Publications
ldri | Bruxelles Woluwe
Frédérick Raphael
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Article de journalAncia, M., Wahni, K., Chakrowf, J., El Aakchioui, A., Claude, E., de Lhoneux, G., Liberelle, M., Janvier, S., Baranova, E., Malo Pueyo, J., Jijon Vergara, A., Papadopoulos, N., Balty, C., Dejeu, J., Decottignies, A., Messens, J., & Frédérick, R. (2025). Structural insights into the interaction between testis-specific Y-encoded-like protein 5 and ubiquitin-specific protease 7. Protein Science, 34(5), e70116. https://doi.org/10.1002/pro.70116 (Original work published 2025)
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Leone, G., Ucakar, B., Perros, F., Frédérick, R., & Vanbever, R. (2025). Synthesis and in vitro evaluation of polyethylene glycol-treprostinil conjugates for sustained local delivery in pulmonary arterial hypertension. European Journal of Pharmaceutical Sciences, 214, 107287. https://doi.org/10.1016/j.ejps.2025.107287 (Original work published 2025)
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Mazhari Dorooee, D., Ravez, S., Vertommen, D., Renault, N., Papadopoulos, N., Marteau, R., Charnelle, E., Porte, K., Gobert, A., Hennuyer, N., Herinckx, G., Pautric, M., Jonneaux, A., Devedjian, J.-C., Devos, D., Staels, B., Melnyk, P., Constantinescu, S., Frédérick, R., & El Bakali, J. (2025). LIBX-A401: A Novel Selective Inhibitor of Acyl-CoA Synthetase Long Chain Family Member 4 (ACSL4) and Its Binding Mode. Angewandte Chemie (International Edition), 64(19), e202500518. https://doi.org/10.1002/anie.202500518 (Original work published 2025)
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Nadal Bufi, F., van Gysel, M., Brustenga, C., Savoyen, P., Mathieu, C., Sonveaux, P., Spillier, Q., Fillet, M., Wouters, J., & Frédérick, R. (2025). Unveiling the activation mechanism of a dimeric LDH isoform and its implications for allosteric inhibition strategies. Protein Science, 34(12), e70367. (Original work published 2025)
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Dechenne, J., Wierzbicka, M., Krimou, R., El Aakchioui, A., Malo Pueyo, J., Messens, J., Fillet, M., Spillier, Q., & Frédérick, R. (2025). Examining Arginase-1 Trimerization Uncovers a Promising Allosteric Site for Inhibition. Journal of Medicinal Chemistry, 68(2), 1433-1445. https://doi.org/10.1021/acs.jmedchem.4c01993 (Original work published 2025)
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Leone, G., Ucakar, B., Perros, F., Frédérick, R., & Vanbever, R. (2025). Synthesis and in vitro evaluation of polyethylene glycol-treprostinil conjugates for sustained local delivery in pulmonary arterial hypertension. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 214(11), 107287. https://doi.org/10.1016/j.ejps.2025.107287 (Original work published 2025)
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Boughaleb, H., Verdoy, R., Pochet, A., Fabian, N., Bella, R., Muruganandam, G., Frédérick, R., Boudjeltia, K. Z., Bourez, A., Delporte, C., Van Antwerpen, P., Robert, A., Haufroid, V., Dewulf, J., Balligand, J.-L., & Montiel, V. (2025). Repurposing Bacopa monnieri extracts containing Aquaporin-1 blockers to improve systemic oxidative stress: The BacOxy_I study. Advances in redox research, 15, 100126 [1-21]. https://doi.org/10.1016/j.arres.2025.100126 (Original work published 2025)
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Article de journalGeeraerts, Z., Ishigami, I., Lewis-Ballester, A., Pham, K. N., Kozlova, A., Mathieu, C., Frédérick, R., Yeh, S.-R., & et al. (2024). Structural Insights into Protein-Inhibitor Interactions in Human Tryptophan Dioxygenase. Journal of Medicinal Chemistry, 67(16), 14543-14552. https://doi.org/10.1021/acs.jmedchem.4c01360 (Original work published 2024)
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Tan, Y., Pierrard, F., Frédérick, R., & Riant, O. (2024). Enhancing Tsuji–Trost deallylation in living cells with an internal-nucleophile coumarin-based probe. RSC Advances, 14(8), 5492-5498. https://doi.org/10.1039/d3ra08938j (Original work published 2024)
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Deskeuvre, M., Lan, J., Messens, J., Riant, O., Feron, O., & Frédérick, R. (2024). A novel approach to pH-Responsive targeted cancer Therapy: Inhibition of FaDu cancer cell proliferation with a pH low insertion Peptide-Conjugated DGAT1 inhibitor. International Journal of Pharmaceutics, 657, 124132. https://doi.org/10.1016/j.ijpharm.2024.124132 (Original work published 2024)
