Publications

LAMBERT Didier

Prevost, J.R.C., Kozlova, A., Es Saadi, B., Yildiz, E., Modaffari, S., Lambert, D.M., Pochet, L., Wouters, J., Dolušić, E., Frédérick, R.
Convenient one-pot formation of highly functionalized 5-bromo-2aminothiazoles, potential endocannabinoid hydrolase MAGL inhibitors.
Tet. Lett. (2018) 59(49), 4315-4319.

El Bakali J., Muccioli GG., Body-Malapel M., Djouina M., Klupsch F., Ghinet A., Barczyk A., Renault N., Chavatte P., Desreumaux P., Lambert D.M., Millet R.
Conformational Restriction Leading to a Selective CB2 Cannabinoid Receptor Agonist Orally Active Against Colitis.
ACS Med. Chem. Lett. (2014), 6(2):198-203.

Kapanda C.N., Masquelier J., Labar G., Muccioli G.G., Poupaert J.H., Lambert D.M.
Synthesis anpharmacological evaluation of 2,4-dinitroaryldithiocarbamate derivatives as novel monoacylglycerol lipase inhibitors.
J. Med. Chem. (2012), 55: 5774-5783.

Labar G., Bauvois C., Borel F., Ferrer J.L., Wouters J., Lambert D.M.
Crystal structure of the human monoacylglycerol lipase, a key actor in endocannabinoid signaling.
Chembiochem (2010), 11:218-27.

Kapanda C.N., Muccioli G.G., Labar G., Poupaert J.H., Lambert D.M.
Bis (dialkylaminethiocarbonyl) disulfides as potent and selective monoglyceride lipase inhibitors.
J Med Chem. (2009), 52:7310-4.

Matuszak N., Muccioli G.G., Labar G., Lambert D.M.
Synthesis and in vitro evaluation of N-substituted maleimide derivatives as selective monoglyceride lipase inhibitors.
J Med Chem. (2009), 52:7410-20.

FREDERICK Raphaël

Marteau, Romain ; Ravez, Séverine (co-first author) ; Mazhari Dorooee, Darius ; Bouchaoui, Hind ; Porte, Karine ; Devedjian, Jean-Christophe ; Melnyk, Patricia ; Devos, David ; Frédérick, Raphaël ; El Bakali, Jamal.
Repositioning of FDA-Approved antifungal agents to interrogate Acyl-CoA synthetase long chain family member 4 (ACSL4) in ferroptosis.
Biochemical Pharmacology, Vol. 204, no.-, p. 115239 (2022).

Deskeuvre, Marine ; Lan, Junjie ; Dierge, Emeline ; Messens, Joris ; Riant, Olivier ; Corbet, Cyril ; Feron, Olivier ; Frédérick, Raphaël.
Targeting cancer cells in acidosis with conjugates between the carnitine palmitoyltransferase 1 inhibitor etomoxir and pH (low) insertion peptides.
International Journal of Pharmaceutics, Vol. 624, no.1, p. 122041 (2022).

Thabault, Léopold ; Brustenga, Chiara ; Savoyen, Perrine ; Van Gysel, Mégane ; Wouters, Johan ; Sonveaux, Pierre ; Frédérick, Raphaël ; Liberelle, Maxime.
Discovery of small molecules interacting at lactate dehydrogenases tetrameric interface using a biophysical screening cascade.
European Journal of Medicinal Chemistry, Vol. 230, p. 114102 (2022).

Kozlova, A.; Thabault, L.; Dauguet, N.; Deskeuvre, M.; Stroobant, V.; Pilotte, L.; Liberelle, M.; Van den Eynde, B.; Frédérick, R.
Investigation of chalcogen bioisosteric replacement in a series of heterocyclic inhibitors of tryptophan 2,3-dioxygenase.
Eur J Med Chem (2021), 227, 113892.

Thabault L, Brisson L, Brustenga C, Martinez Gache SA, Prévost JRC, Kozlova A, Spillier Q, Liberelle M, Benyahia Z, Messens J, Copetti T, Sonveaux P, Frédérick R.
Interrogating the Lactate Dehydrogenase Tetramerization Site Using (Stapled)
Peptides. (2020) J Med Chem 63(9):4628-4643.

