Publications

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

Tan, Yonghua ; Lefevre, Marine ; Pierrard, François ; Soetens, Mathieu ; Shoueiry, Maria ; Yildiz, Esra ; Ibanez, Sébastien ; Ozkan, Kubra ; 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, no.-, p. 122743 (2023). doi:10.1016/j.jorganchem.2023.122743.

http://hdl.handle.net/2078.1/275937

Solvay, Marie ; Holfelder, Pauline ; 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 (2023). doi:10.1136/jitc-2023-006728.

http://hdl.handle.net/2078.1/275939

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

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

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

Kassehin, Comlan Urbain ; Adjibode, Steeve A ; Bautista, Oscar ; Gbaguidi, Fernand A ; Quetin-Leclercq, Joëlle ; McCurdy, Christopher R ; Frédérick, Raphaël ; Poupaert, Jacques. Anomalous reactivity of benzopinacolone towards 4-phenylthiosemicarbazide, a nucleophile endowed with alpha-effect. In: Journal of Medicinal and Chemical Sciences, Vol. 2, no.1, p. 17-20 (2019). doi:10.26655/JMCHEMSCI.2019.6.3.

http://hdl.handle.net/2078.1/209781

Spillier, Quentin ; Vertommen, Didier ; Séverine Ravez ; Marteau, Romain ; THÉMANS, Quentin ; Corbet, Cyril ; Feron, Olivier ; Wouters, Johan ; Frédérick, Raphaël. Anti-alcohol abuse drug disulfiram inhibits human PHGDH via disruption of its active tetrameric form through a specific cysteine oxidation. In: Scientific Reports, Vol. 9, no. 1, p. 4737 (2019).

http://hdl.handle.net/2078/210036

Kozlova, Arina ; Frédérick, Raphaël. Current state on tryptophan 2,3-dioxygenase inhibitors: a patent review. In: Expert Opinion on Therapeutic Patents, Vol. 29, no. 1, p. 11-23 (2019). doi:10.1080/13543776.2019.1556638 (Accepté/Sous presse).

http://hdl.handle.net/2078.1/209019

Ameryckx, Alice ; Thabault, Léopold ; Pochet, Lionel ; Leimanis, Serge ; Poupaert, Jacques ; Wouters, Johan ; Joris, Bernard ; Van Bambeke, Françoise ; Frédérick, Raphaël. 1-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting d-alanine-d-alanine ligase in bacterio. In: European Journal of Medicinal Chemistry, Vol. 159, p. 324-338 (2018). doi:10.1016/j.ejmech.2018.09.067.

http://hdl.handle.net/2078.1/208975

Prevost, Julien R.C. ; Kozlova, Arina ; Es Saadi, Bouazza ; Yildiz, Esra ; Modaffari, Sara ; Lambert, Didier M. ; Pochet, Lionel ; Wouters, Johan ; Dolušić, Eduard ; Frédérick, Raphaël. Convenient one-pot formation of highly functionalized 5-bromo-2-aminothiazoles, potential endocannabinoid hydrolase MAGL inhibitors. In: Tetrahedron Letters, Vol. 59, no.49, p. 4315-4319 (2018). doi:10.1016/j.tetlet.2018.10.055.

http://hdl.handle.net/2078.1/209011

Frédérick, Raphaël ; Pochet, Lionel ; De Tullio, Pascal ; Dufrasne, François. 31ièmes Journées Franco-Belges de Pharmacochimie: Meeting Report.. In: Pharmaceuticals, Vol. 10, p. 94 [1-12] (2017). doi:10.3390/ph10040094.

http://hdl.handle.net/2078.1/195091

Mortier, Jérémie ; Prévost, Julien ; Sydow, Dominique ; Teuchert, Sabine ; Omieczynski, Christian ; Bermudez, Marcel ; Frédérick, Raphaël ; Wolber, Gerhard. Arginase Structure and Inhibition: Catalytic Site Plasticity Reveals New Modulation Possibilities.. In: Scientific Reports, Vol. 7, p. 13616 [1-9] (2017). doi:10.1038/s41598-017-13366-4.

http://hdl.handle.net/2078.1/195088

Ravez, Séverine ; Spillier, Quentin ; Marteau, Romain ; Feron, Olivier ; Frédérick, Raphaël. Challenges and Opportunities in the Development of Serine Synthetic Pathway Inhibitors for Cancer Therapy.. In: Journal of Medicinal Chemistry, Vol. 60, no. 4, p. 1227-1237 (2017). doi:10.1021/acs.jmedchem.6b01167.

http://hdl.handle.net/2078.1/180991

Kassehin, Urbain C. ; Fagla, Sèdami M. ; Gbaguidi, Fernand A. ; Prévost, Julien ; Frédérick, Raphaël ; Poupaert, Jacques. DMF. I2 Complex as Efficient Green Catalyst in the Diels-alder Reaction of Anthracene-9-Methanol with Maleimide. In: Current Green Chemistry, Vol. 4, no. 1, p. 45-49 (2017). doi:10.2174/2213346104666170704112332.

http://hdl.handle.net/2078.1/195092

Van Hee, Vincent F ; Labar, Daniel ; Dehon, Gwenaël ; Grasso, Debora ; Gregoire, Vincent ; Muccioli, Giulio ; Frédérick, Raphaël ; Sonveaux, Pierre. Radiosynthesis and validation of (±)-[18F]-3-fluoro-2-hydroxypropionate ([18F]-FLac) as a PET tracer of lactate to monitor MCT1-dependent lactate uptake in tumors. In: OncoTarget, Vol. 8, no. 15, p. 24415-24428 (2017). doi:10.18632/oncotarget.14705.

http://hdl.handle.net/2078.1/179754

Ravez, Séverine ; Corbet, Cyril ; Spillier, Quentin ; Dutu, Alice ; Robin, Anita D ; Mullarky, Edouard ; Cantley, Lewis Clayton ; Feron, Olivier ; Frédérick, Raphaël. α-Ketothioamide derivatives: a promising tool to interrogate the phosphoglycerate dehydrogenase (PHGDH).. In: Journal of Medicinal Chemistry, (2017). doi:10.1021/acs.jmedchem.6b01166 (Accepté/Sous presse).

http://hdl.handle.net/2078.1/180996

Neyrinck, Audrey M. ; Pachikian, Barbara D. ; Taminiau , Bernard ; Daube , Georges ; Frédérick, Raphaël ; Cani, Patrice D. ; Bindels, Laure B. ; Delzenne, Nathalie M.. Intestinal Sucrase as a Novel Target Contributing to the Regulation of Glycemia by Prebiotics. In: PLoS One, Vol. 11, no.8, p. e0160488 [1-13] (2016). doi:10.1371/journal.pone.0160488.

http://hdl.handle.net/2078.1/179136

Brisson, Lucie ; Banski, Piotr ; Sboarina, Martina ; Dethier, Coralie ; Danhier, Pierre ; Fontenille, Marie-Joséphine ; Van Hee, Vincent F ; Vazeille, Thibaut ; Tardy, Morgane ; Falces Ramos, Jorge ; Bouzin, Caroline ; Porporato, Paolo ; Frédérick, Raphaël ; Michiels, Carine ; Copetti, Tamara ; Sonveaux, Pierre. Lactate Dehydrogenase B Controls Lysosome Activity and Autophagy in Cancer.. In: Cancer Cell, Vol. 30, no.3, p. 418-431 (2016). doi:10.1016/j.ccell.2016.08.005.

http://hdl.handle.net/2078.1/176817

Luo, Tian ; Magnusson, J ; Préat, Véronique ; Frédérick, Raphaël ; Alexander, Cameron ; Bosquillon, Cynthia ; Vanbever, Rita. Synthesis and in vitro evaluation of polyethylene glycol paclitaxel conjugates for lung cancer therapy. In: Pharmaceutical Research, Vol. 33, no. 7, p. 1671-1681. doi:10.1007/s11095-016-1908-2.

http://hdl.handle.net/2078.1/162065

Bouckaert, Charlotte ; Serra, Silvia ; Rondelet, Grégoire ; Dolušić, Eduard ; Wouters, Johan ; Dogné, Jean-Michel ; Frédérick, Raphaël ; Pochet, Lionel. Synthesis, evaluation and structure-activity relationship of new 3-carboxamide coumarins as FXIIa inhibitors. In: European Journal of Medicinal Chemistry, Vol. 110, p. 181-194 (2016). doi:10.1016/j.ejmech.2016.01.023.

http://hdl.handle.net/2078.1/172296

The Members of the Organizing Committee ; Frédérick, Raphaël ; Pochet, Lionel ; De Tullio, Pascal ; Dufrasne, François E.. 29ièmes Journées Franco-Belges de Pharmacochimie: Meeting Report. In: Pharmaceuticals, Vol. 8, no.4, p. 758-777 (2015). doi:10.3390/ph8040758.

http://hdl.handle.net/2078.1/170021

Meinguet, Céline ; Bruyère, Céline ; Frédérick, Raphaël ; Mathieu, Véronique ; Vancraeynest, Christelle ; Pochet, Lionel ; Laloy, Julie ; Mortier, Jérémie ; Wolber, Gerhard ; Kiss, Robert ; Masereel, Bernard ; Wouters, Johan. 3D-QSAR, design, synthesis and characterization of trisubstituted harmine derivatives with in vitro antiproliferative properties. In: European Journal of Medicinal Chemistry, Vol. 94, no. 1, p. 45-55 (2015). doi:10.1016/j.ejmech.2015.02.044.

http://hdl.handle.net/2078.1/165298

Gbaguidi, Fernand A. ; Kassehin, Comlan Urbain ; Prévost, Julien ; Frédérick, Raphaël ; McCurdy, Christopher R. ; Poupaert, Jacques. Insight into the Diels-Alder reaction : A green chemistry revisitation of the synthesis of a cantharidine-like trypanocidal pilot-molecule . In: Journal of Chemical and Pharmaceutical Research, Vol. 7, no.7, p. 1109-1113 (2015).

http://hdl.handle.net/2078.1/167578

Ravez, Séverine ; Arsenlis, Stéphane ; Barczyk, Amélie ; Dupont, Anthony ; Frédérick, Raphaël ; Hesse, Stéphanie ; Kirsch, Gilbert ; Depreux, Patrick ; Goossens, Laurence. Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors. In: Bioorganic & Medicinal Chemistry : the tetrahedron journal for research at the interface of chemistry and biology, Vol. 23, no.22, p. 7340-7347 (2015). doi:10.1016/j.bmc.2015.10.035.