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Article de journalSolvay, M., Holfelder, P., Klaessens, S., Pilotte, L., Stroobant, V., Lamy, J., Naulaerts, S., Spillier, Q., Frédérick, R., De Plaen, E., Sers, C., Opitz, C. A., Van den Eynde, B., & Zhu, J. (2023). Tryptophan depletion sensitizes the AHR pathway by increasing AHR expression and GCN2/LAT1-mediated kynurenine uptake, and potentiates induction of regulatory T lymphocytes. Journal for immunotherapy of cancer, 11(6), e006728 [1-15]. https://doi.org/10.1136/jitc-2023-006728 (Original work published 2023)
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Tan, Y., Lefevre, M., Pierrard, F., Soetens, M., Shoueiry, M., Yildiz, E., Ibanez, S., Özkan, K., Feron, O., Frédérick, R., & Riant, O. (2023). Tandem Heck/Tsuji-Trost Reaction for Uncaging of Alloc-Protected Amines with Palladium Complexes in Living Cells. Journal of Organometallic Chemistry, 996, 122743 [1-9]. https://doi.org/10.1016/j.jorganchem.2023.122743 (Original work published 2023)
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Article de journalMarteau, R., Ravez, S., Mazhari Dorooee, D., Bouchaoui, H., Porte, K., Devedjian, J.-C., Melnyk, P., Devos, D., Frédérick, R., & El Bakali, J. (2022). Repositioning of FDA-Approved antifungal agents to interrogate Acyl-CoA synthetase long chain family member 4 (ACSL4) in ferroptosis. Biochemical Pharmacology, 204, 115239 [1-12]. https://doi.org/10.1016/j.bcp.2022.115239 (Original work published 2022)
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Kozlova, A., Thabault, L., Dauguet, N., Deskeuvre, M., Stroobant, V., Pilotte, L., Liberelle, M., Van den Eynde, B., & Frédérick, R. (2022). Investigation of chalcogen bioisosteric replacement in a series of heterocyclic inhibitors of tryptophan 2,3-dioxygenase. European Journal of Medicinal Chemistry, 227, 113892 [1-12]. https://doi.org/10.1016/j.ejmech.2021.113892 (Original work published 2022)
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Reynaerts, A., Vermeulen, F., Mottais, A., Gohy, S., Lebecque, P., Frédérick, R., Vanbever, R., & Leal, T. (2022). Needle-free iontophoresis-driven β-adrenergic sweat rate test. Journal of Cystic Fibrosis, 21(3), 407-415. https://doi.org/10.1016/j.jcf.2021.08.012 (Original work published 2022)
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Mirgaux, M., Scaillet, T., Kozlova, A., Tumanov, N., Frédérick, R., Bodart, L., & Wouters, J. (2022). Structural study of bioisosteric derivatives of 5-(1<i>H</i>-indol-3-yl)-benzotriazole and their ability to form chalcogen bonds. Acta Crystallographica Section E: Crystallographic Communications, 78(4), 418-424. https://doi.org/10.1107/s2056989022002948 (Original work published 2022)
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Thabault, L., Brustenga, C., Savoyen, P., Van Gysel, M., Wouters, J., Sonveaux, P., Frédérick, R., & Liberelle, M. (2022). Discovery of small molecules interacting at lactate dehydrogenases tetrameric interface using a biophysical screening cascade. European Journal of Medicinal Chemistry, 230, 114102 [1-10]. https://doi.org/10.1016/j.ejmech.2022.114102 (Original work published 2022)
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Shrestha, N., Xu, Y., Prévost, J. R. C., McCartney, F., Brayden, D., Frédérick, R., Beloqui Garcia, A., & Préat, V. (2022). Impact of PEGylation on an antibody-loaded nanoparticle-based drug delivery system for the treatment of inflammatory bowel disease. Acta Biomaterialia, 140, 561-572. https://doi.org/10.1016/j.actbio.2021.12.015 (Original work published 2022)
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Deskeuvre, M., Lan, J., Dierge, E., Messens, J., Riant, O., Corbet, C., Feron, O., & Frédérick, R. (2022). Targeting cancer cells in acidosis with conjugates between the carnitine palmitoyltransferase 1 inhibitor etomoxir and pH (low) insertion peptides. International Journal of Pharmaceutics, 624(1), 122041. https://doi.org/10.1016/j.ijpharm.2022.122041 (Original work published 2022)