Raphael Frédérick

2025
- Article de journal
  
  Dechenne, Juhans ; Wierzbicka, Magdalena ; Krimou, Reda ; El Aakchioui, Asia ; Malo Pueyo, Julia ; Messens, Joris ; Fillet, Marianne ; Spillier, Quentin ; Frédérick, Raphaël.
  
  Examining Arginase-1 Trimerization Uncovers a Promising Allosteric Site for Inhibition. In: Journal of Medicinal Chemistry. doi:10.1021/acs.jmedchem.4c01993.
  
  http://hdl.handle.net/2078.1/299208
- Mazhari Dorooee, Darius ; Ravez, Séverine ; Vertommen, Didier ; Renault, Nicolas ; Papadopoulos, Nicolas ; Marteau, Romain ; Charnelle, Emeline ; Porte, Karine ; Gobert, Alexandre ; Hennuyer, Nathalie ; Herinckx, Gaëtan ; Pautric, Maëla ; Jonneaux, Aurélie ; Devedjian, Jean-Christophe ; Devos, David ; Staels, Bart ; Melnyk, Patricia ; Constantinescu, Stefan N. ; Frédérick, Raphaël ; El Bakali, Jamal.
  
  LIBX-A401: A Novel Selective Inhibitor of Acyl-CoA Synthetase Long Chain Family Member 4 (ACSL4) and Its Binding Mode. In: Angewandte Chemie (International Edition), (2025). doi:10.26434/chemrxiv-2024-pd863 (Accepté/Sous presse).
  
  http://hdl.handle.net/2078.1/299348
2024
- Article de journal
  
  Deskeuvre, Marine ; Lan, Junjie ; Messens, Joris ; Riant, Olivier ; Feron, Olivier ; Frédérick, Raphaël.
  
  A novel approach to pH-Responsive targeted cancer Therapy: Inhibition of FaDu cancer cell proliferation with a pH low insertion Peptide-Conjugated DGAT1 inhibitor. In: International Journal of Pharmaceutics, Vol. 657, p. 124132 (2024). doi:10.1016/j.ijpharm.2024.124132.
  
  http://hdl.handle.net/2078.1/289133
- Tan, Yonghua ; Pierrard, François ; Frédérick, Raphaël ; Riant, Olivier.
  
  Enhancing Tsuji–Trost deallylation in living cells with an internal-nucleophile coumarin-based probe. In: RSC Advances, Vol. 14, no.8, p. 5492-5498 (2024). doi:10.1039/d3ra08938j.
  
  http://hdl.handle.net/2078.1/286977
- Geeraerts, Zachary ; Ishigami, Izumi ; Lewis-Ballester, Ariel ; Pham, Khoa N. ; Kozlova, Arina ; Mathieu, Caroline ; Frédérick, Raphaël ; Yeh, Syun-Ru.
  
  Structural Insights into Protein-Inhibitor Interactions in Human Tryptophan Dioxygenase. In: Journal of Medicinal Chemistry, Vol. 67, no. 16, p. 14543 - 14552 (2024). doi:10.1021/acs.jmedchem.4c01360.
  
  http://hdl.handle.net/2078.1/299263
2023
- Article de journal
  
  Tan, Yonghua ; Lefevre, Marine ; Pierrard, François ; Soetens, Mathieu ; Shoueiry, Maria ; Yildiz, Esra ; Ibanez, Sébastien ; Özkan, Kübra ; Feron, Olivier ; Frédérick, Raphaël ; Riant, Olivier.
  
  Tandem Heck/Tsuji-Trost Reaction for Uncaging of Alloc-Protected Amines with Palladium Complexes in Living Cells. In: Journal of organometallic chemistry, Vol. 996, p. 122743 [1-9] (2023). doi:10.1016/j.jorganchem.2023.122743.
  
  http://hdl.handle.net/2078.1/275937
- Solvay, Marie ; Holfelder, Pauline (co-first author) ; Klaessens, Simon ; Pilotte, Luc ; Stroobant, Vincent ; Lamy, Juliette ; Naulaerts, Stefan ; Spillier, Quentin ; Frédérick, Raphaël ; De Plaen, Etienne ; Sers, Christine ; Opitz, Christiane A ; Van den Eynde, Benoit ; Zhu, Jingjing.
  
