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9. Laryngeal Muscle-Evoked Potential Recording as an Indicator of Vagal Nerve Fiber Activation

Author

UCL - SSS/IONS/NEUR - Clinical Neuroscience, UCL - (SLuc) Service de neurologie, Bouckaert, Charlotte, Raedt, Robrecht, Larsen, Lars Emil, El Tahry, Riëm, Gadeyne, Stefanie, Carrette, Evelien, Proesmans, Silke, Dewaele, Frank, Delbeke, Jean, De Herdt, Veerle, Meurs, Alfred, Mertens, Ann, Boon, Paul, Vonck, Kristl, UCL - SSS/IONS/NEUR - Clinical Neuroscience, UCL - (SLuc) Service de neurologie, Bouckaert, Charlotte, Raedt, Robrecht, Larsen, Lars Emil, El Tahry, Riëm, Gadeyne, Stefanie, Carrette, Evelien, Proesmans, Silke, Dewaele, Frank, Delbeke, Jean, De Herdt, Veerle, Meurs, Alfred, Mertens, Ann, Boon, Paul, and Vonck, Kristl

Abstract

Vagus nerve stimulation (VNS) is an adjunctive therapy for drug-resistant epilepsy. Noninvasive evoked potential recordings in laryngeal muscles (LMEPs) innervated by vagal branches may provide a marker to assess effective vagal nerve fiber activation. We investigated VNS-induced LMEPs in patients with epilepsy in acute and chronic settings.

Published
2022

15. Development of a Rat Model for Glioma-Related Epilepsy

Author

Bouckaert, Charlotte, primary, Germonpré, Charlotte, additional, Verhoeven, Jeroen, additional, Chong, Seon-Ah, additional, Jacquin, Lucas, additional, Mairet-Coello, Georges, additional, André, Véronique Marie, additional, Leclercq, Karine, additional, Vanhove, Christian, additional, De Vos, Filip, additional, Van den Broecke, Caroline, additional, Goethals, Ingeborg, additional, Descamps, Benedicte, additional, Donche, Sam, additional, Carrette, Evelien, additional, Wadman, Wytse, additional, Boon, Paul, additional, Vonck, Kristl, additional, and Raedt, Robrecht, additional

Published
2020
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16. Identification of vagus nerve stimulation parameters affecting rat hippocampal electrophysiology without temperature effects

Author

Van Lysebettens, Wouter, primary, Vonck, Kristl, additional, Larsen, Lars Emil, additional, Stevens, Latoya, additional, Bouckaert, Charlotte, additional, Germonpré, Charlotte, additional, Sprengers, Mathieu, additional, Carrette, Evelien, additional, Delbeke, Jean, additional, Wadman, Wytse Jan, additional, Boon, Paul, additional, and Raedt, Robrecht, additional

Published
2020
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17. Vagus Nerve Stimulation-Induced Laryngeal Motor Evoked Potentials: A Possible Biomarker of Effective Nerve Activation

Author

UCL - SSS/IONS/NEUR - Clinical Neuroscience, UCL - SSS/IONS/CEMO - Pôle Cellulaire et moléculaire, UCL - (SLuc) Service de neurologie, UCL - (SLuc) Service de neurochirurgie, Vespa, Simone, Stumpp, Lars, Bouckaert, Charlotte, Delbeke, Jean, Smets, Hugo, Cury, Joaquin, Ferrao Santos, Susana, Rooijakkers, Herbert, Nonclercq, Antoine, Raedt, Robrecht, Vonck, Kristl, El Tahry, Riëm, UCL - SSS/IONS/NEUR - Clinical Neuroscience, UCL - SSS/IONS/CEMO - Pôle Cellulaire et moléculaire, UCL - (SLuc) Service de neurologie, UCL - (SLuc) Service de neurochirurgie, Vespa, Simone, Stumpp, Lars, Bouckaert, Charlotte, Delbeke, Jean, Smets, Hugo, Cury, Joaquin, Ferrao Santos, Susana, Rooijakkers, Herbert, Nonclercq, Antoine, Raedt, Robrecht, Vonck, Kristl, and El Tahry, Riëm