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Article de journalZampieri, L., Sboarina, M., Cacace, A., Grasso, D., Thabault, L., Hamelin, L., Vazeille, T., Dumon, E., Rossignol, R., Frédérick, R., Sonveaux, E., Lefranc, F., & Sonveaux, P. (2021). Olaparib is a mitochondrial Complex I inhibitor that kills temozolomide-resistant human glioblastoma cells. International Journal of Molecular Sciences, 22(11938), 17. https://doi.org/10.3390/ijms222111938 (Original work published 2021)
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Kozlova, A., Thabault, L., Liberelle, M., Klaessens, S., Prévost, J. R. C., Mathieu, C., Pilotte, L., Stroobant, V., Van den Eynde, B., & Frédérick, R. (2021). Rational Design of Original Fused-Cycle Selective Inhibitors of Tryptophan 2,3-Dioxygenase. Journal of Medicinal Chemistry. Accepted/in-press. https://doi.org/10.1021/acs.jmedchem.1c00323 (Original work published 2021)
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Spillier, Q., & Frédérick, R. (2021). Phosphoglycerate dehydrogenase (PHGDH) inhibitors: a comprehensive review 2015-2020. Expert Opinion on Therapeutic Patents, 31(7), 597-608. https://doi.org/10.1080/13543776.2021.1890028 (Original work published 2021)
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Thabault, L., Liberelle, M., & Frédérick, R. (2021). Targeting protein self-association in drug design. Drug Discovery Today, 26(5), 1148-1163. https://doi.org/10.1016/j.drudis.2021.01.028 (Original work published 2021)
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Kentache, T., Thabault, L., Deumer, G., Haufroid, V., Frédérick, R., Linster, C., Peracchi, A., Veiga da Cunha, M., Bommer, G., & Van Schaftingen, E. (2021). The metalloprotein YhcH is an anomerase providing N-acetylneuraminate aldolase with the open form of its substrate. Journal of Biological Chemistry, 296, 100699 [1-12]. https://doi.org/10.1016/j.jbc.2021.100699 (Original work published 2021)
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Thabault, L., Liberelle, M., Koruza, K., Yildiz, E., Joudiou, N., Messens, J., Brisson, L., Wouters, J., Sonveaux, P., & Frédérick, R. (2021). Discovery of a novel lactate dehydrogenase tetramerization domain using epitope mapping and peptides. Journal of Biological Chemistry, 296, 100422. https://doi.org/10.1016/j.jbc.2021.100422 (Original work published 2021)
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Spillier, Q., Ravez, S., Dochain Simon, Vertommen, D., Thabault, L., Feron, O., & Frédérick, R. (2021). Unravelling the Allosteric Targeting of PHGDH at the ACT-Binding Domain with a Photoactivatable Diazirine Probe and Mass Spectrometry Experiments. Molecules, 26(2), 477. https://doi.org/10.3390/molecules26020477 (Original work published 2021)
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Article de journalThabault, L., Brisson, L., Brustenga, C., Martinez Gache, S. A., Prévost, J., Kozlova, A., Spillier, Q., Liberelle, M., Benyahia, Z., Messens, J., Copetti, T., Sonveaux, P., & Frédérick, R. (2020). Interrogating the lactate dehydrogenase tetramerization site using (stapled) peptides. Journal of Medicinal Chemistry, 63(9), 4628-4643. https://doi.org/10.1021/acs.jmedchem.9b01955 (Original work published 2020)
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Kentache, T., Thabault, L., Peracchi, A., Frédérick, R., Bommer, G., & Van Schaftingen, E. (2020). The putative Escherichia coli dehydrogenase YjhC metabolises two dehydrated forms of N-acetylneuraminate produced by some sialidases. Bioscience Reports : molecular and cellular biology of the cell surface, 40(6), 1-15. https://doi.org/10.1042/bsr20200927 (Original work published 2020)
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Spillier, Q., Ravez, S., Unterlass, J., Corbet, C., Degavre, C., Feron, O., & Frédérick, R. (2020). Structure–Activity Relationships (SARs) of α-Ketothioamides as Inhibitors of Phosphoglycerate Dehydrogenase (PHGDH). Pharmaceuticals, 13(2), 20. https://doi.org/10.3390/ph13020020 (Original work published 2020)
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Ameryckx, A., Pochet, L., Wang, G., Yildiz, E., Es Saadi, B., Wouters, J., Van Bambeke, F., & Frédérick, R. (2020). Pharmacomodulations of the benzoyl-thiosemicarbazide scaffold reveal antimicrobial agents targeting D-alanyl-D-alanine ligase in bacterio. European Journal of Medicinal Chemistry, 200(1), 112444. https://doi.org/10.1016/j.ejmech.2020.112444 (Original work published 2020)
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Lambert Didier
Wrong bibliography request.