http://hdl.handle.net/2078.1/167596

Kendall, Jackie D. ; Marshall, Andrew J. ; Giddens, Anna C. ; Tsang, Kit Yee ; Boyd, Maruta ; Frédérick, Raphaël ; Lill, Claire L. ; Lee, Woo-Jeong ; Kolekar, Sharada ; Chao, Mindy ; Malik, Alisha ; Yu, Shuqiao ; Chaussade, Claire ; Buchanan, Christina M. ; Rewcastle, Gordon W. ; Baguley, Bruce C. ; Flanagan, Jack U. ; Denny, William A. ; Shepherd, Peter R.. Novel pyrazolo[1,5-a]pyridines as PI3K inhibitors: variation of the central linker group. In: MedChemComm, Vol. 5, no.1, p. 41 [1-6] (2014). doi:10.1039/C3MD00221G.

http://hdl.handle.net/2078.1/145674

Serra, Silvia ; Moineaux, Laurence ; Vancraeynest, Christelle ; Masereel, Bernard ; Wouters, Johan ; Pochet, Lionel ; Frédérick, Raphaël. Thiosemicarbazide, a fragment with promising indolamine-2,3-dioxygenase (IDO) inhibition properties. In: European Journal of Medicinal Chemistry, Vol. 82, p. 96-105 (2014). doi:10.1016/j.ejmech.2014.05.044.

http://hdl.handle.net/2078.1/159719

Dolusic, Eduard ; Frédérick, Raphaël. Indoleamine 2,3-dioxygenase inhibitors: a patent review (2008 - 2012).. In: Expert Opinion on Therapeutic Patents, Vol. 23, no.10, p. 1367-1381 (2013). doi:10.1517/13543776.2013.827662.

http://hdl.handle.net/2078.1/146379

Dolusic, Eduard ; Larrieu, Pierre ; Meinguet, Céline ; Colette, Delphine ; Rives, Arnaud ; Blanc, Sébastien ; Ferain, Thierry ; Pilotte, Luc ; Stroobant, Vincent ; Wouters, Johan ; Van den Eynde, Benoît ; Masereel, Bernard ; Delfourne, Evelyne ; Frédérick, Raphaël. Indoleamine 2,3-dioxygenase inhibitory activity of derivatives of marine alkaloid tsitsikammamine A.. In: Bioorganic & Medicinal Chemistry Letters, Vol. 23, no.1, p. 47-54 (2013). doi:10.1016/j.bmcl.2012.11.036.

http://hdl.handle.net/2078/121072

Rogez-Florent, Tiphaine ; Meignan, Samuel ; Foulon, Catherine ; Six, Perrine ; Gros, Abigaëlle ; Bal-Mahieu, Christine ; Supuran, Claudiu T. ; Scozzafava, Andrea ; Frédérick, Raphaël ; Masereel, Bernard ; Depreux, Patrick ; Lansiaux, Amélie ; Goossens, Jean-François ; Gluszok, Sébastien ; Goossens, Laurence. New selective carbonic anhydrase IX inhibitors: Synthesis and pharmacological evaluation of diarylpyrazole-benzenesulfonamides. In: Bioorganic & Medicinal Chemistry : the tetrahedron journal for research at the interface of chemistry and biology, Vol. 21, no. 6, p. 1451-1464 (2013). doi:10.1016/j.bmc.2012.10.029.

http://hdl.handle.net/2078.1/162946

Mortier, Jeremie ; Rakers, Christin ; Frédérick, Raphaël ; Wolber, Gerhard. Computational tools for in silico fragment-based drug design. In: Current Topics in Medicinal Chemistry, Vol. 12, no. 17, p. 1935-1943 (2012). doi:10.2174/156802612804547371.

http://hdl.handle.net/2078.1/162945

Kendall, Jackie D. ; O'Connor, Patrick D. ; Marshall, Andrew J. ; Frédérick, Raphaël ; Marshall, Elaine S. ; Lill, Claire L. ; Lee, Woo-Jeong ; Kolekar, Sharada ; Chao, Mindy ; Malik, Alisha ; Yu, Shuqiao ; Chaussade, Claire ; Buchanan, Christina ; Rewcastle, Gordon W. ; Baguley, Bruce C. ; Flanagan, Jack U. ; Jamieson, Stephen M.F. ; Denny, William A. ; Shepherd, Peter R.. Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors. In: Bioorganic & Medicinal Chemistry : the tetrahedron journal for research at the interface of chemistry and biology, Vol. 20, no. 1, p. 69-85 (2012).

http://hdl.handle.net/2078.1/162924

Kendall, Jackie D. ; Giddens, Anna C. ; Tsang, Kit Yee ; Frédérick, Raphaël ; Marshall, Elaine S. ; Singh, Ripudaman ; Lill, Claire L. ; Lee, Woo-Jeong ; Kolekar, Sharada ; Chao, Mindy ; Malik, Alisha ; Yu, Shuqiao ; Chaussade, Claire ; Buchanan, Christina ; Rewcastle, Gordon W. ; Baguley, Bruce C. ; Flanagan, Jack U. ; Jamieson, Stephen M.F. ; Denny, William A. ; Shepherd, Peter R.. Novel pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR. In: Bioorganic & Medicinal Chemistry : the tetrahedron journal for research at the interface of chemistry and biology, Vol. 20, no. 1, p. 58-68 (2012). doi:10.1016/j.bmc.2011.11.031.

http://hdl.handle.net/2078.1/162923

Frédérick, Raphaël ; Bruyére, Céline ; Vancraeynest, Christelle ; Reniers, Jérémy ; Meinguet, Céline ; Pochet, Lionel ; Backlund, Anders ; Masereel, Bernard ; Kiss, Robert ; Wouters, Johan. Novel trisubstituted harmine derivatives with original in vitro anticancer activity. In: Journal of Medicinal Chemistry, Vol. 55, no. 14, p. 6489-6501 (2012). doi:10.1021/jm300542e.

http://hdl.handle.net/2078.1/162942

Pilotte, Luc ; Larrieu, Pierre ; Stroobant, Vincent ; Colau, Didier ; Dolusic, Eduard ; Frédérick, Raphaël ; De Plaen, Etienne ; Uyttenhove, Catherine ; Wouters, Johan ; Masereel, Bernard ; Van den Eynde, Benoît. Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase.. In: Proceedings of the National Academy of Sciences of the United States of America, Vol. 109, no. 7, p. 2497-2502 (2012). doi:10.1073/pnas.1113873109.

http://hdl.handle.net/2078/121066

Moineaux, Laurence ; Laurent, Sophie ; Reniers, Jérémy ; Dolušić, Eduard ; Galleni, Moreno ; Frère, Jean-Marie ; Masereel, Bernard ; Frédérick, Raphaël ; Wouters, Johan. Synthesis, crystal structures and electronic properties of isomers of chloro-pyridinylvinyl-1H-indoles. In: European Journal of Medicinal Chemistry, Vol. 54, no. 1, p. 95-102 (2012). doi:10.1016/j.ejmech.2012.04.033.

http://hdl.handle.net/2078.1/162944

Dolusic, Eduard ; Larrieu, Pierre ; Blanc, Sébastien ; Sapunaric, Frédéric ; Norberg, Bernadette ; Moineaux, Laurence ; Colette, Delphine ; Stroobant, Vincent ; Pilotte, Luc ; Colau, Didier ; Ferain, Thierry ; Fraser, Graeme ; Galleni, Moreno ; Frre, Jean-Marie ; Masereel, Bernard ; Van den Eynde, Benoît ; Wouters, Johan ; Frédérick, Raphaël. Corrigendum to "Indol-2-yl ethanones as novel indoleamine 2,3-dioxygenase (IDO) inhibitors" (Bioorganic and Medicinal Chemistry (2011) (1550-1561)). In: Bioorganic & Medicinal Chemistry : the tetrahedron journal for research at the interface of chemistry and biology, Vol. 19, no.9, p. 3029 (2011).

http://hdl.handle.net/2078.1/170172

Dolusic, Eduard ; Larrieu, Pierre ; Blanc, Sébastien ; Sapunaric, Frédéric ; Pouyez, Jenny ; Moineaux, Laurence ; Colette, Delphine ; Stroobant, Vincent ; Pilotte, Luc ; Colau, Didier ; Ferain, Thierry ; Fraser, Graeme ; Galleni, Moreno ; Frère, Jean-Marie ; Masereel, Bernard ; Van den Eynde, Benoît ; Wouters, Johan ; Frédérick, Raphaël. Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (IDO) inhibitors. In: European Journal of Medicinal Chemistry, Vol. 46, no. 7, p. 3058-3065 (2011). doi:10.1016/j.ejmech.2011.02.049.

http://hdl.handle.net/2078.1/106226

Dolusic, Eduard ; Larrieu, Pierre ; Blanc, Sébastien ; Sapunaric, Frédéric ; Norberg, Bernadette ; Moineaux, Laurence ; Colette, Delphine ; Stroobant, Vincent ; Pilotte, Luc ; Colau, Didier ; Ferain, Thierry ; Fraser, Graeme ; Galleni, Moreno ; Frère, Jean-Marie ; Masereel, Bernard ; Van den Eynde, Benoît ; Wouters, Johan ; Frédérick, Raphaël. Indol-2-yl ethanones as novel indoleamine 2,3-dioxygenase (IDO) inhibitors. In: Bioorganic & Medicinal Chemistry, Vol. 19, no. 4, p. 1550-1561 (2011). doi:10.1016/j.bmc.2010.12.032.

http://hdl.handle.net/2078.1/106246

Rewcastle, Gordon W. ; Gamage, Swarna A. ; Flanagan, Jack U. ; Frédérick, Raphaël ; Denny, William A. ; Baguley, Bruce C. ; Kestell, Philip ; Singh, Ripudaman ; Kendall, Jackie D. ; Marshall, Elaine S. ; Lill, Claire L. ; Lee, Woo-Jeong ; Kolekar, Sharada ; Buchanan, Christina M. ; Jamieson, Stephen M.F. ; Shepherd, Peter R.. Synthesis and biological evaluation of novel analogues of the pan class i phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(Difluoromethyl)-1-[4,6-di(4- morpholinyl)-1,3,5-triazin-2-yl]-1 H -benzimidazole (ZSTK474). In: Journal of Medicinal Chemistry, Vol. 54, no.20, p. 7105-7126 (2011). doi:10.1021/jm200688y.

http://hdl.handle.net/2078.1/162912

Reniers, Jérémy ; Robert, S. ; Frédérick, Raphaël ; Masereel, Bernard ; Vincent, S. ; Wouters, Johan. Synthesis and evaluation of β-carboline derivatives as potential monoamine oxidase inhibitors. In: European Journal of Medicinal Chemistry, Vol. 19, no. 1, p. 134-144 (2011). doi:10.1016/j.bmc.2010.11.041.