Abstract

Vagus nerve stimulation (VNS) therapy is associated with laryngeal muscle activation and induces voice modifications, well-known side effects of the therapy resulting from co-activation of the recurrent laryngeal nerve. In this study, we describe the non-invasive transcutaneous recording of laryngeal motor evoked potentials (LMEPs), which could serve as a biomarker of effective nerve activation and individual titration in patients with drug-resistant epilepsy. We recruited drug-resistant epileptic patients treated for at least 6 months with a VNS. Trains of 600–1200 VNS pulses were delivered with increasing current outputs. We placed six skin electrodes on the ventral surface of the neck, in order to record LMEPs whenever the laryngeal muscular threshold was reached. We studied the internal consistency and the variability of LMEP recordings, and compared different methods for amplitude calculation. Recruitment curves were built based on the stimulus–response relationship. We also determined the electrical axis of the LMEPs dipole in order to define the optimal electrode placement for LMEPs recording in a clinical setting. LMEPs were successfully recorded in 11/11 patients. The LMEPs threshold ranged from 0.25 to 1 mA (median 0.50 mA), and onset latency was between 5.37 and 8.77 ms. The signal-to-noise ratio was outstanding in 10/11 patients. In these cases, excellent reliability (Intraclass correlation coefficient, ICC > 0.90 across three different amplitude measurements) was achieved with 10 sample averages. Moreover, our recordings showed very good internal consistency (Cronbach’s alpha > 0.95 for 10 epochs). Area-under-the-curve and peak-to-peak measurement proved to be complementary methods for amplitude calculation. Finally, we determined that an optimal derivation requires only two recording electrodes, aligned on a horizontal axis around the laryngeal prominence. In conclusion, we describe here an optimal methodology for the recording of VNS-induced motor evo

Published
2019

18. Vagus nerve stimulation-induced laryngeal motor evoked potentials: A possible biomarker of effective nerve activation

Author

Vespa, Simone, Stumpp, Lars LS, Bouckaert, Charlotte, Delbeke, Marie Jeanne, Smets, Hugo, Cury, Joaquin, Ferrao Santos, Susana, Rooijakkers, Herbert, Nonclercq, Antoine, Raedt, Robrecht, Vonck, Kristl, El Tahry, Riëm, Vespa, Simone, Stumpp, Lars LS, Bouckaert, Charlotte, Delbeke, Marie Jeanne, Smets, Hugo, Cury, Joaquin, Ferrao Santos, Susana, Rooijakkers, Herbert, Nonclercq, Antoine, Raedt, Robrecht, Vonck, Kristl, and El Tahry, Riëm

Abstract

Vagus nerve stimulation (VNS) therapy is associated with laryngeal muscle activation and induces voice modifications, well-known side effects of the therapy resulting from co-activation of the recurrent laryngeal nerve. In this study, we describe the non-invasive transcutaneous recording of laryngeal motor evoked potentials (LMEPs), which could serve as a biomarker of effective nerve activation and individual titration in patients with drug-resistant epilepsy. We recruited drug-resistant epileptic patients treated for at least 6 months with a VNS. Trains of 600–1200 VNS pulses were delivered with increasing current outputs. We placed six skin electrodes on the ventral surface of the neck, in order to record LMEPs whenever the laryngeal muscular threshold was reached. We studied the internal consistency and the variability of LMEP recordings, and compared different methods for amplitude calculation. Recruitment curves were built based on the stimulus–response relationship. We also determined the electrical axis of the LMEPs dipole in order to define the optimal electrode placement for LMEPs recording in a clinical setting. LMEPs were successfully recorded in 11/11 patients. The LMEPs threshold ranged from 0.25 to 1 mA (median 0.50 mA), and onset latency was between 5.37 and 8.77 ms. The signal-to-noise ratio was outstanding in 10/11 patients. In these cases, excellent reliability (Intraclass correlation coefficient, ICC > 0.90 across three different amplitude measurements) was achieved with 10 sample averages. Moreover, our recordings showed very good internal consistency (Cronbach’s alpha > 0.95 for 10 epochs). Area-under-the-curve and peak-to-peak measurement proved to be complementary methods for amplitude calculation. Finally, we determined that an optimal derivation requires only two recording electrodes, aligned on a horizontal axis around the laryngeal prominence. In conclusion, we describe here an optimal methodology for the recording of VNS-induced motor evo, SCOPUS: ar.j, info:eu-repo/semantics/published