  Tryptophan depletion sensitizes the AHR pathway by increasing AHR expression and GCN2/LAT1-mediated kynurenine uptake, and potentiates induction of regulatory T lymphocytes. In: Journal for immunotherapy of cancer, Vol. 11, no. 6, p. e006728 [1-15] (2023). doi:10.1136/jitc-2023-006728.
  
  http://hdl.handle.net/2078.1/275939
2022
- Article de journal
  
  Thabault, Léopold ; Brustenga, Chiara ; Savoyen, Perrine ; Van Gysel, Mégane ; Wouters, Johan ; Sonveaux, Pierre ; Frédérick, Raphaël ; Liberelle, Maxime.
  
  Discovery of small molecules interacting at lactate dehydrogenases tetrameric interface using a biophysical screening cascade.. In: European journal of medicinal chemistry, Vol. 230, p. 114102 [1-10] (2022). doi:10.1016/j.ejmech.2022.114102.
  
  http://hdl.handle.net/2078/258221
- Shrestha, Neha ; Xu, Yining ; Prévost, Julien R C ; McCartney, Fiona ; Brayden, David ; Frédérick, Raphaël ; Beloqui Garcia, Ana ; Préat, Véronique.
  
  Impact of PEGylation on an antibody-loaded nanoparticle-based drug delivery system for the treatment of inflammatory bowel disease.. In: Acta biomaterialia, Vol. 140, p. 561-572 (2022). doi:10.1016/j.actbio.2021.12.015.
  
  http://hdl.handle.net/2078.1/261328
- Kozlova, Arina ; Thabault, Léopold ; Dauguet, Nicolas ; Deskeuvre, Marine ; Stroobant, Vincent ; Pilotte, Luc ; Liberelle, Maxime ; Van den Eynde, Benoit ; Frédérick, Raphaël.
  
  Investigation of chalcogen bioisosteric replacement in a series of heterocyclic inhibitors of tryptophan 2,3-dioxygenase. In: European journal of medicinal chemistry, Vol. 227, p. 113892 [1-12] (2022). doi:10.1016/j.ejmech.2021.113892.
  
  http://hdl.handle.net/2078.1/269055
- Reynaerts, Audrey ; Vermeulen, François ; Mottais, Angélique ; Gohy, Sophie ; Lebecque, Patrick ; Frédérick, Raphaël ; Vanbever, Rita ; Leal, Teresinha.
  
  Needle-free iontophoresis-driven β-adrenergic sweat rate test.. In: Journal of cystic fibrosis, Vol. 21, no. 3, p. 407-415 (2022). doi:10.1016/j.jcf.2021.08.012.
  
  http://hdl.handle.net/2078.1/261968
- Marteau, Romain ; Ravez, Séverine (co-first author) ; Mazhari Dorooee, Darius ; Bouchaoui, Hind ; Porte, Karine ; Devedjian, Jean-Christophe ; Melnyk, Patricia ; Devos, David ; Frédérick, Raphaël ; El Bakali, Jamal.
  
  Repositioning of FDA-Approved antifungal agents to interrogate Acyl-CoA synthetase long chain family member 4 (ACSL4) in ferroptosis. In: Biochemical pharmacology, Vol. 204, p. 115239 [1-12] (2022). doi:10.1016/j.bcp.2022.115239.
  
  http://hdl.handle.net/2078.1/269051
- Mirgaux, Manon ; Scaillet, Tanguy ; Kozlova, Arina ; Tumanov, Nikolay ; Frédérick, Raphaël ; Bodart, Laurie ; Wouters, Johan.
  
  Structural study of bioisosteric derivatives of 5-(1H-indol-3-yl)-benzotriazole and their ability to form chalcogen bonds. In: Acta Crystallographica Section E Crystallographic Communications, Vol. 78, no. 4, p. 418-424 (2022). doi:10.1107/s2056989022002948.
  
  http://hdl.handle.net/2078.1/269053
- Deskeuvre, Marine ; Lan, Junjie ; Dierge, Emeline ; Messens, Joris ; Riant, Olivier ; Corbet, Cyril ; Feron, Olivier ; Frédérick, Raphaël.
  