http://hdl.handle.net/2078.1/162920

Reniers, Jérémy ; Meinguet, Céline ; Moineaux, Laurence ; Masereel, Bernard ; Vincent, S.P. ; Frédérick, Raphaël ; Wouters, Johan. Synthesis and inhibition study of monoamine oxidase, indoleamine 2,3-dioxygenase and tryptophan 2,3-dioxygenase by 3,8-substituted 5H-indeno[1,2-c]pyridazin-5-one derivatives. In: European Journal of Medicinal Chemistry, Vol. 46, no. 12, p. 6104-6111 (2011). doi:10.1016/j.ejmech.2011.09.042.

http://hdl.handle.net/2078.1/162921

Dolusic, Eduard ; Larrieu, Pierre ; Moineaux, Laurence ; Stroobant, Vincent ; Pilotte, Luc ; Colau, Didier ; Pochet, Lionel ; Van den Eynde, Benoît ; Masereel, Bernard ; Wouters, Johan ; Frédérick, Raphaël. Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators. In: Journal of Medicinal Chemistry, Vol. 54, no. 15, p. 5320-5334 (11/08/2011). doi:10.1021/jm2006782.

http://hdl.handle.net/2078.1/106222

Gluszok, Sebastien ; Frédérick, Raphaël ; Foulon, Catherine ; Klupsch, Frederique ; Supuran, Claudiu T. ; Vullo, Daniela ; Scozzafava, Andrea ; Goossens, Jean-Francois ; Masereel, Bernard ; Depreux, Patrick ; Goossens, Laurence. Design, solid-phase synthesis, and biological evaluation of novel 1,5-diarylpyrrole-3-carboxamides as carbonic anhydrase IX inhibitors. In: Bioorganic & Medicinal Chemistry : the tetrahedron journal for research at the interface of chemistry and biology, Vol. 18, no. 21, p. 7392-7401 (2010). doi:10.1016/j.bmc.2010.09.007.

http://hdl.handle.net/2078.2/98097

Mortier, Jérémie ; Masereel, Bernard ; Remouchamps, Caroline ; Ganeff, Corinne ; Piette, Jacques ; Frédérick, Raphaël. NF-κB inducing kinase (NIK) inhibitors: Identification of new scaffolds using virtual screening. In: Bioorganic & Medicinal Chemistry Letters : the tetrahedron journal for research at the interface of chemistry and biology, Vol. 20, no. 15, p. 4515-4520 (2010). doi:10.1016/j.bmcl.2010.06.027.

http://hdl.handle.net/2078.1/162919

Mortier, Jérémie ; Frédérick, Raphaël ; Ganeff, Corinne ; Remouchamps, Caroline ; Talaga, Patrice ; Pochet, Lionel ; Wouters, Johan ; Piette, Jacques ; Dejardin, Emmanuel ; Masereel, Bernard. Pyrazolo[4,3-c]isoquinolines as potential inhibitors of NF-κB activation. In: Biochemical Pharmacology, Vol. 79, no. 10, p. 1462-1472 (2010). doi:10.1016/j.bcp.2010.01.007.

http://hdl.handle.net/2078.1/162918

Thiry, Anne ; Ledecq, Marie ; Cecchi, Alessandro ; Frédérick, Raphaël ; Dogné, Jean-Michel ; Supuran, Caudiu T ; Wouters, Johan ; Masereel, Bernard. Ligand-based and structure-based virtual screening to identify carbonic anhydrase IX inhibitors. In: Bioorganic & medicinal chemistry, Vol. 17, no. 2, p. 553-557 (2009). doi:10.1016/j.bmc.2008.11.071.

http://hdl.handle.net/2078.2/20784

Frédérick, Raphaël ; Mawson, Claire ; Kendall, Jackie D ; Chaussade, Claire ; Rewcastle, Gordon W ; Shepherd, Peter R ; Denny, William A. Phosphoinositide-3-kinase (PI3K) inhibitors: identification of new scaffolds using virtual screening. In: Bioorganic & Medicinal Chemistry Letters : the tetrahedron journal for research at the interface of chemistry and biology, Vol. 19, no.20, p. 5842-5847 (2009). doi:10.1016/j.bmcl.2009.08.087.

http://hdl.handle.net/2078.1/170378

Frédérick, Raphaël ; Denny, William A.. Phosphoinositide-3-kinases (PI3Ks): Combined comparative modeling and 3D-QSAR to rationalize the inhibition of p110α. In: Journal of Chemical Information and Modeling, Vol. 48, no. 3, p. 629-638 (2008). doi:10.1021/ci700348m.

http://hdl.handle.net/2078.1/162917

Frédérick, Raphaël ; Robert, S. ; Charlier, Caroline ; Wouters, Johan ; Masereel, Bernard ; Pochet, Lionel. Mechanism-based thrombin inhibitors: design, synthesis, and molecular docking of a new selective 2-oxo-2H-1-benzopyran derivative.. In: Journal of medicinal chemistry, Vol. 50, no. 15, p. 3645-3650 (2007). doi:10.1021/jm061368v.

http://hdl.handle.net/2078.2/8137

Kendall, Jackie D. ; Rewcastle, Gordon W. ; Frédérick, Raphaël ; Mawson, Claire ; Denny, William A. ; Marshall, Elaine S. ; Baguley, Bruce C. ; Chaussade, Claire ; Jackson, Shaun P. ; Shepherd, Peter R.. Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110α inhibitors. In: Bioorganic & Medicinal Chemistry : the tetrahedron journal for research at the interface of chemistry and biology, Vol. 15, no. 24, p. 7677-7687 (2007). doi:10.1016/j.bmc.2007.08.062.

http://hdl.handle.net/2078.1/162914

Frédérick, Raphaël ; Charlier, Caroline ; Robert, S. ; Wouters, Johan ; Masereel, Bernard ; Pochet, Lionel. Investigation of mechanism-based thrombin inhibitors: Implications of a highly conserved water molecule for the binding of coumarins within the S pocket.. In: Bioorganic & Medicinal Chemistry Letters : the tetrahedron journal for research at the interface of chemistry and biology, Vol. 16, no. 7, p. 2017-2021 (2006). doi:10.1016/j.bmcl.2005.12.070.

http://hdl.handle.net/2078.2/7690

Frédérick, Raphaël ; Dumont, Willy ; Ooms, Frederic ; Aschenbach, Lindsey ; van der Schyf, Cornelis J. ; Castagnoli, Neal ; Wouters, Johan ; Krief, Alain. Synthesis, structural reassignment, and biological activity of type B MAO inhibitors based on the 5H-indeno[1,2-c]pyridazin-5-one core. In: Journal of Medicinal Chemistry, Vol. 49, no. 12, p. 3743-3747 (2006). doi:10.1021/jm051091j.

http://hdl.handle.net/2078.2/98663

Frédérick, Raphaël ; Ooms, Frédéric ; Castagnoli, Neal ; Petzer, Jacques P ; Feng, JiangFan ; Schwarzschild, Michael A ; Van der Schyf, Cornelis J. ; Wouters, Johan. (E)-8-(3-Chlorostyryl)-1,3,7-trimethylxanthine, a caffeine derivative acting both as antagonist of adenosine A2A receptors and as inhibitor of MAO-B. In: Acta crystallographica. Section C , Crystal structure communications, Vol. 61, no. Pt 9, p. O531-O532 (2005). doi:10.1107/S0108270105023140.

http://hdl.handle.net/2078.2/101604

Frédérick, Raphaël ; Robert, S. ; Charlier, Caroline ; de Ruyck, Jérôme ; Wouters, Johan ; Pirotte, Bernard ; Masereel, Bernard ; Pochet, Lionel. 3,6-disubstituted coumarins as mechanism-based inhibitors of thrombin and factor Xa. In: Journal of Medicinal Chemistry, Vol. 48, no. 24, p. 7592-7603 (2005). doi:10.1021/jm050448g.

http://hdl.handle.net/2078.2/7697

Frédérick, Raphaël ; Pochet, Lionel ; Charlier, Caroline ; Masereel, Bernard. Modulators of the coagulation cascade: focus and recent advances in inhibitors of tissue factor, factor VIIa and their complex. In: Current medicinal chemistry, Vol. 12, no. 4, p. 397-417 (2005). doi:10.2174/0929867053363108#sthash.ktd5dWDd.dpuf.

http://hdl.handle.net/2078.2/7731

Pochet, Lionel ; Frédérick, Raphaël ; Masereel, Bernard. Coumarin and isocoumarin as serine protease inhibitors. In: Current pharmaceutical design, Vol. 10, no. 30, p. 3781-3796 (2004). doi:10.2174/1381612043382684.

http://hdl.handle.net/2078.2/7742

Frédérick, Raphaël ; Norberg, Bernadette ; Durant, François ; Ooms, Frederic ; Wouters, Johan. Three 5H-indeno[1,2-c]pyridazin-5-one derivatives, potent type-B monoamine oxidase inhibitors. In: Acta crystallographica. Section C, Crystal structure communications, Vol. 60, no. Pt 9, p. O623-O626 (2004). doi:10.1107/S0108270104014660.

http://hdl.handle.net/2078.2/7761

Pochet, Lionel ; Dieu, Marc ; Frédérick, Raphaël ; Murray, Anne-Marie ; Kempen, Isabelle ; Pirotte, Bernad ; Masereel, Bernard. Investigation of the inhibition mechanism of coumarins on chymotrypsin by mass spectrometry. In: Tetrahedron, Vol. 59, no. 25, p. 4557-4561 (2003). doi:10.1016/S0040-4020(03)00660-4.

http://hdl.handle.net/2078.2/99006

Ooms, Frédéric ; Frédérick, Raphaël ; Durant, François ; Petzer, Jacobus P ; Castagnoli, Neal ; Van der Schyf, Cornelis J ; Wouters, Johan. Rational approaches towards reversible inhibition of type B monoamine oxidase. Design and evaluation of a novel 5H-Indeno[1,2-c]pyridazin-5-one derivative. In: Bioorganic & medicinal chemistry letters, Vol. 13, no. 1, p. 69-73 (2003). doi:10.1016/S0960-894X(02)00838-7.

http://hdl.handle.net/2078.2/7834

Sonveaux, Pierre ; Frédérick, Raphaël ; Spillier, Quentin ; Kluge, Andreas ; Kaiser, Florian Tobias ; Leberecht Christoph ; Haupt, Joachim. Inhibitor of lactate dehydrogenase. Numéro de priorité ; Déposé (14/10/2024). European Patent Office.

http://hdl.handle.net/2078.1/292735

Sonveaux, Pierre ; Frédérick, Raphaël ; Spillier, Quentin ; Kluge, Andreas ; Kaiser, Florian Tobias ; Leberecht, Christoph ; Haupt, Joachim. Inhibitors of lactate dehydrogenase. Numéro de priorité ; Déposé (14/10/2024). European Patent Office.

