Search Results - "Blanque, Roland"
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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-carbonitrile (GLPG1690), a First-in-Class Autotaxin Inhibitor Undergoing Clinical Evaluation for the Treatment of Idiopathic Pulmonary Fibrosis
Published in Journal of medicinal chemistry (11-05-2017)“…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…”
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Population Pharmacokinetic and Pharmacodynamic Analysis of GLPG1690, an Autotaxin Inhibitor, in Healthy Volunteers and Patients with Idiopathic Pulmonary Fibrosis
Published in Clinical pharmacokinetics (01-09-2019)“…Background and Objectives GLPG1690 is an autotaxin inhibitor in development for the treatment of idiopathic pulmonary fibrosis. Several publications suggested…”
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Targeting of αv -Integrins in Stem/Progenitor Cells and Supportive Microenvironment Impairs Bone Metastasis in Human Prostate Cancer
Published in Neoplasia (New York, N.Y.) (01-06-2011)“…Abstract Acquisition of an invasive phenotype by cancer cells is a requirement for bone metastasis. Transformed epithelial cells can switch to a motile,…”
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Characterization of GLPG0492, a selective androgen receptor modulator, in a mouse model of hindlimb immobilization
Published in BMC musculoskeletal disorders (03-09-2014)“…Muscle wasting is a hallmark of many chronic conditions but also of aging and results in a progressive functional decline leading ultimately to disability…”
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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 Modulator Undergoing Evaluation in a Phase II Clinical Trial
Published in Journal of medicinal chemistry (25-11-2020)“…GPR84 is a medium chain free fatty acid-binding G-protein-coupled receptor associated with inflammatory and fibrotic diseases. As the only reported antagonist…”
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Discovery and Optimization of an Azetidine Chemical Series As a Free Fatty Acid Receptor 2 (FFA2) Antagonist: From Hit to Clinic
Published in Journal of medicinal chemistry (11-12-2014)“…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…”
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Identification of a 4‑(Hydroxymethyl)diarylhydantoin as a Selective Androgen Receptor Modulator
Published in Journal of medicinal chemistry (11-10-2012)“…Structural modification performed on a 4-methyl-4-(4-hydroxyphenyl)hydantoin series is described which resulted in the development of a new series of…”
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Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS‑5 Inhibitor for the Treatment of Osteoarthritis
Published in Journal of medicinal chemistry (25-03-2021)“…There are currently no approved disease-modifying osteoarthritis (OA) drugs (DMOADs). The aggrecanase ADAMTS-5 is key in the degradation of human aggrecan…”
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Discovery of GLPG3667, a Selective ATP Competitive Tyrosine Kinase 2 Inhibitor for the Treatment of Autoimmune Diseases
Published in Journal of medicinal chemistry (13-06-2024)“…Tyrosine kinase 2 (TYK2) mediates cytokine signaling through type 1 interferon, interleukin (IL)-12/IL-23, and the IL-10 family. There appears to be an…”
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Targeting of α(v)-integrins in stem/progenitor cells and supportive microenvironment impairs bone metastasis in human prostate cancer
Published in Neoplasia (New York, N.Y.) (01-06-2011)“…Acquisition of an invasive phenotype by cancer cells is a requirement for bone metastasis. Transformed epithelial cells can switch to a motile, mesenchymal…”
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11
A TNF receptor loop peptide mimic blocks RANK ligand-induced signaling, bone resorption, and bone loss
Published in The Journal of clinical investigation (01-06-2006)“…Activating receptor activator of NF-kappaB (RANK) and TNF receptor (TNFR) promote osteoclast differentiation. A critical ligand contact site on the TNFR is…”
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Targeting of αv-Integrins in Stem/Progenitor Cells and Supportive Microenvironment Impairs Bone Metastasis in Human Prostate Cancer12
Published in Neoplasia (New York, N.Y.) (01-06-2011)“…Acquisition of an invasive phenotype by cancer cells is a requirement for bone metastasis. Transformed epithelial cells can switch to a motile, mesenchymal…”
Get full text
Journal Article -
13
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-carbonitrile (GLPG1690), a First-in-Class Autotaxin Inhibitor Undergoing Clinical Evaluation for the Treatment of Idiopathic Pulmonary Fibrosis
Published in Journal of medicinal chemistry (11-05-2017)“…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…”
Get full text
Journal Article -
14
FACTORS INFLUENCING THE EFFECT OF THE SOLUBLE IL-6 RECEPTOR ON IL-6 RESPONSES IN HepG2 HEPATOCYTES
Published in Cytokine (Philadelphia, Pa.) (01-06-2000)“…The soluble IL-6 receptor (sIL-6R) can increase IL-6-induced signalling by forming a complex with IL-6 and membrane-bound gp130 (the receptor beta chain which…”
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