Published
2019

20. Vagus Nerve Stimulation-Induced Laryngeal Motor Evoked Potentials: A Possible Biomarker of Effective Nerve Activation

Author

Vespa, Simone, primary, Stumpp, Lars, additional, Bouckaert, Charlotte, additional, Delbeke, Jean, additional, Smets, Hugo, additional, Cury, Joaquin, additional, Ferrao Santos, Susana, additional, Rooijakkers, Herbert, additional, Nonclercq, Antoine, additional, Raedt, Robrecht, additional, Vonck, Kristl, additional, and El Tahry, Riëm, additional

Published
2019
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21. Evoked hippocampal seizures are associated with bursts of locus coeruleus neuronal activity in the anaesthetized rat: a mechanism of ‘pathological memory formation’ in epilepsy?

Author

Larsen, Lars, primary, Stevens, Latoya, additional, Acharya, Anirudh, additional, Bouckaert, Charlotte, additional, Craey, Erine, additional, Desloovere, Jana, additional, Goossens, Marie-Gabrielle, additional, Germonpré, Charlotte, additional, Proesmans, Silke, additional, Boon, Paul, additional, Vonck, Kristl, additional, Vanhove, Chris, additional, Van Mierlo, Pieter, additional, and Raedt, Robrecht, additional

Published
2019
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22. Enhancing Action of Positive Allosteric Modulators through the Design of Dimeric Compounds

Author

Drapier, Thomas, Geubelle, Pierre, Bouckaert, Charlotte, Nielsen, Lise, Laulumaa, Saara, Goffin, Eric, Dilly, Sébastien, Francotte, Pierre, Hanson, Julien, Pochet, Lionel, Kastrup, Jette Sandholm, Pirotte, Bernard, Drapier, Thomas, Geubelle, Pierre, Bouckaert, Charlotte, Nielsen, Lise, Laulumaa, Saara, Goffin, Eric, Dilly, Sébastien, Francotte, Pierre, Hanson, Julien, Pochet, Lionel, Kastrup, Jette Sandholm, and Pirotte, Bernard

Abstract

The present study describes the identification of highly potent dimeric 1,2,4-benzothiadiazine 1,1-dioxide (BTD)-type positive allosteric modulators of the AMPA receptors (AMPApams) obtained by linking two monomeric BTD scaffolds through their respective 6-positions. Using previous X-ray data from monomeric BTDs cocrystallized with the GluA2 ligand-binding domain (LBD), a molecular modeling approach was performed to predict the preferred dimeric combinations. Two 6,6-ethylene-linked dimeric BTD compounds (16 and 22) were prepared and evaluated as AMPApams on HEK293 cells expressing GluA2o( Q) (calcium flux experiment). These compounds were found to be about 10,000 times more potent than their respective monomers, the most active dimeric compound being the bis-4-cyclopropyl-substituted compound 22 [6,6'-(ethane-1,2-diyl)bis(4-cyclopropyl-3,4-dihydro-2 H-1,2,4-benzothiadiazine 1,1-dioxide], with an EC50 value of 1.4 nM. As a proof of concept, the bis-4-methyl-substituted dimeric compound 16 (EC50 = 13 nM) was successfully cocrystallized with the GluA2o-LBD and was found to occupy the two BTD binding sites at the LBD dimer interface.