http://hdl.handle.net/2078.1/292736

Sonveaux, Pierre ; Thabault, Léopold ; Liberelle, Maxime ; Frédérick, Raphaël. Polypeptide inhibitors of lactate dehydrogenase activity for use in cancer therapy. Déposé. .

http://hdl.handle.net/2078.1/243464

Frédérick, Raphaël ; Thabault, Léopold ; Brisson, Lucie ; Copetti, Tamara ; Sonveaux, Pierre. Lactate dehydrogenase inhibitor polypeptides for use in treatment of cancer. .

http://hdl.handle.net/2078.1/217639

Sonveaux, Pierre ; Labar, Daniel ; Van Hee, Vincent F ; Dehon, Gwenaël ; Frédérick, Raphaël. [18F]-labelled lactate derivative as PET radiotracer. Numéro de priorité ; Déposé (09/09/2016) ; Publié (31/12/2018). EU.

http://hdl.handle.net/2078.1/176821

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

Feledziak, Marion ; Michaux, Catherine ; Lambert, Didier ; Marchand-Brynaert, Jacqueline. An unprecedented reversible mode of action of β-lactams for the inhibition of human fatty acid amide hydrolase (hFAAH). In: European Journal of Medicinal Chemistry, Vol. 60, p. 101-111 (2013). doi:10.1016/j.ejmech.2012.11.035.

http://hdl.handle.net/2078.1/134736

Kapanda Nankwa, Coco ; Poupaert, Jacques ; Lambert, Didier. Insight into the medicinal chemistry of the endocannabinoid hydrolase inhibitors.. In: Current Medicinal Chemistry, Vol. 20, no.14, p. 1824-1846 (2013). doi:10.2174/09298673113209990108.

http://hdl.handle.net/2078.1/134654

Bosier, Barbara ; Muccioli, Giulio ; Lambert, Didier. The FAAH inhibitor URB597 efficiently reduces tyrosine hydroxylase expression through CB(1) and FAAH-independent mechanisms. In: British Journal of Pharmacology, Vol. 169, no. 4, p. 794-807 (2013). doi:10.1111/j.1476-5381.2012.02208.x.

http://hdl.handle.net/2078.1/119601

El Bakali, Jamal ; Gilleron, Pauline ; Body-Malapel, Mathilde ; Mansouri, Roxane ; Muccioli, Giulio ; Djouina, Madjid ; Barczyk, Amélie ; Klupsch, Frédérique ; Andrzejak, Virginie ; Lipka, Emmanuelle ; Furman, Christophe ; Lambert, Didier ; Chavatte, Philippe ; Desreumaux, Pierre ; Millet, Régis. 4-Oxo-1,4-dihydropyridines as selective CB₂ cannabinoid receptor ligands. Part 2: discovery of new agonists endowed with protective effect against experimental colitis. In: Journal of Medicinal Chemistry, Vol. 55, no. 20, p. 8948-8952 (2012). doi:10.1021/jm3008568.

http://hdl.handle.net/2078.1/141066

Morera, Ludovica ; Labar, Geoffray ; Ortar, Giorgio ; Lambert, Didier. Development and characterization of endocannabinoid hydrolases FAAH and MAGL inhibitors bearing a benzotriazol-1-yl carboxamide scaffold. In: Bioorganic & Medicinal Chemistry : the tetrahedron journal for research at the interface of chemistry and biology, Vol. 20, no. 21, p. 6260-6275 (2012). doi:10.1016/j.bmc.2012.09.011.

http://hdl.handle.net/2078.1/161142

Hamtiaux, Laurie ; Masquelier, Julien ; Muccioli, Giulio ; Bouzin, Caroline ; Feron, Olivier ; Gallez, Bernard ; Lambert, Didier. The association of N-palmitoylethanolamine with the FAAH inhibitor URB597 impairs melanoma growth through a supra-additive action. In: BMC Cancer, Vol. 12, p. 92 [1-12] (2012). doi:10.1186/1471-2407-12-92.

http://hdl.handle.net/2078/119829

Vandeputte, Caroline ; Evens, Nele ; Toelen, Jaan ; Deroose, Christophe M ; Bosier, Barbara ; Ibrahimi, Abdelilah ; Van der Perren, Anke ; Gijsbers, Rik ; Janssen, Peter ; Lambert, Didier ; Verbruggen, Alfons ; Debyser, Zeger ; Bormans, Guy ; Baekelandt, Veerle ; Van Laere, Koen. A PET brain reporter gene system based on type 2 cannabinoid receptors. In: Journal of Nuclear Medicine, Vol. 52, no. 7, p. 1102-1109 (2011). doi:10.2967/jnumed.110.084426.

http://hdl.handle.net/2078.1/105226

Matuszak, Nicolas ; Es Saadi, Bouazza ; Labar, Geoffray ; Marchand-Brynaert, Jacqueline ; Lambert, Didier. Benzisothiazolinone as a useful template for the design of new monoacylglycerol lipase inhibitors : investigation of the target residues and comparison with octhilinone. In: Bioorganic & Medicinal Chemistry Letters : the tetrahedron journal for research at the interface of chemistry and biology, Vol. 21, no. 24, p. 7321-4 (2011). doi:10.1016/j.bmcl.2011.10.026.

http://hdl.handle.net/2078.1/105985

Guenadil, Faouzi ; Aichaoui, Hocine ; Kapanda Nankwa, Coco ; Lambert, Didier ; McCurdy, Christopher R. ; Poupaert, Jacques. Design and synthesis of 3-acyl-2(3H)-benzoxazolone and 3-acyl-2(3H)-benzothiazolone derivatives. In: Monatshefte für Chemie, Vol. 142, no. 1, p. 67-80 (2011). doi:10.1007/s00706-010-0419-9.

http://hdl.handle.net/2078.1/106174

Hamtiaux, Laurie ; Hansoulle, Laurie ; Dauguet, Nicolas ; Muccioli, Giulio ; Gallez, Bernard ; Lambert, Didier. Increasing antiproliferative properties of endocannabinoids in N1E-115 neuroblastoma cells through inhibition of their metabolism. In: PLoS One, Vol. 6, no. 10, p. [1-14] (2011). doi:10.1371/journal.pone.0026823.

http://hdl.handle.net/2078.1/105968

Al Houayek, Mireille ; Lambert, Didier ; Delzenne, Nathalie M. ; Cani, Patrice D. ; Muccioli, Giulio. Increasing endogenous 2-arachidonoylglycerol levels counteracts colitis and related systemic inflammation. In: The FASEB Journal, Vol. 25, no. 8, p. 2711-2721 (2011). doi:10.1096/fj.10-176602.

http://hdl.handle.net/2078.1/104024

Thabuis, Clémentine ; Destaillats, Frédéric ; Lambert, Didier ; Muccioli, Giulio ; Maillot, Matthieu ; Harach, Touafiq ; Tissot-Favre, Delphine ; Martin, Jean-Charles. Lipid transport function is the main target of oral oleoylethanolamide to reduce adiposity in high-fat-fed mice. In: Journal of Lipid Research, Vol. 52, no. 7, p. 1373-82 (2011). doi:10.1194/jlr.M013391.

http://hdl.handle.net/2078.1/106001

Andrzejak, Virginie ; Muccioli, Giulio ; Body-Malapel, Mathilde ; El Bakali, Jamal ; Djouina, Madjid ; Renault, Nicolas ; Chavatte, Philippe ; Desreumaux, Pierre ; Lambert, Didier ; Millet, Régis. New FAAH inhibitors based on 3-carboxamido-5-aryl-isoxazole scaffold that protect against experimental colitis. In: Bioorganic & Medicinal Chemistry : the tetrahedron journal for research at the interface of chemistry and biology, Vol. 19, no. 12, p. 3777-3786 (2011). doi:10.1016/j.bmc.2011.04.057.

http://hdl.handle.net/2078.1/105699

Feledziak, Marion ; Muccioli, Giulio ; Lambert, Didier ; Marchand-Brynaert, Jacqueline. SAR and LC/MS studies of β-lactamic inhibitors of human fatty acid amide hydrolase (hFAAH) : evidence of a nonhydrolytic process. In: Journal of Medicinal Chemistry, Vol. 54, no. 19, p. 6812-6823 (2011). doi:10.1021/jm200723m.

http://hdl.handle.net/2078.1/105950

Glinma, Bienvenu ; Kpoviessi, D. S. Salomé ; Fatondji, Raymond H. ; Gbaguigi, Fernand A. ; Kapanda Nankwa, Coco ; Bero, Joanne ; Lambert, Didier ; Hannaert, Véronique ; Quetin-Leclercq, Joëlle ; Mandachirou, Mansourou ; Poupaert, Jacques ; Accrombessi, Gearges C.. Synthesis, characterization and anti-trypanosomal activity of R-(-)carvone and arylketones-thiosemi carbazones and toxicity against Artemia salina Leach. In: Journal of Applied Pharmaceutical Science, Vol. 1, no. 8, p. 65-70 (2011).

http://hdl.handle.net/2078.1/106168

Evens, Nele ; Vandeputte, Caroline ; Muccioli, Giulio ; Lambert, Didier ; Baekelandt, Veerle ; Verbruggen, Alfons M. ; Debyser, Zeger ; Van Laere, Koen ; Bormans, Guy M.. Synthesis, in vitro and in vivo evaluation of fluorine-18 labelled FE-GW405833 as a PET tracer for type 2 cannabinoid receptor imaging. In: Bioorganic & Medicinal Chemistry : the tetrahedron journal for research at the interface of chemistry and biology, Vol. 19, no. 15, p. 4499-4505 (2011). doi:10.1016/j.bmc.2011.06.033.

http://hdl.handle.net/2078.1/105757

El Bakali, Jamal ; Muccioli, Giulio ; Renault, Nicolas ; Pradal, Delphine ; Body-Malapel, Mathilde ; Djouina, Madjid ; Hamtiaux, Laurie ; Andrzejak, Virginie ; Desreumaux, Pierre ; Chavatte, Philippe ; Lambert, Didier ; Millet, Régis. 4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands : structural insights into the design of a novel inverse agonist series.. In: Journal of Medicinal Chemistry, Vol. 53, no. 22, p. 7918-7931 (2010). doi:10.1021/jm100286k.

http://hdl.handle.net/2078.1/106428

Labar, Geoffray ; Wouters, Johan ; Lambert, Didier. A Review on the Monoacylglycerol Lipase : at the Interface between Fat and Endocannabinoid Signalling. In: Current Medicinal Chemistry, Vol. 17, no. 24, p. 2588-2607 (2010). doi:10.2174/092986710791859414.