Spilier Quentin
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Article de journalNadal Bufi, F., van Gysel, M., Brustenga, C., Savoyen, P., Mathieu, C., Sonveaux, P., Spillier, Q., Fillet, M., Wouters, J., & Frédérick, R. (2025). Unveiling the activation mechanism of a dimeric LDH isoform and its implications for allosteric inhibition strategies. Protein Science, 34(12), e70367. (Original work published 2025)
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Dechenne, J., Wierzbicka, M., Krimou, R., El Aakchioui, A., Malo Pueyo, J., Messens, J., Fillet, M., Spillier, Q., & Frédérick, R. (2025). Examining Arginase-1 Trimerization Uncovers a Promising Allosteric Site for Inhibition. Journal of Medicinal Chemistry, 68(2), 1433-1445. https://doi.org/10.1021/acs.jmedchem.4c01993 (Original work published 2025)
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Shi, G., Miller, C., Kuno, S., Rey Hipolito, A., El Nagar, S., Riboldi, G., Korn, M., Tran, W., Zixuan, W., Ficaro, L., Lin, T., Spillier, Q., Gamallo-Lana, B., Jones, D., Snuderl, M., Song, S., Mar, A., Joyner, A., Sillitoe, R., et al. (2025). Coenzyme Q headgroup intermediates treat a mitochondrial encephalopathy. Nature. Accepted/in-press. https://doi.org/10.1038/s41586-025-09246-x (Original work published 2025)
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Article de journalSolvay, M., Holfelder, P., Klaessens, S., Pilotte, L., Stroobant, V., Lamy, J., Naulaerts, S., Spillier, Q., Frédérick, R., De Plaen, E., Sers, C., Opitz, C. A., Van den Eynde, B., & Zhu, J. (2023). Tryptophan depletion sensitizes the AHR pathway by increasing AHR expression and GCN2/LAT1-mediated kynurenine uptake, and potentiates induction of regulatory T lymphocytes. Journal for immunotherapy of cancer, 11(6), e006728 [1-15]. https://doi.org/10.1136/jitc-2023-006728 (Original work published 2023)
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Article de journalSpillier, Q., & Frédérick, R. (2021). Phosphoglycerate dehydrogenase (PHGDH) inhibitors: a comprehensive review 2015-2020. Expert Opinion on Therapeutic Patents, 31(7), 597-608. https://doi.org/10.1080/13543776.2021.1890028 (Original work published 2021)
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Banh, R. S., Kim, E. S., Spillier, Q., Biancur, D. E., Yamamoto, K., Sohn, A. S. W., Shi, G., Jones, D. R., Kimmelman, A. C., & Pacold, M. E. (2021). The polar oxy-metabolome reveals the 4-hydroxymandelate CoQ10 synthesis pathway. Nature, 597(7876), 420-425. https://doi.org/10.1038/s41586-021-03865-w (Original work published 2021)
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Spillier, Q., Ravez, S., Dochain Simon, Vertommen, D., Thabault, L., Feron, O., & Frédérick, R. (2021). Unravelling the Allosteric Targeting of PHGDH at the ACT-Binding Domain with a Photoactivatable Diazirine Probe and Mass Spectrometry Experiments. Molecules, 26(2), 477. https://doi.org/10.3390/molecules26020477 (Original work published 2021)
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Article de journalThabault, L., Brisson, L., Brustenga, C., Martinez Gache, S. A., Prévost, J., Kozlova, A., Spillier, Q., Liberelle, M., Benyahia, Z., Messens, J., Copetti, T., Sonveaux, P., & Frédérick, R. (2020). Interrogating the lactate dehydrogenase tetramerization site using (stapled) peptides. Journal of Medicinal Chemistry, 63(9), 4628-4643. https://doi.org/10.1021/acs.jmedchem.9b01955 (Original work published 2020)
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Spillier, Q., Ravez, S., Unterlass, J., Corbet, C., Degavre, C., Feron, O., & Frédérick, R. (2020). Structure–Activity Relationships (SARs) of α-Ketothioamides as Inhibitors of Phosphoglycerate Dehydrogenase (PHGDH). Pharmaceuticals, 13(2), 20. https://doi.org/10.3390/ph13020020 (Original work published 2020)
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