Search Results - "CHAVATTE, Philippe"
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1
Therapeutic Potential of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and N‑Acylethanolamine Acid Amidase Inhibitors
Published in Journal of medicinal chemistry (12-01-2017)“…Fatty acid ethanolamides (FAEs) and endocannabinoids (ECs) have been shown to alleviate pain and inflammation, regulate motility and appetite, and produce…”
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2
GED-0507 attenuates lung fibrosis by counteracting myofibroblast transdifferentiation in vivo and in vitro
Published in PloS one (16-09-2021)“…The development of more effective, better tolerated drug treatments for progressive pulmonary fibrosis (of which idiopathic pulmonary fibrosis is the most…”
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3
Targeting Peroxisome Proliferator-Activated Receptors (PPARs): Development of Modulators
Published in Journal of medicinal chemistry (10-05-2012)Get full text
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4
GED-0507 is a novel potential antifibrotic treatment option for pulmonary fibrosis
Published in Cellular & molecular immunology (01-12-2020)Get full text
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5
Synthesis and Structure–Activity Relationships of (Aryloxy)quinazoline Ureas as Novel, Potent, and Selective Vascular Endothelial Growth Factor Receptor-2 Inhibitors
Published in Journal of medicinal chemistry (09-02-2012)“…In our continuing search for medicinal agents to treat proliferative diseases, quinazoline derivatives were synthesized and evaluated pharmacologically as…”
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6
Polycyclic nitrogen heterocycles as potential thymidine phosphorylase inhibitors: synthesis, biological evaluation, and molecular docking study
Published in Journal of enzyme inhibition and medicinal chemistry (01-12-2022)“…New polycyclic heterocycles were synthesised and evaluated as potential inhibitors of thymidine phosphorylase (TP). Inspired by the pharmacophoric…”
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7
Importance of the second extracellular loop for melatonin MT1 receptor function and absence of melatonin binding in GPR50
Published in British journal of pharmacology (01-08-2018)“…Background and Purpose Recent crystal structures of GPCRs have emphasized the previously unappreciated role of the second extracellular (E2) loop in ligand…”
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8
Relationships between Th1 or Th2 iNKT cell activity and structures of CD1d-antigen complexes: meta-analysis of CD1d-glycolipids dynamics simulations
Published in PLoS computational biology (01-11-2014)“…A number of potentially bioactive molecules can be found in nature. In particular, marine organisms are a valuable source of bioactive compounds. The activity…”
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9
Novel structural insights for drug design of selective 5-HT2C inverse agonists from a ligand-biased receptor model
Published in European journal of medicinal chemistry (01-11-2010)Get full text
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10
Three-Dimensional Quantitative Structure−Activity Relationships of Cyclo-oxygenase-2 (COX-2) Inhibitors: A Comparative Molecular Field Analysis
Published in Journal of medicinal chemistry (27-09-2001)“…The three-dimensional quantitative structure−activity relationship (3D-QSAR) approach using comparative molecular field analysis (CoMFA) was applied to an…”
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11
Synthesis and Structure−Affinity−Activity Relationships of Novel Benzofuran Derivatives as MT2 Melatonin Receptor Selective Ligands
Published in Journal of medicinal chemistry (20-06-2002)“…A series of N-(2-phenylbenzofuran-3-yl) ethyl amide and N-(2-arylalkylbenzofuran-3-yl) ethyl amide derivatives were synthesized and evaluated as melatonin…”
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12
2,6-Diphenylthiazolo[3,2- b][1,2,4]triazoles as telomeric G-quadruplex stabilizers
Published in Bioorganic & medicinal chemistry letters (01-07-2009)“…Two of the title compounds ( 14a, 19) bearing cationic side chains present high selectivity for telomeric G-quadruplex over duplex DNA. The design and…”
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13
A computational view of COX-2 inhibition
Published in Anti-cancer agents in medicinal chemistry (01-05-2006)“…Selective inhibition of COX-2 provided a new class of anti-inflammatory, analgesic and antipyretic drugs with significantly reduced side effects and could also…”
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14
Investigations of new lead structures for the design of novel cyclooxygenase-2 inhibitors
Published in European journal of medicinal chemistry (01-06-2002)“…On the basis of molecular modelling studies, five new compounds were synthesised and studied in an attempt to design new lead structures as selective COX-2…”
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15
Docking study of ligands into the colchicine binding site of tubulin
Published in Journal of enzyme inhibition and medicinal chemistry (01-12-2004)“…Cancer is a major cause of mortality in developed countries, following only cardiovascular diseases. Death of cancerous cells can be achieved by stopping…”
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16
2D QSAR Consensus Prediction for High-Throughput Virtual Screening. An Application to COX-2 Inhibition Modeling and Screening of the NCI Database
Published in Journal of Chemical Information and Computer Sciences (01-01-2004)“…Using classification (SOM, LVQ, Binary, Decision Tree) and regression algorithms (PLS, BRANN, k-NN, Linear), this paper details the building of eight 2D-QSAR…”
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17
SINAPs: A Software Tool for Analysis and Visualization of Interaction Networks of Molecular Dynamics Simulations
Published in Journal of chemical information and modeling (28-03-2022)“…As long as the structural study of molecular mechanisms requires multiple molecular dynamics reflecting contrasted bioactive states, the subsequent analysis of…”
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18
Chitin-glucan improves important pathophysiological features of irritable bowel syndrome
Published in World journal of gastroenterology : WJG (28-04-2024)“…Irritable bowel syndrome (IBS) is one of the most frequent and debilitating conditions leading to gastroenterological referrals. However, recommended…”
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Pharmacophoric Search and 3D-QSAR Comparative Molecular Field Analysis Studies on Agonists of Melatonin Sheep Receptors
Published in Journal of medicinal chemistry (05-11-1998)“…Conformational analysis was used to characterize the agonist pharmacophore for melatonin sheep brain receptor recognition and activation. The molecular…”
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20
Design, Synthesis, and Pharmacological Evaluation of New Farnesyl Protein Transferase Inhibitors
Published in Journal of medicinal chemistry (17-01-2002)“…New CA1A2X peptidomimetics are described as Ras farnesyl transferase inhibitors (FTIs). They include cysteine and methionine as mimetics of the C-terminus…”
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