http://hdl.handle.net/2078.1/32279

De Wael, Frédéric ; Muccioli, Giulio ; Lambert, Didier ; Sergent, Thérèse ; Schneider, Yves-Jacques ; Rees, Jean-François ; Marchand-Brynaert, Jacqueline. Chemistry around imidazopyrazine and ibuprofen : discovery of novel fatty acid amide hydrolase (FAAH) inhibitors. In: European Journal of Medicinal Chemistry, Vol. 45, no. 9, p. 3564-3574 (2010). doi:10.1016/j.ejmech.2010.04.040.

http://hdl.handle.net/2078.1/32578

Labar, Geoffray ; Bauvois, Cédric ; Borel, Franck ; Ferrer, Jean-Luc ; Wouters, Johan ; Lambert, Didier. Crystal Structure of the Human Monoacylglycerol Lipase, a Key Actor in Endocannabinoid Signaling.. In: ChemBioChem, Vol. 11, no. 2, p. 218-227 (2010). doi:10.1002/cbic.200900621.

http://hdl.handle.net/2078.1/28818

Bosier, Barbara ; Muccioli, Giulio ; Hermans, Emmanuel ; Lambert, Didier. Functionally selective cannabinoid receptor signalling : therapeutic implications and opportunities. In: Biochemical Pharmacology, Vol. 80, no. 1, p. 1-12 (2010). doi:10.1016/j.bcp.2010.02.013.

http://hdl.handle.net/2078.1/33886

Gerard, Nathalie ; Ceccarini, Jenny ; Bormans, Guy M. ; Vanbilloen, Bert ; Casteels, Cindy ; Goffin, Karolien ; Bosier, Barbara ; Lambert, Didier ; Van Laere, Koen. Influence of Chronic Nicotine Administration on Cerebral Type 1 Cannabinoid Receptor Binding : an In Vivo Micro-PET Study in the Rat Using [F-18]MK-9470. In: Journal of Molecular Neuroscience, Vol. 42, no. 2, p. 162-7 (2010). doi:10.1007/s12031-010-9340-2.

http://hdl.handle.net/2078.1/33604

Casteels, Cindy ; Vanbilloen, Bert ; Vercammen, Dorien ; Bosier, Barbara ; Lambert, Didier ; Bormans, Guy M. ; Van Laere, Koen. Influence of chronic bromocriptine and levodopa administration on cerebral type 1 cannabinoid receptor binding. In: Synapse (New York), Vol. 64, no. 8, p. 617-623 (2010). doi:10.1002/syn.20769.

http://hdl.handle.net/2078.1/33702

Collard, François ; Stroobant, Vincent ; Lamosa, Pedro ; Kapanda Nankwa, Coco ; Lambert, Didier ; Muccioli, Giulio ; Poupaert, Jacques ; Opperdoes, Frederik ; Van Schaftingen, Emile. Molecular identification of N-acetylaspartylglutamate synthase and beta-citrylglutamate synthase.. In: Journal of Biological Chemistry, Vol. 285, no. 39, p. 29826-29833 (2010). doi:10.1074/jbc.M110.152629.

http://hdl.handle.net/2078.1/33133

Wyffels, Leonie ; Muccioli, Giulio ; Kapanda Nankwa, Coco ; Labar, Geoffray ; De Bruyne, Sylvie ; De Vos, Filip ; Lambert, Didier. PET imaging of fatty acid amide hydrolase in the brain : synthesis and biological evaluation of an C-11-labelled URB597 analogue. In: Nuclear Medicine and Biology, Vol. 37, no. 5, p. 665-75 (2010). doi:10.1016/j.nucmedbio.2010.03.009.

http://hdl.handle.net/2078.1/33726

Bosier, Barbara ; Sarre, Sophie ; Smolders, Ilse ; Michotte, Yvette ; Hermans, Emmanuel ; Lambert, Didier. Revisiting the complex influences of cannabinoids on motor functions unravels pharmacodynamic differences between cannabinoid agonists.. In: Neuropharmacology, Vol. 59, no. 6, p. 503-510 (2010). doi:10.1016/j.neuropharm.2010.07.005.

http://hdl.handle.net/2078.1/32837

Braun, Julie ; Boittiaux, Irving ; Tilborg, Anaëlle ; Lambert, Didier ; Wouters, Johan. The dicyclohexylamine salt of RG108 (N-phthalyl-L-tryptophan), a potential epigenetic modulator. In: Acta crystallographica. Section E, Structure reports online, Vol. E66, no. Part 12, p. o3175-o3176 (2010). doi:10.1107/S160053681004626X.

http://hdl.handle.net/2078.1/106425

Muccioli, Giulio ; Naslain, Damien ; Bäckhed, Fredrik ; Reigstad, Christopher S. ; Lambert, Didier ; Delzenne, Nathalie M. ; Cani, Patrice D.. The endocannabinoid system links gut microbiota to adipogenesis. In: Molecular Systems Biology, Vol. 6, p. 392 [1-15] (2010). doi:10.1038/msb.2010.46.

http://hdl.handle.net/2078.1/33126

Feledziak, Marion ; Michaux, Catherine ; Urbach, Allan ; Labar, Geoffray ; Muccioli, Giulio ; Lambert, Didier ; Marchand-Brynaert, Jacqueline. Beta-lactams derived from a carbapenem chiron are selective inhibitors of human fatty acid amide hydrolase versus human monoacylglycerol lipase. In: Journal of Medicinal Chemistry, Vol. 52, no. 22, p. 7054-7068 (2009). doi:10.1021/jm9008532.

http://hdl.handle.net/2078.1/28546

Kapanda, Coco N. ; Muccioli, Giulio ; Labar, Geoffray ; Poupaert, Jacques ; Lambert, Didier. Bis(dialkylaminethiocarbonyl)disulfides as Potent and Selective Monoglyceride Lipase Inhibitors. In: Journal of Medicinal Chemistry, Vol. 52, no. 22, p. 7310-7314 (2009). doi:10.1021/jm901323s.

http://hdl.handle.net/2078.1/28544

Cani, Patrice D. ; Possemiers, S. ; Van de Wiele, T. ; Guiot, Yves ; Everard, Amandine ; Rottier, O. ; Geurts, Lucie ; Naslain, Damien ; Neyrinck, Audrey M. ; Lambert, Didier ; Muccioli, Giulio ; Delzenne, Nathalie M.. Changes in gut microbiota control inflammation in obese mice through a mechanism involving GLP-2-driven improvement of gut permeability. In: Gut, Vol. 58, no. 8, p. 1091-1103 (2009). doi:10.1136/gut.2008.165886.

http://hdl.handle.net/2078.1/27380

Bosier, Barbara ; Hermans, Emmanuel ; Lambert, Didier. Concomitant activation of adenylyl cyclase suppresses the opposite influences of CB(1) cannabinoid receptor agonists on tyrosine hydroxylase expression.. In: Biochemical Pharmacology, Vol. 77, no. 2, p. 216-227 (2009). doi:10.1016/j.bcp.2008.10.010.

http://hdl.handle.net/2078.1/19695

Wyffels, Leonie ; De Bruyne, Sylvie ; Blanckaert, Peter ; Lambert, Didier ; De Vos, Filip. Radiosynthesis, in vitro and in vivo evaluation of I-123-labeled anandamide analogues for mapping brain FAAH. In: Bioorganic & Medicinal Chemistry : the tetrahedron journal for research at the interface of chemistry and biology, Vol. 17, no. 1, p. 49-56 (2009). doi:10.1016/j.bmc.2008.11.019.

http://hdl.handle.net/2078.1/35944

Kapanda Nankwa, Coco ; Muccioli, Giulio ; Labar, Geoffray ; Draoui, Nihed ; Lambert, Didier ; Poupaert, Jacques. Search for monoglyceride lipase inhibitors : synthesis and screening of arylthioamides derivatives. In: Medicinal Chemistry Research, Vol. 18, no. 4, p. 243-254 (2009). doi:10.1007/s00044-008-9123-2.

http://hdl.handle.net/2078.1/35613

Evens, Nele ; Muccioli, Giulio ; Houbrechts, Nele ; Lambert, Didier ; Verbruggen, Alfons M. ; Van Laere, Koen ; Bormans, Guy M.. Synthesis and biological evaluation of carbon-11-and fluorine-18-labeled 2-oxoquinoline derivatives for type 2 cannabinoid receptor positron emission tomography imaging. In: Nuclear Medicine and Biology, Vol. 36, no. 4, p. 455-465 (2009). doi:10.1016/j.nucmedbio.2009.01.009.

http://hdl.handle.net/2078.1/35555

Matuszak, Nicolas ; Muccioli, Giulio ; Labar, Geoffray ; Lambert, Didier. Synthesis and in vitro evaluation of N-substituted maleimide derivatives as selective monoglyceride lipase inhibitors. In: Journal of Medicinal Chemistry, Vol. 52, no. 23, p. 7410-7420 (2009). doi:10.1021/jm900461w.

http://hdl.handle.net/2078.1/22828

Aichaoui, Hocine ; Guenadil, Faouzi ; Kapanda Nankwa, Coco ; Lambert, Didier ; McCurdy, Christopher R. ; Poupaert, Jacques. Synthesis and pharmacological evaluation of antioxidant chalcone derivatives of 2(3H)-benzoxazolones. In: Medicinal Chemistry Research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, Vol. 18, no. 6, p. 467-476 (2009). doi:10.1007/s00044-008-9143-y.

http://hdl.handle.net/2078.1/35514

Wyffels, Leonie ; Muccioli, Giulio ; De Bruyne, Sylvie ; Moerman, Lieselotte ; Sambre, Johan ; Lambert, Didier ; De Vos, Filip. Synthesis, in vitro and in vivo evaluation, and radiolabeling of aryl anandamide analogues as candidate radioligands for in vivo imaging of fatty acid amide hydrolase in the brain. In: Journal of Medicinal Chemistry, Vol. 52, no. 15, p. 4613-4622 (2009). doi:10.1021/jm900324e.

http://hdl.handle.net/2078.1/35421

Urbach, Allan ; Muccioli, Giulio ; Stern, Eric ; Lambert, Didier ; Marchand-Brynaert, Jacqueline. 3-Alkenyl-2-azetidinones as fatty acid amide hydrolase inhibitors.. In: Bioorganic & Medicinal Chemistry Letters, Vol. 18, no. 14, p. 4163-4167 (2008). doi:10.1016/j.bmcl.2008.05.081.

http://hdl.handle.net/2078.1/12696

Labar, Geoffray ; Vliet, Françoise V. ; Wouters, Johan ; Lambert, Didier. A MBP-FAAH fusion protein as a tool to produce human and rat fatty acid amide hydrolase : expression and pharmacological comparison. In: Amino Acids, Vol. 34, no. 1, p. 127-133 (2008). doi:10.1007/s00726-007-0540-1.

