmacophore of COX-2 selective inhibitors was derived from a training set of 16 compounds, using the Catalyst program. It consists of a H bond…”
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New developments on thromboxane and prostacyclin modulators part II: prostacyclin modulators
Published in Current medicinal chemistry (01-05-2004)“…Prostacyclin (PGI(2)) is a potent endogenous inhibitor of platelet function and possesses a strong vasodilator effect. Furthermore, prostacyclin is currently…”
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13
Increased Expression of Bone Sialoprotein in Bone Metastases Compared with Visceral Metastases in Human Breast and Prostate Cancers
Published in Journal of bone and mineral research (01-05-2000)“…The recent demonstration that bone sialoprotein (BSP) is expressed in osteotropic cancers suggests that this bone matrix protein might be implicated in the…”
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14
New developments on thromboxane and prostacyclin modulators part I: thromboxane modulators
Published in Current medicinal chemistry (01-05-2004)“…The pathogenesis of numerous cardiovascular, pulmonary, inflammatory, and thromboembolic diseases can be related to arachidonic acid (AA) metabolites. One of…”
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15
From the design to the clinical application of thromboxane modulators
Published in Current pharmaceutical design (01-03-2006)“…Arachidonic acid (AA) metabolites are key mediators involved in the pathogenesis of numerous cardiovascular, pulmonary, inflammatory, and thromboembolic…”
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16
Pharmacological characterization of N-tert-butyl-N'-[2-(4'-methylphenylamino)-5-nitrobenzenesulfonyl]urea (BM-573), a novel thromboxane A2 receptor antagonist and thromboxane synthase inhibitor in a rat model of arterial thrombosis and its effects on bleeding time
Published in The Journal of pharmacology and experimental therapeutics (01-05-2004)“…The present study was undertaken to characterize the antiplatelet and antithrombotic effects of BM-573…”
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A new potential cyclooxygenase-2 inhibitor, pyridinic analogue of nimesulide
Published in European journal of medicinal chemistry (01-12-2005)“…In this paper, the binding mode of original pyridinic compounds structurally related to nimesulide, a preferential cyclooxygenase (COX)-2 inhibitor, is…”
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18
Synthesis, molecular modelling and enzymatic evaluation of (±)3,5-diphenyl-2-thioxoimidazolidin-4-ones as new potential cyclooxygenase inhibitors
Published in Bioorganic & medicinal chemistry (15-02-2006)“…Substituted (±)2-thioxoimidazolin-4-ones were synthesized in order to design new type-2 cyclooxygenase (COX-2) inhibitors. Some of them completely inhibit…”
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19
Effects of COX-2 inhibitors on ROS produced by Chlamydia pneumoniae-primed human promonocytic cells (THP-1)
Published in Biochemical and biophysical research communications (24-12-2004)“…Chronic inflammation through foam cells and macrophages is important in atherosclerosis development, and can be considered as therapeutic targets…”
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Spectral and Crystallographic Study of Pyridinic Analogues of Nimesulide: Determination of the Active Form of Methanesulfonamides as COX-2 Selective Inhibitors
Published in Journal of medicinal chemistry (07-11-2002)“…Compound 7, N-(3-phenoxy-4-pyridinyl)trifluoromethanesulfonamide, showed in vitro (whole blood assay) a strong inhibitory activity on the two cyclooxygenase…”
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