Publications by authors named "Reginald Brys"

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Discovery of GLPG4471, a potent and selective IRAK4 inhibitor for the treatment of inflammatory and autoimmune diseases.
Oscar Mammoliti, Florence Bonnaterre, Gregory Newsome, Rhalid Akkari, Miriam López-Ramos, Reginald Brys

Bioorg Med Chem Lett· December 2025

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Structure activity relationship exploration of imidazo[1,2-a]pyridine series to reverse isoform selectivity and identify potent SIK1 selective inhibitors.
Christophe Peixoto, Elsa De Lemos, Laëtitia Cherel, Gregory Newsome, Aurelie Dos Santos, Reginald Brys

Bioorg Med Chem Lett· December 2025

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Structure-Activity Relationship Guided Scaffold Hopping Resulted in the Identification of GLPG4970, a Highly Potent Dual SIK2/SIK3 Inhibitor.
Hans Kelgtermans, Maxim De Wachter, Stijn Heyndrickx, Sandy El Bkassiny, Tatiana Lacarriere, Reginald Brys

J Med Chem· August 2025

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Design of a potent and selective dual JAK1/TYK2 inhibitor.
Oscar Mammoliti, Christel Menet, Céline Cottereaux, Javier Blanc, Ann De Blieck, Reginald Brys

Bioorg Med Chem· November 2024

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Discovery of GLPG3667, a Selective ATP Competitive Tyrosine Kinase 2 Inhibitor for the Treatment of Autoimmune Diseases.
Oscar Mammoliti, Sébastien Martina, Pieter Claes, Ghjuvanni Coti, Roland Blanque, Reginald Brys

J Med Chem· June 2024

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Discovery of Clinical Candidate GLPG3970: A Potent and Selective Dual SIK2/SIK3 Inhibitor for the Treatment of Autoimmune and Inflammatory Diseases.
Christophe Peixoto, Agnes Joncour, Taouès Temal-Laib, Amynata Tirera, Aurélie Dos Santos, Reginald Brys

J Med Chem· April 2024

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Optimization of Selectivity and Pharmacokinetic Properties of Salt-Inducible Kinase Inhibitors that Led to the Discovery of Pan-SIK Inhibitor GLPG3312.
Taouès Temal-Laib, Christophe Peixoto, Nicolas Desroy, Elsa De Lemos, Florence Bonnaterre, Reginald Brys

J Med Chem· January 2024

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IRAK4 inhibition dampens pathogenic processes driving inflammatory skin diseases.
Stéphanie Lavazais, Manja Jargosch, Sonia Dupont, Frédéric Labéguère, Christel Menet, Reginald Brys

Sci Transl Med· February 2023

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Discovery and Optimization of Orally Bioavailable Phthalazone and Cinnolone Carboxylic Acid Derivatives as S1P2 Antagonists against Fibrotic Diseases.
Oscar Mammoliti, Koen Jansen, Sandy El Bkassiny, Adeline Palisse, Nicolas Triballeau, Reginald Brys

J Med Chem· October 2021

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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]urea), a Preclinical Candidate for the Treatment of Idiopathic Pulmonary Fibrosis.
Oscar Mammoliti, Adeline Palisse, Caroline Joannesse, Sandy El Bkassiny, Brigitte Allart, Reginald Brys

J Med Chem· May 2021

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Discovery and development of ASK1 inhibitors.
Reginald Brys, Karl Gibson, Tanja Poljak, Steven Van Der Plas, David Amantini

Prog Med Chem· November 2020

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Discovery of 9-Cyclopropylethynyl-2-(()-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1-]isoquinolin-4-one (GLPG1205), a Unique GPR84 Negative Allosteric Modulator Undergoing Evaluation in a Phase II Clinical Trial.
Frédéric Labéguère, Sonia Dupont, Luke Alvey, Florilène Soulas, Gregory Newsome, Reginald Brys

J Med Chem· November 2020

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The Medium-Chain Fatty Acid Receptor GPR84 Mediates Myeloid Cell Infiltration Promoting Steatohepatitis and Fibrosis.
Tobias Puengel, Steve De Vos, Jana Hundertmark, Marlene Kohlhepp, Nurdan Guldiken, Reginald Brys

J Clin Med· April 2020

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Neutralization of IL-17C Reduces Skin Inflammation in Mouse Models of Psoriasis and Atopic Dermatitis.
Nick Vandeghinste, Jürgen Klattig, Catherine Jagerschmidt, Stéphanie Lavazais, Florence Marsais, Reginald Brys

J Invest Dermatol· July 2018

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Correction to Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2- a]pyridine Series of Autotaxin Inhibitors.
Agnès Joncour, Nicolas Desroy, Christopher Housseman, Xavier Bock, Natacha Bienvenu, Reginald Brys

J Med Chem· May 2018

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Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2-a]pyridine Series of Autotaxin Inhibitors.
Agnès Joncour, Nicolas Desroy, Christopher Housseman, Xavier Bock, Natacha Bienvenu, Reginald Brys

J Med Chem· September 2017

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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.
Nicolas Desroy, Christopher Housseman, Xavier Bock, Agnès Joncour, Natacha Bienvenu, Reginald Brys

J Med Chem· May 2017

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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.
Mathieu Pizzonero, Sonia Dupont, Marielle Babel, Stéphane Beaumont, Natacha Bienvenu, Reginald Brys

J Med Chem· December 2014

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Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.
Christel J Menet, Stephen R Fletcher, Guy Van Lommen, Raphael Geney, Javier Blanc, Reginald Brys

J Med Chem· November 2014

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Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases.
Luc Van Rompaey, René Galien, Ellen M van der Aar, Philippe Clement-Lacroix, Luc Nelles, Reginald Brys

J Immunol· October 2013

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Discovery of a series of imidazopyrazine small molecule inhibitors of the kinase MAPKAPK5, that show activity using in vitro and in vivo models of rheumatoid arthritis.
Martin J I Andrews, J Andrew Clase, Gregory Bar, Giovanni Tricarico, Paul J Edwards, Reginald Brys

Bioorg Med Chem Lett· March 2012

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A multiparameter approach to monitor disease activity in collagen-induced arthritis.
Sylvie Seeuws, Peggy Jacques, Jens Van Praet, Michael Drennan, Julie Coudenys, Reginald Brys

Arthritis Res Ther· January 2011

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The alpha7 nicotinic acetylcholine receptor on fibroblast-like synoviocytes and in synovial tissue from rheumatoid arthritis patients: a possible role for a key neurotransmitter in synovial inflammation.
Marjolein A van Maanen, Susanne P Stoof, Esmerij P van der Zanden, Wouter J de Jonge, Richard A Janssen, Reginald Brys

Arthritis Rheum· May 2009

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Adenoviral vectors expressing siRNAs for discovery and validation of gene function.
Gert-Jan Arts, Ellen Langemeijer, Rudi Tissingh, Libin Ma, Heidi Pavliska, Reginald Brys

Genome Res· October 2003

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Arrayed adenoviral expression libraries for functional screening.
Frits Michiels, Helmuth van Es, Luc van Rompaey, Pascal Merchiers, Bart Francken, Reginald Brys

Nat Biotechnol· November 2002

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