http://hdl.handle.net/2078.1/10953

Goffin, Karolien ; Bormans, Guy M. ; Casteels, Cindy ; Bosier, Barbara ; Lambert, Didier ; Grachev, Igor D. ; Van Paesschen, Wim ; Van Laere, Koen. An in vivo [F-18]MK-9470 microPET study of type 1 cannabinoid receptor binding in Wistar rats after chronic administration of valproate and levetiracetam. In: Neuropharmacology, Vol. 54, no. 7, p. 1103-6 (2008). doi:10.1016/j.neuropharm.2008.02.018.

http://hdl.handle.net/2078.1/36548

Muccioli, Giulio ; Labar, Geoffray ; Lambert, Didier. CAY10499, a novel monoglyceride lipase inhibitor evidenced by an expeditious MGL assay. In: ChemBioChem : a European journal of chemical biology, Vol. 9, no. 16, p. 2704-2710 (2008). doi:10.1002/cbic.200800428.

http://hdl.handle.net/2078.1/19641

Bosier, Barbara ; Hermans, Emmanuel ; Lambert, Didier. Differential modulation of AP-1- and CRE-driven transcription by cannabinoid agonists emphasizes functional selectivity at the CB(1) receptor. In: British Journal of Pharmacology, Vol. 155, no. 1, p. 24-33 (2008). doi:10.1038/bjp.2008.230.

http://hdl.handle.net/2078.1/12700

Guenadil, Faouzi ; Aichaoui, Hocine ; Lambert, Didier ; McCurdy, Christopher R. ; Poupaert, Jacques. Highly Selective Catalytic Friedel-Crafts Acylation of Activated Aromatic Compounds Using the I-2.DMF Complex as Catalyst. In: Letters in Organic Chemistry, Vol. 5, no. 8, p. 665-668 (2008). doi:10.2174/157017808786857624.

http://hdl.handle.net/2078.1/35919

Evens, Nele ; Bosier, Barbara ; Lavey, Brian J. ; Kozlowski, Joseph A. ; Vermaelen, Peter ; Baudemprez, Luc ; Busson, Roger ; Lambert, Didier ; Van Laere, Koen ; Verbruggen, Alfons M. ; Bormans, Guy M.. Labelling and biological evaluation of [C-11]methoxy-Sch225336 : a radioligand for the cannabinoide-type 2 receptor. In: Nuclear Medicine and Biology, Vol. 35, no. 7, p. 793-800 (2008). doi:10.1016/j.nucmedbio.2008.07.004.

http://hdl.handle.net/2078.1/36299

Gallienne, Estelle ; Muccioli, Giulio ; Lambert, Didier ; Shipman, Michael. Microwave-assisted four-component reaction for the synthesis of a monothiohydantoin inhibitor of a fatty acid amide hydrolase. In: Tetrahedron Letters, Vol. 49, no. 46, p. 6495-6497 (2008). doi:10.1016/j.tetlet.2008.08.100.

http://hdl.handle.net/2078.1/37107

Bosier, Barbara ; Lambert, Didier ; Hermans, Emmanuel. Reciprocal influences of CB(1) cannabinoid receptor agonists on ERK and JNK signalling in N1E-115 cells. In: FEBS Letters, Vol. 582, no. 28, p. 3861-3867 (2008). doi:10.1016/j.febslet.2008.10.022.

http://hdl.handle.net/2078.1/19663

Bosier, Barbara ; Tilleux, Sébastien ; Najimi, Mustapha ; Lambert, Didier ; Hermans, Emmanuel. Agonist selective modulation of tyrosine hydroxylase expression by cannabinoid ligands in a murine neuroblastoma cell line.. In: Journal of neurochemistry, Vol. 102, no. 6, p. 1996-2007 (2007). doi:10.1111/j.1471-4159.2007.04679.x.

http://hdl.handle.net/2078.1/10989

Lambert, Didier. Allergic Contact Dermatitis and the Endocannabinoid System: From Mechanisms to Skin Care.. In: ChemMedChem, Vol. 2, no. 12, p. 1701-2 (2007). doi:10.1002/cmdc.200700168.

http://hdl.handle.net/2078.1/11108

Lambert, Didier. CB1 cannabinoid receptor antagonism for treating inflammation and arthritis. In: Expert Opinion on Therapeutic Patents, Vol. 17, no. 8, p. 1027-1031 (2007). doi:10.1517/13543776.17.8.1027.

http://hdl.handle.net/2078.1/37395

Lambert, Didier. Cannabis and endocannabinoids: 'The old man and the teenagers'. In: Chemistry & Biodiversity, Vol. 4, no. 8, p. 1609-1613 (2007). doi:10.1002/cbdv.200790143.

http://hdl.handle.net/2078.1/37356

Labar, Geoffray ; Bauvois, Cedric ; Muccioli, Giulio ; Wouters, Johan ; Lambert, Didier. Disulfiram is an inhibitor of human purified monoacylglycerol lipase, the enzyme regulating 2-arachidonoylglycerol signaling. In: ChemBioChem, Vol. 8, no. 11, p. 1293-1297 (2007). doi:10.1002/cbic.200700139.

http://hdl.handle.net/2078.1/11009

Lambert, Didier ; Muccioli, Giulio. Endocannabinoids and related N-acylethanolamines in the control of appetite and energy metabolism: emergence of new molecular players.. In: Current opinion in clinical nutrition and metabolic care, Vol. 10, no. 6, p. 735-744 (2007). doi:10.1097/MCO.0b013e3282f00061.

http://hdl.handle.net/2078.1/11229

Muccioli, Giulio ; Xu, Cong ; Odah, Emma ; Cudaback, Eiron ; Antonio Cisneros, Jose ; Lambert, Didier ; Lopez Rodriguez, Maria Luz ; Bajjalieh, Sandra ; Stella, Nephi. Identification of a novel endocannabinoid-hydrolyzing enzyme expressed by microglial cells. In: The Journal of Neuroscience, Vol. 27, no. 11, p. 2883-9 (2007). doi:10.1523/JNEUROSCI.4830-06.2007.

http://hdl.handle.net/2078.1/37698

Vandevoorde, Séverine ; Jonsson, Kent-Olov ; Labar, Geoffray ; Persson, Emma ; Lambert, Didier ; Fowler, Christopher J.. Lack of selectivity of URB602 for 2-oleoylglycerol compared to anandamide hydrolysis in vitro.. In: British Journal of Pharmacology, Vol. 150, no. 2, p. 186-91 (2007). doi:10.1038/sj.bjp.0706971.

http://hdl.handle.net/2078.1/106726

Stern, Eric ; Lambert, Didier. Medicinal chemistry endeavors around the phytocannabinoids.. In: Chemistry & biodiversity, Vol. 4, no. 8, p. 1707-28 (2007). doi:10.1002/cbdv.200790149.

http://hdl.handle.net/2078.1/11076

Stern, Eric ; Muccioli, Giulio ; Bosier, Barbara ; Hamtiaux, Laurie ; Millet, Regis ; Poupaert, Jacques ; Henichart, Jean-Pierre ; Depreux, Patrick ; Goossens, Jean-Francois ; Lambert, Didier. Pharmacomodulations around the 4-oxo-1,4-dihydroquinoline-3-carboxamides, a class of potent CB2-selective cannabinoid receptor ligands: Consequences in receptor affinity and functionality. In: Journal of Medicinal Chemistry, Vol. 50, no. 22, p. 5471-84 (2007). doi:10.1021/jm070387h.

http://hdl.handle.net/2078.1/37270

Philip, Ashok E. ; Poupaert, Jacques ; Cheve, Gwenael ; Muccioli, Giulio ; Lambert, Didier ; McCurdy, Christopher R.. Structure-activity relationship of phenytoinergic antiepileptic drugs related to ameltolide. In: Medicinal Chemistry Research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, Vol. 16, no. 3, p. 130-135 (2007). doi:10.1007/s00044-007-9016-9.

http://hdl.handle.net/2078.1/36853

Wallace, V. C. J. ; Segerdahl, A. R. ; Lambert, Didier ; Vandevoorde, Severine ; Blackbeard, J. ; Pheby, T. ; Hasnie, F. ; Rice, A. S. C.. The effect of the palmitoylethanolamide analogue, palmitoylallylamide (L-29) on pain behaviour in rodent models of neuropathy. In: British Journal of Pharmacology, Vol. 151, no. 7, p. 1117-28 (2007). doi:10.1038/sj.bjp.0707326.

http://hdl.handle.net/2078.1/37343

Michaux, Catherine ; Muccioli, Giulio ; Lambert, Didier ; Wouters, Johan. Binding mode of new (thio)hydantoin inhibitors of fatty acid amide hydrolase: comparison with two original compounds, OL-92 and JP104. In: Bioorganic & Medicinal Chemistry Letters : the tetrahedron journal for research at the interface of chemistry and biology, Vol. 16, no. 18, p. 4772-4776 (2006). doi:10.1016/j.bmcl.2006.06.087.

http://hdl.handle.net/2078.1/141075

Muccioli, Giulio ; Lambert, Didier. Latest advances in cannabinoid receptor antagonists and inverse agonists. In: Expert Opinion on Therapeutic Patents, Vol. 16, no. 10, p. 1405-1423 (2006). doi:10.1517/13543776.16.10.1405.

http://hdl.handle.net/2078.1/38222

Stern, Eric ; Muccioli, Giulio ; Millet, R ; Goossens, JF ; Farce, A ; Chavatte, P ; Poupaert, Jacques ; Lambert, Didier ; Depreux, P. ; Hénichart, Jean-Pierre. Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: Synthesis, pharmacological properties and molecular modeling. In: Journal of Medicinal Chemistry, Vol. 49, no. 1, p. 70-79 (2006). doi:10.1021/jm050467q.

http://hdl.handle.net/2078.1/38710

Muccioli, Giulio ; Fazio, Nicola ; Scriba, Gerhard K E ; Poppitz, Wolfgang ; Cannata, Fabio ; Poupaert, Jacques ; Wouters, Johan ; Lambert, Didier. Substituted 2-thioxoimidazolidin-4-ones and imidazolidine-2,4-diones as fatty acid amide hydrolase inhibitors templates.. In: Journal of Medicinal Chemistry, Vol. 49, no. 1, p. 417-425 (2006). doi:10.1021/jm050977k.

http://hdl.handle.net/2078.1/10442

Muccioli, Giulio ; Wouters, Johan ; Charlier, Caroline ; Scriba, Gerhard K E ; Pizza, Teresa ; Di Pace, Pierluigi ; De Martino, Paolo ; Poppitz, Wolfgang ; Poupaert, Jacques ; Lambert, Didier. Synthesis and activity of 1,3,5-triphenylimidazolidine-2,4-diones and 1,3,5-triphenyl-2-thioxoimidazolidin-4-ones: characterization of new CB1 cannabinoid receptor inverse agonists/antagonists.. In: Journal of medicinal chemistry, Vol. 49, no. 3, p. 872-82 (2006). doi:10.1021/jm050484f.