  Targeting cancer cells in acidosis with conjugates between the carnitine palmitoyltransferase 1 inhibitor etomoxir and pH (low) insertion peptides. In: International Journal of Pharmaceutics, Vol. 624, no.1, p. 122041 (2022). doi:10.1016/j.ijpharm.2022.122041.
  
  http://hdl.handle.net/2078.1/264539
2021
- Article de journal
  
  Thabault, Léopold ; Liberelle, Maxime ; Koruza, Katarina ; Yildiz, Esra ; Joudiou, Nicolas ; Messens, Joris ; Brisson, Lucie ; Wouters, Johan ; Sonveaux, Pierre ; Frédérick, Raphaël.
  
  Discovery of a novel lactate dehydrogenase tetramerization domain using epitope mapping and peptides. In: Journal of Biological Chemistry, Vol. 296, p. 100422 (2021). doi:10.1016/j.jbc.2021.100422.
  
  http://hdl.handle.net/2078/243463
- Zampieri, Luca ; Sboarina, Martina ; Cacace, Andrea ; Grasso, Debora ; Thabault, Léopold ; Hamelin, Loïc ; Vazeille, Thibaut ; Dumon, Elodie ; Rossignol, Rodrigue ; Frédérick, Raphaël ; Sonveaux, Etienne ; Lefranc, Florence ; Sonveaux, Pierre.
  
  Olaparib is a mitochondrial Complex I inhibitor that kills temozolomide-resistant human glioblastoma cells. In: International Journal of Molecular Sciences, Vol. 22, no.11938, p. 17 (2021). doi:10.3390/ijms222111938.
  
  http://hdl.handle.net/2078.1/252707
- Spillier, Quentin ; Frédérick, Raphaël.
  
  Phosphoglycerate dehydrogenase (PHGDH) inhibitors: a comprehensive review 2015-2020. In: Expert Opinion on Therapeutic Patents, Vol. 31, no. 7, p. 597-608 (2021). doi:10.1080/13543776.2021.1890028 (Accepté/Sous presse).
  
  http://hdl.handle.net/2078.1/245991
- Kozlova, Arina ; Thabault, Léopold ; Liberelle, Maxime ; Klaessens, Simon ; Prévost, Julien R. C. ; Mathieu, Caroline ; Pilotte, Luc ; Stroobant, Vincent ; Van den Eynde, Benoît ; Frédérick, Raphaël.
  
  Rational Design of Original Fused-Cycle Selective Inhibitors of Tryptophan 2,3-Dioxygenase. In: Journal of Medicinal Chemistry, (2021). doi:10.1021/acs.jmedchem.1c00323 (Accepté/Sous presse).
  
  http://hdl.handle.net/2078.1/249792
- Thabault, Léopold ; Liberelle, Maxime ; Frédérick, Raphaël.
  
  Targeting protein self-association in drug design.. In: Drug Discovery Today, Vol. 26, no. 5, p. 1148-1163 (2021). doi:10.1016/j.drudis.2021.01.028.
  
  http://hdl.handle.net/2078.1/245989
- Kentache, Takfarinas ; Thabault, Léopold ; Deumer, Gladys ; Haufroid, Vincent ; Frédérick, Raphaël ; Linster, Carole ; Peracchi, Alessio ; Veiga da Cunha, Maria ; Bommer, Guido ; Van Schaftingen, Emile.
  
  The metalloprotein YhcH is an anomerase providing N-acetylneuraminate aldolase with the open form of its substrate. In: The Journal of biological chemistry, Vol. 296, p. 100699 [1-12] (2021). doi:10.1016/j.jbc.2021.100699.
  
  http://hdl.handle.net/2078.1/245992
- Spillier, Quentin ; Ravez, Séverine ; Dochain Simon ; Vertommen, Didier ; Thabault, Léopold ; Feron, Olivier ; Frédérick, Raphaël.
  