Published
2018

23. Enhancing Action of Positive Allosteric Modulators through the Design of Dimeric Compounds

Author

Drapier, Thomas, primary, Geubelle, Pierre, additional, Bouckaert, Charlotte, additional, Nielsen, Lise, additional, Laulumaa, Saara, additional, Goffin, Eric, additional, Dilly, Sébastien, additional, Francotte, Pierre, additional, Hanson, Julien, additional, Pochet, Lionel, additional, Kastrup, Jette Sandholm, additional, and Pirotte, Bernard, additional

Published
2018
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24. 30th Franco-Belgian conference of pharmacochemistry

Author

Bouckaert, Charlotte, Goffin, Eric, Dilly, Sebastien, Hanson, Julien, Pochet, Lionel, Kastrup, Jette Sandholm, Francotte, Pierre, Pirotte, Bernard, Michiels, Carine, Champire, Anthony, Ple, Karen, Robin, Laurent, Suzenet, Franck, Bouyssou, Pascal, Burgy, Guillaume, Limanton, Emmanuelle, Guiheneuf, Solene, Carreaux, Francois, Tahtouh, Tania, Durieu, Emilie, Meijer, Laurent, Pipelier, Muriel, Plenevaux, Alain, Place, Mattieu, Copin, Chloe, Ambeu, Christelle, Coulibaly, Wacothon Karime, Mamyrbekova-Berkro, Janat, Benie, Anoubile, Corlu, Anne, Bach, Stephane, Dago, Camille Deliko, Paquin, Ludovic, Mamyrbekova-Bekro, Janat Akhanovna, Bekro, Yves-Alain, Ruchaud, Sandrine, Le Guevel, Remy, Brigaudeau, Christophe, Mignen, Olivier, Bazureau, Jean-Pierre, Gally, Jose-Manuel, Heinrich, Jean-Thomas, Obled, Alan, Aci-Seche, Samia, Bonnet, Pascal, Gibault, Floriane, Corvaisier, Matthieu, Bailly, Fabrice, Huet, Guillemette, Cotelle, Philippe, Duroux, Romain, Renault, Nicolas, Agouridas, Laurence, Lopes, Luisa, Melnyk, Patricia, Yous, Said, Piguel, Sandrine, Stutzmann, Aurelien, Schnetterle, Marine, Caclard, Arnaud, Biot, Fabrice, Valade, Eric, Bolla, Jean-Michel, Pages, Jean-Marie, Boyer, Gerard, Alibert, Sandrine, Neulat-Ripoll, Fabienne, Elie, Jonathan, Bidault, Rudy, Arlicot, Nicolas, GUILLOTEAU, Denis, Vercouille, Johnny, D'Attoma, Joseph, Brun, Pierre-Louis, Robin, Yves, Bostyn, Stephane, Ejjoummany, Abdelaziz, Buron, Frederic, El Hakmaoui, Ahmed, Routier, Sylvain, Guillaumet, Gerald, Akssira, Mohamed, Marx, Sebastien, Dal Maso, Thomas, Michiels, Cerine, Wouters, Johan, Prevost, Julien R. C., Van Ham, Nicolas J. P., Kozlova, Arina, Frederick, Raphael, Drapier, Thomas, Geubelle, Pierre, Department of Medicinal Chemistry, Natural and Synthetic Drugs Research Centre, Université de Liège, Université de Namur [Namur] (UNamur), Institut de Chimie Organique et Analytique (ICOA), Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Université d'Orléans (UO)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), ManRos Therapeutics, Institut des Sciences Chimiques de Rennes (ISCR), Université de Rennes (UR)-Institut National des Sciences Appliquées - Rennes (INSA Rennes), Institut National des Sciences Appliquées (INSA)-Institut National des Sciences Appliquées (INSA)-Ecole Nationale Supérieure de Chimie de Rennes (ENSCR)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Phophorylation de protéines et Pathologies Humaines (P3H), Station biologique de Roscoff [Roscoff] (SBR), Université Pierre et Marie Curie - Paris 6 (UPMC)-Centre National de la Recherche Scientifique (CNRS)-Université Pierre et Marie Curie - Paris 6 (UPMC)-Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS), Université Pierre et Marie Curie - Paris 6 (UPMC)-Centre National de la Recherche Scientifique (CNRS), Chimie Et Interdisciplinarité : Synthèse, Analyse, Modélisation (CEISAM), Université de Nantes - UFR des Sciences et des Techniques (UN UFR ST), Université de Nantes (UN)-Université de Nantes (UN)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Laboratoire de Chimie Bioorganique et des Substances Naturelles (LCBOSN), Université Abobo-Adjamé, Université Péléforo Gon Coulibaly, UFR des Sciences Biologiques, Korhogo BP 1328, Côte d’Ivoire, Plate-forme ImPACcell (ImPACcell), Structure Fédérative de Recherche en Biologie et Santé de Rennes ( Biosit : Biologie - Santé - Innovation Technologique ), Université Nangui Abrogoua (UNA), Immunologie et Pathologie (EA2216), Université de Brest (UBO)-IFR148, LabEX IGO Immunothérapie Grand Ouest, Nantes Université (Nantes Univ), Laboratoire d'Innovation