http://hdl.handle.net/2078.1/10469

Muccioli, Giulio ; Wouters, Johan ; Scriba, Gerhard K E ; Poppitz, Wolfgang ; Poupaert, Jacques ; Lambert, Didier. 1-Benzhydryl-3-phenylurea and 1-benzhydryl-3-phenylthiourea derivatives: new templates among the CB1 cannabinoid receptor inverse agonists.. In: Journal of medicinal chemistry, Vol. 48, no. 23, p. 7486-90 (2005). doi:10.1021/jm0503906.

http://hdl.handle.net/2078.1/10384

Muccioli, Giulio ; Lambert, Didier. Current knowledge on the antagonists and inverse agonists of cannabinoid receptors.. In: Current medicinal chemistry, Vol. 12, no. 12, p. 1361-94 (2005). doi:10.2174/0929867054020891.

http://hdl.handle.net/2078.1/10233

Vandevoorde, Severine ; Lambert, Didier. Focus on the three key enzymes hydrolysing endocannabinoids as new drug targets.. In: Current pharmaceutical design, Vol. 11, no. 20, p. 2647-68 (2005). doi:10.2174/1381612054546914.

http://hdl.handle.net/2078.1/10296

Muccioli, Giulio ; Martin, Diana ; Scriba, Gerhard K E ; Poppitz, Wolfgang ; Poupaert, Jacques ; Wouters, Johan ; Lambert, Didier. Substituted 5,5'-diphenyl-2-thioxoimidazolidin-4-one as CB1 cannabinoid receptor ligands: synthesis and pharmacological evaluation.. In: Journal of medicinal chemistry, Vol. 48, no. 7, p. 2509-17 (2005). doi:10.1021/jm049263k.

http://hdl.handle.net/2078.1/10150

Lambert, Didier ; Fowler, Christopher J. The endocannabinoid system: drug targets, lead compounds, and potential therapeutic applications.. In: Journal of medicinal chemistry, Vol. 48, no. 16, p. 5059-5087 (2005). doi:10.1021/jm058183t.

http://hdl.handle.net/2078.1/10279

Govaerts, Sophie ; Muccioli, Giulio ; Hermans, Emmanuel ; Lambert, Didier. Characterization of the pharmacology of imidazolidinedione derivatives at cannabinoid CB1 and CB2 receptors.. In: European Journal of Pharmacology, Vol. 495, no. 1, p. 43-53 (2004). doi:10.1016/j.ejphar.2004.05.023.

http://hdl.handle.net/2078.1/9888

Govaerts, Sophie ; Hermans, Emmanuel ; Lambert, Didier. Comparison of cannabinoid ligands affinities and efficacies in murine tissues and in transfected cells expressing human recombinant cannabinoid receptors.. In: European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, Vol. 23, no. 3, p. 233-43 (2004). doi:10.1016/j.ejps.2004.07.013.

http://hdl.handle.net/2078.1/9999

Vandevoorde, Séverine ; Lambert, Didier. Gros plan sur les endocannabinoïdes, de nouveaux agents thérapeutiques. In: Chimie Nouvelle, , no.87, p. 102-105 (2004).

http://hdl.handle.net/2078.1/239110

Tsuboi, Kazuhito ; Hilligsmann, Christine ; Vandevoorde, Severine ; Lambert, Didier ; Ueda, Natsuo. N-cyclohexanecarbonylpentadecylamine: a selective inhibitor of the acid amidase hydrolysing N-acylethanolamines, as a tool to distinguish acid amidase from fatty acid amide hydrolase. In: Biochemical Journal, Vol. 379, p. 99-106 (2004). doi:10.1042/BJ20031695.

http://hdl.handle.net/2078.1/40248

Cani, Patrice D. ; Montoya, Maite Lasa ; Neyrinck, Audrey M. ; Delzenne, Nathalie M. ; Lambert, Didier. Potential modulation of plasma ghrelin and glucagon-like peptide-1 by anorexigenic cannabinoid compounds, SR141716A (rimonabant) and oleoylethanolamide. In: The British Journal of Nutrition : an international journal of nutritional science, Vol. 92, no. 5, p. 757-761 (2004). doi:10.1079/bjn20041256.

http://hdl.handle.net/2078.1/10020

Muccioli, Giulio ; Poupaert, Jacques ; Wouters, Johan ; Norberg, Bernadette ; Poppitz, Wolfgang ; Scriba, Gerhard K. E. ; Lambert, Didier. A rapid and efficient microwave-assisted synthesis of hydantoins and thiohydantoins. In: Tetrahedron, Vol. 59, no. 8, p. 1301-1307 (2003). doi:10.1016/S0040-4020(03)00033-4.

http://hdl.handle.net/2078.1/41451

Jonsson, Kent-Olov ; Andersson, Anna ; Jacobsson, Stig O.P. ; Vandevoorde, Séverine ; Lambert, Didier ; Fowler, Christopher J.. AM404 and VDM 11 non-specifically inhibit C6 glioma cell proliferation at concentrations used to block the cellular accumulation of the endocannabinoid anandamide. In: Archives of Toxicology, Vol. 77, no. 4, p. 201-207 (2003). doi:10.1007/s00204-002-0435-6.

http://hdl.handle.net/2078.1/41003

Vandevoorde, Severine ; Tsuboi, Kazuhito ; Ueda, Natsuo ; Jonsson, Kent-Olov ; Fowler, Christopher J ; Lambert, Didier. Esters, retroesters, and a retroamide of palmitic acid: pool for the first selective inhibitors of N-palmitoylethanolamine-selective acid amidase.. In: Journal of medicinal chemistry, Vol. 46, no. 21, p. 4373-6 (2003). doi:10.1021/jm0340795.

http://hdl.handle.net/2078.1/9637

Fowler, Christophe J. ; Jonsson, Kent-Olov ; Andersson, Anna ; Juntunen, Juha ; Jarvinen, Tomi ; Vandevoorde, Severine ; Lambert, Didier ; Jerman, Jerman C. ; Smart, Darren. Inhibition of C6 glioma cell proliferation by anandamide, 1-arachidonoylglycerol, and by a water soluble phosphate ester of anandamide: variability in response and involvement of arachidonic acid. In: Biochemical Pharmacology, Vol. 66, no. 5, p. 757-767 (2003). doi:10.1016/S0006-2952(03)00392-7.

http://hdl.handle.net/2078.1/40799

Vandevoorde, Severine ; Jonsson, Kent-Olov ; Fowler, Christopher J. ; Lambert, Didier. Modifications of the ethanolamine head in N-palmitoylethanolamine: synthesis and evaluation of new agents interfering with the metabolism of anandamide. In: Journal of Medicinal Chemistry, Vol. 46, no. 8, p. 1440-1448 (2003). doi:10.1021/jm0209679.

http://hdl.handle.net/2078.1/9421

Vandevoorde, Severine ; Lambert, Didier ; Smart, Darren ; Jonsson, Kent Olov ; Fowler, Christopher J. N-Morpholino- and N-diethyl-analogues of palmitoylethanolamide increase the sensitivity of transfected human vanilloid receptors to activation by anandamide without affecting fatty acid amidohydrolase activity.. In: Bioorganic & medicinal chemistry, Vol. 11, no. 6, p. 817-25 (2003). doi:10.1016/S0968-0896(02)00567-9.

http://hdl.handle.net/2078.1/9389

Muccioli, Giulio ; Wouters, Johan ; Poupaert, Jacques ; Norberg, Bernadette ; Poppitz, Wolfgang ; Scriba, Gerhard K E ; Lambert, Didier. Versatile access to benzhydryl-phenylureas through an unexpected rearrangement during microwave-enhanced synthesis of hydantoins.. In: Organic letters, Vol. 5, no. 20, p. 3599-602 (2003). doi:10.1021/ol035282x.

http://hdl.handle.net/2078.1/9632

Wouters, J ; Vandevoorde, S ; Culot, C ; Docquir, F ; Lambert, Didier. Polymorphism of N-stearoylethanolamine: differential scanning calorimetric, vibrational spectroscopic (FTIR), and crystallographic studies.. In: Chemistry and physics of lipids, Vol. 119, no.1-2, p. 13-21 (2002). doi:10.1016/s0009-3084(02)00031-2.

http://hdl.handle.net/2078.1/236477

Fuzfa, A. ; Gérard, Jean-Marc ; Lambert, Didier. The Lemaitre-Schwarzschild problem revisited. In: Gen.Rel.Grav., Vol. 34, p. 1411-1422 (2002). doi:10.1023/A:1020030919033.

http://hdl.handle.net/2078/30809

Lambert, Didier ; Vandevoorde, Severine ; Diependaele, G ; Govaerts, Sophie ; Robert, Annie. Anticonvulsant activity of N-palmitoylethanolamide, a putative endocannabinoid, in mice.. In: Epilepsia, Vol. 42, no. 3, p. 321-327 (2001). doi:10.1046/j.1528-1157.2001.41499.x.

http://hdl.handle.net/2078.1/8879

Lambert, Didier. Les vertus thérapeutiques du Cannabis à travers les millénaires.. In: Journal de pharmacie de Belgique, Vol. 56, no. 5, p. 111-8 (2001).

http://hdl.handle.net/2078.1/9025

Ngakeu, F. ; Majid, S. ; Lambert, Didier. Noncommutative Riemannian geometry of the alternating group A(4). In: Journal of Geometry and Physics, Vol. 42, no. 3, p. 259-282 (2002). doi:10.1016/S0393-0440(01)00089-4.

http://hdl.handle.net/2078/30789

Lambert, Didier. Rationale and applications of lipids as prodrug carriers.. In: European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, Vol. 11 Suppl 2, p. S15-27 (2000). doi:10.1016/S0928-0987(00)00161-5.

http://hdl.handle.net/2078.1/8659

Kanyonyo, M ; Govaerts, Sophie ; Hermans, Emmanuel ; Poupaert, Jacques ; Lambert, Didier. 3-Alkyl-(5,5'-diphenyl)imidazolidineiones as new cannabinoid receptor ligands.. In: Bioorganic & medicinal chemistry letters, Vol. 9, no. 15, p. 2233-6 (1999). doi:10.1016/S0960-894X(99)00353-4.

