Results 1 to 10 of about 115 (104)

A Potential Off-Target Effect of the Wnt/β-Catenin Inhibitor KYA1797K: PD-L1 Binding and Checkpoint Inhibition [PDF]

Biomedicine Hub, 2023
Introduction: The quest for small molecule inhibitors of the PD-1/PD-L1 checkpoint continues in parallel to the extensive development of monoclonal antibodies directed against this immune checkpoint. Drug screening strategies are being set up to identify
Xavier Thuru, Romain Magnez, Gérard Vergoten, Christian Bailly   +3 more
doaj   +2 more sources

Antioxidant Properties and Aldehyde Reactivity of PD-L1 Targeted Aryl-Pyrazolone Anticancer Agents [PDF]

Molecules, 2022
Small molecules targeting the PD-1/PD-L1 checkpoint are actively searched to complement the anticancer arsenal. Different molecular scaffolds have been reported, including phenyl-pyrazolone derivatives which potently inhibit binding of PD-L1 to PD-1 ...
Natascha Leleu-Chavain, Romain Regnault, Hania Ahouari, Raphaël Le Biannic, Mostafa Kouach, Frédérique Klupsch, Romain Magnez, Hervé Vezin, Xavier Thuru, Christian Bailly, Jean-François Goossens, Régis Millet   +11 more
doaj   +2 more sources

Novel PD-L1-Targeted Phenyl-Pyrazolone Derivatives with Antioxidant Properties [PDF]

Molecules, 2023
Orally-active anticancer small molecules targeting the PD-1/PD-L1 immune checkpoint are actively searched. Phenyl-pyrazolone derivatives with a high affinity for PD-L1 have been designed and characterized.
Romain Regnault, Frédérique Klupsch, Hassiba El-Bouazzati, Romain Magnez, Raphaël Le Biannic, Natascha Leleu-Chavain, Hania Ahouari, Hervé Vezin, Régis Millet, Jean-François Goossens, Xavier Thuru, Christian Bailly   +11 more
doaj   +2 more sources

Discovery and characterization of small molecule inhibitors of cystathionine gamma‐synthase with in planta activity [PDF]

Plant Biotechnology Journal, Volume 19, Issue 9, Page 1785-1797, September 2021., 2021
Summary The synthesis of essential amino acids in plants is pivotal for their viability and growth, and these cellular pathways are therefore targeted for the discovery of new molecules for weed control. Herein, we describe the discovery and design of small molecule inhibitors of cystathionine gamma‐synthase, a key enzyme in the biosynthesis of ...
Itai Bloch, Hadar Haviv, Irena Rapoport, Elad Cohen, Rotem Shelly Ben Shushan, Nesly Dotan, Inbal Sher, Yael Hacham, Rachel Amir, Maayan Gal   +9 more
wiley   +2 more sources

Tau Stabilizes Chromatin Compaction [PDF]

Frontiers in Cell and Developmental Biology, 2021
An extensive body of literature suggested a possible role of the microtubule-associated protein Tau in chromatin functions and/or organization in neuronal, non-neuronal, and cancer cells. How Tau functions in these processes remains elusive.
Thomas Rico, Melissa Gilles, Alban Chauderlier, Thomas Comptdaer, Romain Magnez, Maggy Chwastyniak, Herve Drobecq, Florence Pinet, Xavier Thuru, Luc Buée, Marie-Christine Galas, Bruno Lefebvre   +11 more
doaj   +2 more sources

A Phosphosite Mutant Approach on LRRK2 Links Phosphorylation and Dephosphorylation to Protective and Deleterious Markers, Respectively [PDF]

Cells, 2022
The Leucine Rich Repeat Kinase 2 (LRRK2) gene is a major genetic determinant of Parkinson’s disease (PD), encoding a homonymous multi-domain protein with two catalytic activities, GTPase and Kinase, involved in intracellular signaling and trafficking ...
Antoine Marchand, Alessia Sarchione, Panagiotis S. Athanasopoulos, Hélène Bauderlique-Le Roy, Liesel Goveas, Romain Magnez, Matthieu Drouyer, Marco Emanuele, Franz Y. Ho, Maxime Liberelle, Patricia Melnyk, Nicolas Lebègue, Xavier Thuru, R. Jeremy Nichols, Elisa Greggio, Arjan Kortholt, Thierry Galli, Marie-Christine Chartier-Harlin, Jean-Marc Taymans   +18 more
doaj   +2 more sources

Measurement of Protein-Protein Interactions through Microscale Thermophoresis (MST) [PDF]

Bio-Protocol, 2020
The binding interactions of PD-1 and PD-L1 have been studied by surface plasmon resonance (SPR) and isothermal titration calorimetry (ITC) over the past few years, but these investigations resulted in controversy regarding the values of the dissociation ...
Magnez Romain, Bryan Thiroux, Morgane Tardy, Bruno Quesnel, Xavier Thuru   +4 more
doaj   +2 more sources

Direct interaction of TrkA/CD44v3 is essential for NGF-promoted aggressiveness of breast cancer cells [PDF]

Journal of Experimental & Clinical Cancer Research, 2022
Background CD44 is a multifunctional membrane glycoprotein. Through its heparan sulfate chain, CD44 presents growth factors to their receptors. We have shown that CD44 and Tropomyosin kinase A (TrkA) form a complex following nerve growth factor (NGF ...
Sarah Trouvilliez, Julien Cicero, Romain Lévêque, Léo Aubert, Cyril Corbet, Alexandre Van Outryve, Karolin Streule, Pierre-Olivier Angrand, Pamela Völkel, Romain Magnez, Guillaume Brysbaert, Caroline Mysiorek, Fabien Gosselet, Roland Bourette, Eric Adriaenssens, Xavier Thuru, Chann Lagadec, Jérôme de Ruyck, Véronique Orian-Rousseau, Xuefen Le Bourhis, Robert-Alain Toillon   +20 more
doaj   +2 more sources

Safety, Immunogenicity, and Vaccine Compatibility of a Trivalent Inactivated In Ovo Nanovaccine Against Avian Colibacillosis in Broilers Under Commercial Hatchery Conditions [PDF]

Animals
Avian colibacillosis, caused by Escherichia coli, remains a significant threat to poultry health and production, particularly in the context of rising antimicrobial resistance.
Angelo Scuotto, Daniela Ogonczyk-Makowska, Romain Magnez, Bryan Thiroux, Pierre-Louis Herrouin, Thomas Bouillet, Anaïs-Camille Vreulx, Amélie Degraeve, Didier Betbeder   +8 more
doaj   +2 more sources

The impact of magnesium supplementation on the occurrence of selected disease states and physical performance - a review of the literature

Journal of Education, Health and Sport, 2022
Magnez jest jednym z ważnych pierwiastków w ludzkim ciele. Odgrywa niezwykle ważną rolę w ponad 300 reakcjach enzymatycznych. Magnez jest jednym z siedmiu makroelementów.
Katarzyna Cyboran, Monika Kuc, Agnieszka Siedlak, Dominik Machaj, Alicja Płaczek   +4 more
doaj   +1 more source