Discovery of 2-[[2-Ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)thiazole-5 …

…, D Annoot, N Triballeau, A Monjardet, E Wakselman… - 2017 - ACS Publications
Autotaxin is a circulating enzyme with a major role in the production of lysophosphatic acid (LPA)
species in blood. A role for the autotaxin/LPA axis has been suggested in many …

Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic

…, N Vandeghinste, E Wakselman… - Journal of medicinal …, 2014 - ACS Publications
FFA2, also called GPR43, is a G-protein coupled receptor for short chain fatty acids which is
involved in the mediation of inflammatory responses. A class of azetidines was developed …

Discovery of 9-Cyclopropylethynyl-2-((S)-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one (GLPG1205), a Unique GPR84 Negative Allosteric …

…, E van der Aar, E Wakselman… - Journal of Medicinal …, 2020 - ACS Publications
GPR84 is a medium chain free fatty acid-binding G-protein-coupled receptor associated
with inflammatory and fibrotic diseases. As the only reported antagonist of GPR84 (PBI-4050) …

Discovery, Structure–Activity Relationship, and Binding Mode of an Imidazo[1,2-a]pyridine Series of Autotaxin Inhibitors

…, G Pilzak, A Monjardet, E Wakselman… - Journal of Medicinal …, 2017 - ACS Publications
Autotaxin (ATX) is a secreted enzyme playing a major role in the production of lysophosphatidic
acid (LPA) in blood through hydrolysis of lysophosphatidyl choline (LPC). The ATX–LPA …

Discovery and optimization of orally bioavailable phthalazone and cinnolone carboxylic acid derivatives as S1P2 antagonists against fibrotic diseases

…, L Oste, M Borgonovi, E Wakselman… - Journal of Medicinal …, 2021 - ACS Publications
Idiopathic pulmonary fibrosis (IPF) is a chronic and progressive lung disease. Current
treatments only slow down disease progression, making new therapeutic strategies compelling. …

Discovery of the S1P2 antagonist GLPG2938 (1-[2-Ethoxy-6-(trifluoromethyl)-4-pyridyl]-3-[[5-methyl-6-[1-methyl-3-(trifluoromethyl) pyrazol-4-yl] pyridazin-3-yl] methyl] …

…, L Oste, M Borgonovi, E Wakselman… - Journal of Medicinal …, 2021 - ACS Publications
Mounting evidence from the literature suggests that blocking S1P2 receptor (S1PR2) signaling
could be effective for the treatment of idiopathic pulmonary fibrosis (IPF). However, only a …

Pharmacological profile and efficacy of GLPG1690, a novel autotaxin inhibitor for the treatment of idiopathic pulmonary fibrosis

…, C Cottereaux, A Monjardet, E Wakselman… - … AND TARGETS IN …, 2016 - atsjournals.org
Autotaxin (ATX), a secreted lysophospholipase, plays a central role in the production of the
bioactive lipid lysophosphatidic acid (LPA). LPA signals through multiple LPA receptors to …

Pharmacological profile and efficacy of GLPG1690, a novel ATX inhibitor for COPD treatment

…, S Dupont, C Cottereaux, A Monjardet, E Wakselman… - 2015 - Eur Respiratory Soc
Introduction: Autotaxin (ATX), a secreted lysophospholipase, plays a central role in the
production of the bioactive lipid lysophosphatidic acid (LPA). LPA signals through multiple LPA …

Correction to Discovery, Structure–Activity Relationship, and Binding Mode of an Imidazo[1,2-a]pyridine Series of Autotaxin Inhibitors

…, G Pilzak, A Monjardet, E Wakselman… - Journal of Medicinal …, 2018 - ACS Publications
… Agnès Joncour, Nicolas Desroy,* Christopher Housseman, Xavier Bock, Natacha
Bienvenu, Laëtitia Cherel, Virginie Labeguere, Christophe Peixoto, Denis Annoot, Luce …

Estudo do efeito do inibidor da enzima adenosina desaminase, EHNA, sobre a enterite induzida pela toxina a do Clostridium difficile em alça ileal isolada de …

AFTA Junqueira - 2008 - repositorio.ufc.br
O Clostridium difficile tem como principal fator de virulência a toxina A (TxA), a qual provoca
inflamação e destruição tecidual aguda em intestinos de animais experimentais e de …