http://hdl.handle.net/2078.1/8345

Lambert, Didier ; DiPaolo, Federica G. ; Sonveaux, Pierre ; Kanyonyo, Martial ; Govaerts, Sophie ; Hermans, Emmanuel ; Bueb, Jean-Luc ; Delzenne, Nathalie M. ; Tschirhart, Eric J.. Analogues and homologues of N-palmitoylethanolamide, a putative endogenous CB(2) cannabinoid, as potential ligands for the cannabinoid receptors. In: Biochimica et Biophysica Acta : international journal of biochemistry and biophysics, Vol. 1440, no. 2-3, p. 266-274 (1999). doi:10.1016/s1388-1981(99)00132-8.

http://hdl.handle.net/2078.1/8373

Lambert, Didier. New trends in cannabinoid receptor ligands - Preface. In: Current Medicinal Chemistry, Vol. 6, no. 8, p. U2-U2 (1999).

http://hdl.handle.net/2078.1/44250

Lambert, Didier ; Di Marzo, V. The palmitoylethanolamide and oleamide enigmas : are these two fatty acid amides cannabimimetic?. In: Current medicinal chemistry, Vol. 6, no. 8, p. 757-73 (1999).

http://hdl.handle.net/2078.1/8346

Vamecq, J. ; Lambert, Didier ; Poupaert, Jacques ; Masereel, Bernard ; Stables, JP.. Anticonvulsant activity and interactions with neuronal voltage-dependent sodium channel of analogues of ameltolide. In: Journal of Medicinal Chemistry, Vol. 41, no. 18, p. 3307-13 (1998). doi:10.1021/jm9608772.

http://hdl.handle.net/2078.1/45110

Kanyonyo, M R ; Poupaert, Jacques ; Lambert, Didier. Anticonvulsant profile of 4-amino-(2-methyl-4-aminophenyl)benzamide in mice and rats.. In: Pharmacology & toxicology, Vol. 82, no. 1, p. 47-50 (1998). doi:10.1111/j.1600-0773.1998.tb01397.x.

http://hdl.handle.net/2078.1/24218

Gallez, Bernard ; Lambert, Didier. Checking the integrity of albumin after pasteurisation: a fluorescent assay for quantitating monomeric albumin using anthroyloxy-fatty acids analogs.. In: Journal of biochemical and biophysical methods, Vol. 37, no. 1-2, p. 5-9 (1998). doi:10.1016/S0165-022X(98)00009-8.

http://hdl.handle.net/2078.1/24172

Geurts, M ; Poupaert, Jacques ; Scriba, G K ; Lambert, Didier. N-(benzyloxycarbonyl)glycine esters and amides as new anticonvulsants.. In: Journal of medicinal chemistry, Vol. 41, no. 1, p. 24-30 (1998). doi:10.1021/jm970086f.

http://hdl.handle.net/2078.1/24235

Lambert, Didier ; Masereel, Bernard ; Gallez, Bernard ; Geurts, Muriel ; Scriba, Gerhard K. E.. Bioavailability and anticonvulsant activity of 2-cyanoguanidinophenytoin, a structural analogue of phenytoin. In: Journal of Pharmaceutical Sciences, Vol. 85, no. 10, p. 1077-1081 (1996). doi:10.1021/js960093b.

http://hdl.handle.net/2078.1/24316

Lambert, Didier ; Gallez, Bernard. Synthesis and distribution of tritiated N,N'-dibenzoyl-1,3-diaminopropan-2-ol. In: Journal of Labelled Compounds and Radiopharmaceuticals, Vol. 38, no. 10, p. 897-905 (1996). doi:10.1002/(SICI)1099-1344(199610)38:10<897::AID-JLCR916>3.0.CO;2-D.

http://hdl.handle.net/2078.1/46872

Ucar, H ; Vanderpoorten, K ; Kanyonyo, M ; Isa, M. ; Lambert, Didier ; Lesieur, D. ; Poupaert, Jacques. Synthesis of 6-benzoyl-2(3H)-benzoxazolone and 6-benzoyl-2(3H)-benzothiazolone. In: Societes Chimiques Belges. Bulletin, Vol. 105, no. 12, p. 773-776 (1996).

http://hdl.handle.net/2078.1/46586

Charbon, Vinciane ; Latour, Isabelle ; Lambert, Didier ; Buc Calderon, Pedro ; Neuvens, Laurence ; De Keyser, Jean-Luc ; Gallez, Bernard. Targeting of drug to the hepatocytes by fatty acids. Influence of the carrier (albumin or galactosylated albumin) on the fate of the fatty acids and their analogs. In: Pharmaceutical Research, Vol. 13, no. 1, p. 27-31 (1996). doi:10.1023/A:1016012913664.

http://hdl.handle.net/2078.1/24368

Gallez, Bernard ; Baudelet, Christine ; Adline, Jacques ; Charbon, Vinciane ; Lambert, Didier. The uptake of Mn-DPDP by hepatocytes is not mediated by the facilitated transport of pyridoxine. In: Magnetic Resonance Imaging, Vol. 14, no. 10, p. 1191-1195 (1996). doi:10.1016/S0730-725X(96)00140-3.

http://hdl.handle.net/2078.1/13292

Dupont, L. ; Masereel, Bernard ; Lambert, Didier ; Scriba, G.. 2-cyanoimino-5,5-diphenyl-4-imidazolinon Monohydrate. In: Acta Crystallographica. Section C: Crystal Structure Communications, Vol. 51, p. 1901-1903 (1995). doi:10.1107/S0108270195001661.

http://hdl.handle.net/2078.1/47774

Poupaert, Jacques ; Hamoir, G. ; Barbeaux, P. ; Lambert, Didier ; Hénichart, Jean-Pierre. Anticonvulsant Activity of Some N-phenylphthalimide Derivatives in Rats and Mice. In: Journal of Pharmacy and Pharmacology : an international journal of pharmaceutical science, Vol. 47, no. 1, p. 89-91 (1995).

http://hdl.handle.net/2078.1/48213

Lambert, Didier ; Geurts, M ; Scriba, G K ; Poupaert, Jacques ; Dumont, Pierre. Dérivés simples d'acides aminés neurotransmetteurs. Evaluation anticonvulsivante de dérivés amides, carbamates et esters de la glycine et de la beta-alanine.. In: Journal de pharmacie de Belgique, Vol. 50, no. 2-3, p. 194-203 (1995).

http://hdl.handle.net/2078.1/11883

Lambert, Didier ; Mergen, F. ; Berens, C F ; Poupaert, Jacques ; Dumont, Pierre. Synthesis and pharmacological properties of 2-[S-acetylthiorphan]-1,3- diacylaminopropan-2-ol derivatives as chimeric lipid drug carriers containing an enkephalinase inhibitor.. In: Pharmaceutical research, Vol. 12, no. 2, p. 187-91 (1995). doi:10.1023/A:1016214506667.

http://hdl.handle.net/2078.1/24441

Lambert, Didier ; Poupaert, Jacques ; Maloteaux, Jean-Marie ; Dumont, Pierre. Anticonvulsant activities of N-benzyloxycarbonylglycine after parenteral administration.. In: Neuroreport, Vol. 5, no. 7, p. 777-80 (1994). doi:10.1097/00001756-199403000-00010.

http://hdl.handle.net/2078.1/24577

Lambert, Didier ; Neuvens, L ; Mergen, F. ; Gallez, Bernard ; Poupaert, Jacques ; Ghysel-Burton, J ; Maloteaux, Jean-Marie ; Dumont, Pierre. 1,3-Diacylaminopropan-2-ols and corresponding 2-acyl derivatives as drug carriers: unexpected pharmacological properties.. In: The Journal of pharmacy and pharmacology, Vol. 45, no. 3, p. 186-91 (1993).

http://hdl.handle.net/2078.1/24631

Lambert, Didier ; Mergen, F. ; Poupaert, Jacques ; Dumont, Pierre. Analgesic potency of S-acetylthiorphan after intravenous administration to mice.. In: European journal of pharmacology, Vol. 243, no. 2, p. 129-34 (1993). doi:10.1016/0014-2999(93)90371-N.

http://hdl.handle.net/2078.1/24605

Vamecq, J. ; Vallee, L. ; Fontaine, M. ; Lambert, Didier ; Poupaert, Jacques ; Nuyts, JP.. Coa Esters of Valproic Acid and Related Metabolites Are Oxidized in Peroxisomes Through a Pathway Distinct From Peroxisomal Fatty and Bile Acyl-coa Beta-oxidation. In: FEBS Letters, Vol. 322, no. 2, p. 95-100 (1993). doi:10.1016/0014-5793(93)81545-B.

http://hdl.handle.net/2078.1/49751

Vamecq, J. ; Vallee, L. ; Fontaine, M. ; Nuyts, JP. ; Lambert, Didier ; Poupaert, Jacques. Preliminary Studies About Novel Strategies To Reverse Chemoresistance To Adriamycin Regarding Glutathione Metabolism, Peroxisomal and Extraperoxisomal Hydroperoxide and Valproic Acid Metabolic Pathways. In: Biology of the Cell, Vol. 77, no. 1, p. 17-26 (1993). doi:10.1016/S0248-4900(05)80170-4.

http://hdl.handle.net/2078.1/49752

Mergen, F. ; Lambert, Didier ; Poupaert, Jacques ; Bidaine, A ; Dumont, Pierre. Synthesis of 1,3-diacylaminopropan-2-ols and corresponding 2-acyl derivatives as amide isosteres of natural lipids.. In: Chemistry and physics of lipids, Vol. 59, no. 3, p. 267-72 (1991). doi:10.1016/0009-3084(91)90027-9.

http://hdl.handle.net/2078.1/24708

Poupaert, Jacques ; Hermans, Emmanuel ; Jonckheere, Y. ; Mergen, F. ; Lambert, Didier ; Lerot, T. ; Aandrianjara, R. ; Poupaert, EJ. ; Lybrand, T. ; Durant, F.. Synthesis and Pharmacological Evaluation of the Anticonvulsant Activity of Bivalent Ligands Derived From 4-amino-2',6'-dimethylbenzanilide. In: Asia Pacific Journal of Pharmacology, Vol. 5, no. 3, p. 249-251 (1990).

http://hdl.handle.net/2078.1/51567

Bosier, Barbara ; Lambert, Didier. The Endocannabinoid System at a Glance. In: Didier M. Lambert, Cannabinoids in Nature and Medicine, Helvitica Chimica Acta Verlag: (Switzerlands) Zurich, 2009, 1-14. 978-3-906390-56-7.

http://hdl.handle.net/2078.1/105230

Van Bambeke, Françoise ; Lambert, Didier ; Mingeot-Leclercq, Marie-Paule ; Tulkens, Paul M.. Anti-infective therapy: mechanisms of action. In: D. Armstrong and J. Cohen, Infectious Diseases, Mosby: (United-Kingdom) London, 1999, p. 7.1.1-7.1.14. 0-7234-2328-8.

http://hdl.handle.net/2078.1/114704