  Unravelling the Allosteric Targeting of PHGDH at the ACT-Binding Domain with a Photoactivatable Diazirine Probe and Mass Spectrometry Experiments. In: Molecules, Vol. 26, no. 2, p. 477 (2021). doi:10.3390/molecules26020477.
  
  http://hdl.handle.net/2078.1/241588
2020
- Article de journal
  
  Thabault, Léopold ; Brisson, Lucie ; Brustenga, Chiara ; Martinez Gache, Santiago A ; Prévost, Julien ; Kozlova, Arina ; Spillier, Quentin ; Liberelle, Maxime ; Benyahia, Zohra ; Messens, Joris ; Copetti, Tamara ; Sonveaux, Pierre ; Frédérick, Raphaël.
  
  Interrogating the lactate dehydrogenase tetramerization site using (stapled) peptides.. In: Journal of medicinal chemistry, Vol. 63, no.9, p. 4628-4643 (2020). doi:10.1021/acs.jmedchem.9b01955.
  
  http://hdl.handle.net/2078.1/230031
- Ameryckx, Alice ; Pochet, Lionel ; Wang, Gang ; Yildiz, Esra ; Es Saadi, Bouazza ; Wouters, Johan ; Van Bambeke, Françoise ; Frédérick, Raphaël.
  
  Pharmacomodulations of the benzoyl-thiosemicarbazide scaffold reveal antimicrobial agents targeting D-alanyl-D-alanine ligase in bacterio. In: European Journal of Medicinal Chemistry, Vol. 200, no.1, p. 112444 (2020). doi:10.1016/j.ejmech.2020.112444.
  
  http://hdl.handle.net/2078.1/230503
- Spillier, Quentin ; Ravez, Severine ; Unterlass, Judith ; Corbet, Cyril ; Degavre, Charline ; Feron, Olivier ; Frédérick, Raphaël.
  
  Structure–Activity Relationships (SARs) of α-Ketothioamides as Inhibitors of Phosphoglycerate Dehydrogenase (PHGDH). In: Pharmaceuticals, Vol. 13, no.2, p. 20 (2020). doi:10.3390/ph13020020.
  
  http://hdl.handle.net/2078.1/226552
- Kentache, Takfarinas ; Thabault, Léopold ; Peracchi, Alessio ; Frédérick, Raphaël ; Bommer, Guido ; Van Schaftingen, Emile.
  
  The putative Escherichia coli dehydrogenase YjhC metabolises two dehydrated forms of N-acetylneuraminate produced by some sialidases. In: Bioscience Reports, Vol. 40, no.6, p. 1-15 (2020). doi:10.1042/bsr20200927.
  
  http://hdl.handle.net/2078.1/240261

Didier Lambert

2015

2015
- Article de journal
  
  El Bakali, Jamal ; Muccioli, Giulio ; Body-Malapel, Mathilde ; Djouina, Madjid ; Klupsch, Frédérique ; Ghinet, Alina ; Barczyk, Amélie ; Renault, Nicolas ; Chavatte, Philippe ; Desreumaux, Pierre ; Lambert, Didier ; Millet, Régis.
  
  Conformational Restriction Leading to a Selective CB2 Cannabinoid Receptor Agonist Orally Active Against Colitis. In: ACS Medicinal Chemistry Letters, Vol. 6, no.2, p. 198-203 (2015). doi:10.1021/ml500439x.
  
  http://hdl.handle.net/2078.1/157082
- Al Houayek, Mireille ; Bottemanne, Pauline ; Subramanian, Kumar V ; Lambert, Didier ; Makriyannis, Alexandros ; Cani, Patrice D. ; Muccioli, Giulio.
  
  N-Acylethanolamine-hydrolyzing acid amidase inhibition increases colon N-palmitoylethanolamine levels and counteracts murine colitis. In: The FASEB Journal, Vol. 29, no.2, p. 650-661 (2015). doi:10.1096/fj.14-255208.
  
  http://hdl.handle.net/2078.1/157086

Quentin Spillier

2025
- Article de journal
  
  Dechenne, Juhans ; Wierzbicka, Magdalena ; Krimou, Reda ; El Aakchioui, Asia ; Malo Pueyo, Julia ; Messens, Joris ; Fillet, Marianne ; Spillier, Quentin ; Frédérick, Raphaël.
  