Thérapeutique (LIT), Université de Strasbourg (UNISTRA)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Centre de Recherche Jean-Pierre AUBERT Neurosciences et Cancer - U837 (JPArc), Université Lille Nord de France (COMUE)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Université de Lille, Instituto de Medicina Molecular (iMM), Faculdade de Medicina [Lisboa], Universidade de Lisboa = University of Lisbon (ULISBOA)-Universidade de Lisboa = University of Lisbon (ULISBOA), Conception, synthèse et vectorisation de biomolécules. (CSVB), Université Paris Descartes - Paris 5 (UPD5)-Institut Curie [Paris]-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Transporteurs membranaires, chimioresistance et drug-design (TMCD2), Aix Marseille Université (AMU)-Institut National de la Santé et de la Recherche Médicale (INSERM), Institut de Recherche Biomédicale des Armées [Brétigny-sur-Orge] (IRBA), Membranes et cibles thérapeutiques (MCT), Aix Marseille Université (AMU)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Institut de Recherche Biomédicale des Armées [Brétigny-sur-Orge] (IRBA), Imagerie et cerveau (iBrain - Inserm U1253 - UNIV Tours ), Université de Tours (UT)-Institut National de la Santé et de la Recherche Médicale (INSERM), Calculateurs Parallèles (CALCPAR), Institut de Recherche en Informatique et Systèmes Aléatoires (IRISA), Institut National des Sciences Appliquées (INSA)-Institut National des Sciences Appliquées (INSA)-Institut National de Recherche en Informatique et en Automatique (Inria)-Centre National de la Recherche Scientifique (CNRS)-Université de Rennes (UR)-Institut National des Sciences Appliquées - Rennes (INSA Rennes), Institut National des Sciences Appliquées (INSA)-Institut National des Sciences Appliquées (INSA)-Institut National de Recherche en Informatique et en Automatique (Inria)-Centre National de la Recherche Scientifique (CNRS)-INRIA Rennes, Institut National de Recherche en Informatique et en Automatique (Inria), Institut de Combustion, Aérothermique, Réactivité et Environnement (ICARE), Université d'Orléans (UO)-Centre National de la Recherche Scientifique (CNRS)-Institut des Sciences de l'Ingénierie et des Systèmes (INSIS - CNRS), Laboratoire de Chimie Physique & de Chimie Bioorganique, URAC 22 (LCPCB), Faculte des sciences et Techniques Mohammedia [Casablanca] (FSTM), Université Hassan II [Casablanca] (UH2MC)-Université Hassan II [Casablanca] (UH2MC), Laboratoire de Chimie, Bioorganique et analytique, Université Hassan II [Casablanca] (UH2MC), Université Catholique de Louvain = Catholic University of Louvain (UCL), Université d'Orléans (UO)-Centre National de la Recherche Scientifique (CNRS)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Institut de Chimie du CNRS (INC)-Institut National de la Santé et de la Recherche Médicale (INSERM), Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)-Université de Rennes 1 (UR1), Université de Rennes (UNIV-RENNES)-Université de Rennes (UNIV-RENNES)-Ecole Nationale Supérieure de Chimie de Rennes (ENSCR)-Institut National des Sciences Appliquées - Rennes (INSA Rennes), Institut National des Sciences Appliquées (INSA)-Université de Rennes (UNIV-RENNES)-Institut National des Sciences Appliquées (INSA), Université de Nantes (UN)-Université de Nantes (UN)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Université Nangui Abrogoua, Centre de Recherche Jean-Pierre AUBERT Neurosciences et Cancer - U1172 Inserm - U837 (JPArc), Institut National de la Santé et de la Recherche Médicale (INSERM)-Université Lille Nord de France (COMUE)-Université de Lille, Lille Inflammation Research International Center - U 995 (LIRIC), Institut Pasteur de Lille, Réseau International des Instituts Pasteur (RIIP)-Réseau International des Instituts Pasteur (RIIP)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Université de Lille-Centre Hospitalier Régional Universitaire [Lille] (CHRU Lille), Universidade de Lisboa (ULISBOA)-Universidade de Lisboa (ULISBOA), Université Paris Descartes - Paris 5 (UPD5)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Institut Curie [Paris], Institut de Recherche Biomédicale des Armées (IRBA), Aix Marseille Université (AMU)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Institut de Recherche Biomédicale des Armées (IRBA), Institut de Chimie et Biochimie Moléculaires et Supramoléculaires (ICBMS), Université Claude Bernard Lyon 1 (UCBL), Université de Lyon-Université de Lyon-Institut National des Sciences Appliquées de Lyon (INSA Lyon), Institut National des Sciences Appliquées (INSA)-Université de Lyon-Institut National des Sciences Appliquées (INSA)-Institut de Chimie du CNRS (INC)-École Supérieure Chimie Physique Électronique de Lyon-Centre National de la Recherche Scientifique (CNRS), Université de Rennes 1 (UR1), Université de Rennes (UNIV-RENNES)-Université de Rennes (UNIV-RENNES)-Institut National des Sciences Appliquées - Rennes (INSA Rennes), Institut National des Sciences Appliquées (INSA)-Université de Rennes (UNIV-RENNES)-Institut National des Sciences Appliquées (INSA)-Institut National de Recherche en Informatique et en Automatique (Inria)-Centre National de la Recherche Scientifique (CNRS)-Université de Rennes 1 (UR1), Institut National des Sciences Appliquées (INSA)-Université de Rennes (UNIV-RENNES)-Institut National des Sciences Appliquées (INSA)-Institut National de Recherche en Informatique et en Automatique (Inria)-Centre National de la Recherche Scientifique (CNRS)-INRIA Rennes, Université d'Orléans (UO)-Centre National de la Recherche Scientifique (CNRS)-Institut des Sciences de l'Ingénierie et des Systèmes (INSIS), Université de Namur [Namur], Université d'Orléans (UO)-Centre National de la Recherche Scientifique (CNRS)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Institut National de la Santé et de la Recherche Médicale (INSERM), Université d'Orléans (UO)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre National de la Recherche Scientifique (CNRS), Institut National des Sciences Appliquées - Rennes (INSA Rennes), Institut National des Sciences Appliquées (INSA)-Université de Rennes (UNIV-RENNES)-Institut National des Sciences Appliquées (INSA)-Université de Rennes (UNIV-RENNES)-Centre National de la Recherche Scientifique (CNRS)-Ecole Nationale Supérieure de Chimie de Rennes-Université de Rennes 1 (UR1), Université de Rennes (UNIV-RENNES), Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS)-Station biologique de Roscoff (SBR), Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS), Université de Nantes - Faculté des Sciences et des Techniques, Université de Nantes (UN)-Université de Nantes (UN)-Centre National de la Recherche Scientifique (CNRS), Université de Strasbourg (UNISTRA)-Centre National de la Recherche Scientifique (CNRS), Centre de Recherche Jean-Pierre AUBERT Neurosciences et Cancer (JPArc - U1172 Inserm), Université Lille Nord de France (COMUE)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre Hospitalier Régional Universitaire [Lille] (CHRU Lille)-Université Lille 2 - Faculté de Médecine, Centre de recherche Jean-Pierre Aubert-Neurosciences et Cancer, Institut National de la Santé et de la Recherche Médicale (INSERM)-Université de Lille, Droit et Santé, Lille Inflammation Research International Center (LIRIC), Institut Curie-Centre National de la Recherche Scientifique (CNRS)-Université Paris Descartes - Paris 5 (UPD5), Imagerie et cerveau, Université de Tours-Institut National de la Santé et de la Recherche Médicale (INSERM), Université de Lyon-Institut National des Sciences Appliquées (INSA)-Institut National des Sciences Appliquées (INSA)-École Supérieure Chimie Physique Électronique de Lyon-Centre National de la Recherche Scientifique (CNRS), Université Catholique de Louvain (UCL), Institut National des Sciences Appliquées (INSA)-Université de Rennes (UNIV-RENNES)-Institut National des Sciences Appliquées (INSA)-Ecole Nationale Supérieure de Chimie de Rennes (ENSCR)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Institut National de la Santé et de la Recherche Médicale (INSERM)-Institut de Recherche Biomédicale des Armées (IRBA)-Aix Marseille Université (AMU), and Université de Lyon-Institut National des Sciences Appliquées (INSA)-Institut National des Sciences Appliquées (INSA)-Institut de Chimie du CNRS (INC)-École Supérieure Chimie Physique Électronique de Lyon-Centre National de la Recherche Scientifique (CNRS)

