Publications by authors named "Raphael Frederick"

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Unveiling the enzymatic activity of a dimeric LDH isoform and its implications for allosteric inhibition strategies.
Ferran Nadal-Bufi, Mégane Van Gysel, Chiara Brustenga, Perrine Savoyen, Caroline Mathieu

Protein Sci· December 2025

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Synthesis and in vitro evaluation of polyethylene glycol-treprostinil conjugates for sustained local delivery in pulmonary arterial hypertension.
Giuditta Leone, Bernard Ucakar, Frédéric Perros, Raphaël Frédérick, Rita Vanbever

Eur J Pharm Sci· November 2025

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Discovery of Potent Acyl-CoA Synthetase Long-Chain Family Member 4 (ACSL4) Inhibitors with Antiferroptotic Properties.
Emeline Charnelle, Alexandre Gobert, Romain Marteau, Maëla Pautric, Nicolas Renault

J Med Chem· August 2025

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LIBX-A401: A Novel Selective Inhibitor of Acyl-CoA Synthetase Long Chain Family Member 4 (ACSL4) and Its Binding Mode.
Darius Mazhari Dorooee, Séverine Ravez, Didier Vertommen, Nicolas Renault, Nicolas Papadopoulos

Angew Chem Int Ed Engl· May 2025

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Structural insights into the interaction between testis-specific Y-encoded-like protein 5 and ubiquitin-specific protease 7.
Marine Ancia, Khadija Wahni, Joudy Chakrowf, Asia El Aakchioui, Eloïse Claude

Protein Sci· May 2025

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Examining Arginase-1 Trimerization Uncovers a Promising Allosteric Site for Inhibition.
Juhans Dechenne, Magdalena Wierzbicka, Reda Krimou, Asia El Aakchioui, Julia Malo Pueyo

J Med Chem· January 2025

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Structural Insights into Protein-Inhibitor Interactions in Human Tryptophan Dioxygenase.
Zachary Geeraerts, Izumi Ishigami, Ariel Lewis-Ballester, Khoa N Pham, Arina Kozlova

J Med Chem· August 2024

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A novel approach to pH-Responsive targeted cancer Therapy: Inhibition of FaDu cancer cell proliferation with a pH low insertion Peptide-Conjugated DGAT1 inhibitor.
Marine Deskeuvre, Junjie Lan, Joris Messens, Olivier Riant, Olivier Feron

Int J Pharm· May 2024

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Enhancing Tsuji-Trost deallylation in living cells with an internal-nucleophile coumarin-based probe.
Yonghua Tan, François Pierrard, Raphaël Frédérick, Olivier Riant

RSC Adv· February 2024

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Tryptophan depletion sensitizes the AHR pathway by increasing AHR expression and GCN2/LAT1-mediated kynurenine uptake, and potentiates induction of regulatory T lymphocytes.
Marie Solvay, Pauline Holfelder, Simon Klaessens, Luc Pilotte, Vincent Stroobant

J Immunother Cancer· June 2023

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Repositioning of FDA-Approved antifungal agents to interrogate Acyl-CoA synthetase long chain family member 4 (ACSL4) in ferroptosis.
Romain Marteau, Séverine Ravez, Darius Mazhari Dorooee, Hind Bouchaoui, Karine Porte

Biochem Pharmacol· October 2022

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Targeting cancer cells in acidosis with conjugates between the carnitine palmitoyltransferase 1 inhibitor etomoxir and pH (low) insertion peptides.
Marine Deskeuvre, Junjie Lan, Emeline Dierge, Joris Messens, Olivier Riant

Int J Pharm· August 2022

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Needle-free iontophoresis-driven β-adrenergic sweat rate test.
Audrey Reynaerts, François Vermeulen, Angélique Mottais, Sophie Gohy, Patrick Lebecque

J Cyst Fibros· May 2022

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Structural study of bioisosteric derivatives of 5-(1-indol-3-yl)-benzotriazole and their ability to form chalcogen bonds.
Manon Mirgaux, Tanguy Scaillet, Arina Kozlova, Nikolay Tumanov, Raphaël Frederick

Acta Crystallogr E Crystallogr Commun· April 2022

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Impact of PEGylation on an antibody-loaded nanoparticle-based drug delivery system for the treatment of inflammatory bowel disease.
Neha Shrestha, Yining Xu, Julien R C Prévost, Fiona McCartney, David Brayden

Acta Biomater· March 2022

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Discovery of small molecules interacting at lactate dehydrogenases tetrameric interface using a biophysical screening cascade.
Léopold Thabault, Chiara Brustenga, Perrine Savoyen, Mégane Van Gysel, Johan Wouters

Eur J Med Chem· February 2022

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Investigation of chalcogen bioisosteric replacement in a series of heterocyclic inhibitors of tryptophan 2,3-dioxygenase.
Arina Kozlova, Léopold Thabault, Nicolas Dauguet, Marine Deskeuvre, Vincent Stroobant

Eur J Med Chem· January 2022

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Olaparib Is a Mitochondrial Complex I Inhibitor That Kills Temozolomide-Resistant Human Glioblastoma Cells.
Luca X Zampieri, Martina Sboarina, Andrea Cacace, Debora Grasso, Léopold Thabault

Int J Mol Sci· November 2021

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Correction to "Rational Design of Original Fused-Cycle Selective Inhibitors of Tryptophan 2,3-Dioxygenase".
Arina Kozlova, Léopold Thabault, Maxime Liberelle, Simon Klaessens, Julien R C Prévost

J Med Chem· September 2021

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Discovery of a novel lactate dehydrogenase tetramerization domain using epitope mapping and peptides.
Léopold Thabault, Maxime Liberelle, Katarina Koruza, Esra Yildiz, Nicolas Joudiou

J Biol Chem· August 2021

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The metalloprotein YhcH is an anomerase providing N-acetylneuraminate aldolase with the open form of its substrate.
Takfarinas Kentache, Leopold Thabault, Gladys Deumer, Vincent Haufroid, Raphaël Frédérick

J Biol Chem· August 2021

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Rational Design of Original Fused-Cycle Selective Inhibitors of Tryptophan 2,3-Dioxygenase.
Arina Kozlova, Léopold Thabault, Maxime Liberelle, Simon Klaessens, Julien R C Prévost

J Med Chem· August 2021

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Phosphoglycerate dehydrogenase (PHGDH) inhibitors: a comprehensive review 2015-2020.
Quentin Spillier, Raphaël Frédérick

Expert Opin Ther Pat· July 2021

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Targeting protein self-association in drug design.
Léopold Thabault, Maxime Liberelle, Raphaël Frédérick

Drug Discov Today· May 2021

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Unravelling the Allosteric Targeting of PHGDH at the ACT-Binding Domain with a Photoactivatable Diazirine Probe and Mass Spectrometry Experiments.
Quentin Spillier, Séverine Ravez, Simon Dochain, Didier Vertommen, Léopold Thabault

Molecules· January 2021

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