  Examining Arginase-1 Trimerization Uncovers a Promising Allosteric Site for Inhibition. In: Journal of Medicinal Chemistry. doi:10.1021/acs.jmedchem.4c01993.
  
  http://hdl.handle.net/2078.1/299208
2023
- Article de journal
  
  Solvay, Marie ; Holfelder, Pauline (co-first author) ; Klaessens, Simon ; Pilotte, Luc ; Stroobant, Vincent ; Lamy, Juliette ; Naulaerts, Stefan ; Spillier, Quentin ; Frédérick, Raphaël ; De Plaen, Etienne ; Sers, Christine ; Opitz, Christiane A ; Van den Eynde, Benoit ; Zhu, Jingjing.
  
  Tryptophan depletion sensitizes the AHR pathway by increasing AHR expression and GCN2/LAT1-mediated kynurenine uptake, and potentiates induction of regulatory T lymphocytes. In: Journal for immunotherapy of cancer, Vol. 11, no. 6, p. e006728 [1-15] (2023). doi:10.1136/jitc-2023-006728.
  
  http://hdl.handle.net/2078.1/275939
2021
- Article de journal
  
  Spillier, Quentin ; Frédérick, Raphaël.
  
  Phosphoglycerate dehydrogenase (PHGDH) inhibitors: a comprehensive review 2015-2020. In: Expert Opinion on Therapeutic Patents, Vol. 31, no. 7, p. 597-608 (2021). doi:10.1080/13543776.2021.1890028 (Accepté/Sous presse).
  
  http://hdl.handle.net/2078.1/245991
- Banh, Robert S. ; Kim, Esther S. ; Spillier, Quentin ; Biancur, Douglas E. ; Yamamoto, Keisuke ; Sohn, Albert S. W. ; Shi, Guangbin ; Jones, Drew R. ; Kimmelman, Alec C. ; Pacold, Michael E..
  
  The polar oxy-metabolome reveals the 4-hydroxymandelate CoQ10 synthesis pathway. In: Nature, Vol. 597, no.7876, p. 420-425 (2021). doi:10.1038/s41586-021-03865-w.
  
  http://hdl.handle.net/2078/285156
- Spillier, Quentin ; Ravez, Séverine ; Dochain Simon ; Vertommen, Didier ; Thabault, Léopold ; Feron, Olivier ; Frédérick, Raphaël.
  
  Unravelling the Allosteric Targeting of PHGDH at the ACT-Binding Domain with a Photoactivatable Diazirine Probe and Mass Spectrometry Experiments. In: Molecules, Vol. 26, no. 2, p. 477 (2021). doi:10.3390/molecules26020477.
  
  http://hdl.handle.net/2078.1/241588
2020
- Article de journal
  
  Thabault, Léopold ; Brisson, Lucie ; Brustenga, Chiara ; Martinez Gache, Santiago A ; Prévost, Julien ; Kozlova, Arina ; Spillier, Quentin ; Liberelle, Maxime ; Benyahia, Zohra ; Messens, Joris ; Copetti, Tamara ; Sonveaux, Pierre ; Frédérick, Raphaël.
  
  Interrogating the lactate dehydrogenase tetramerization site using (stapled) peptides.. In: Journal of medicinal chemistry, Vol. 63, no.9, p. 4628-4643 (2020). doi:10.1021/acs.jmedchem.9b01955.
  
  http://hdl.handle.net/2078.1/230031
- Spillier, Quentin ; Ravez, Severine ; Unterlass, Judith ; Corbet, Cyril ; Degavre, Charline ; Feron, Olivier ; Frédérick, Raphaël.
  
  Structure–Activity Relationships (SARs) of α-Ketothioamides as Inhibitors of Phosphoglycerate Dehydrogenase (PHGDH). In: Pharmaceuticals, Vol. 13, no.2, p. 20 (2020). doi:10.3390/ph13020020.
  
  http://hdl.handle.net/2078.1/226552

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ldri | Bruxelles Woluwe

Raphael Frédérick

Didier Lambert

Quentin Spillier