Subjects
pharmacochemistry, target discovery, organic and medicinal chemistry, [CHIM]Chemical Sciences, pharmacology, chemoinformatics, medical imagery, ComputingMilieux_MISCELLANEOUS
Abstract

International audience; The “Journées Franco-Belges de Pharmacochimie” is a recognized annual meeting in organic and medicinal chemistry known for the quality of scientific exchange and conviviality. Young researchers were encouraged to present their work and share ideas with senior scientists. Abstracts of plenary lectures, oral communications, and posters presented during the meeting are collected in this report.

Published
2016
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26. Synthesis, evaluation and structure-activity relationship of new 3-carboxamide coumarins as FXIIa inhibitors

Author

UCL - SSS/LDRI - Louvain Drug Research Institute, Bouckaert, Charlotte, Serra, Silvia, Rondelet, Grégoire, Dolušić, Eduard, Wouters, Johan, Dogné, Jean-Michel, Frédérick, Raphaël, Pochet, Lionel, UCL - SSS/LDRI - Louvain Drug Research Institute, Bouckaert, Charlotte, Serra, Silvia, Rondelet, Grégoire, Dolušić, Eduard, Wouters, Johan, Dogné, Jean-Michel, Frédérick, Raphaël, and Pochet, Lionel

Abstract

Inhibitors of the coagulation factor XIIa (FXIIa) are attractive to detail the roles of this protease in hemostasis and thrombosis, to suppress artifact due to contact pathway activation in blood coagulation assays, and they are promising as antithrombotic therapy. The 3-carboxamide coumarins have been previously described as small-molecular-weight FXIIa inhibitors. In this study, we report a structure-activity relationship (SAR) study around this scaffold with the aim to discover new selective FXIIa inhibitors with an improved physico-chemical profile. To better understand these SAR, docking experiments were undertaken. For this purpose, we built an original hybrid model of FXIIa. This model has the advantage to gather the best features from the recently published crystal structure of FXIIa in its zymogen form and a more classical homology model. Results with the hybrid model are encouraging as they help understanding the activity and selectivity of our best compounds.

Published
2016

28. Transrectal potential difference in F508del-CFTR mice: an additional tool to evaluate in vivo ion transport in cystic fibrosis

Author

Dhooghe, Barbara, Lubamba, Bob, Palem, Alain, Bouckaert, Charlotte, Leonard, Anissa Marie, Wallemacq, Pierre, Lebecque, Patrick, Leal, Teresinha, 5th European CF Young Meeting, UCL - SSS/IREC/LTAP - Louvain Centre for Toxicology and Applied Pharmacology, UCL - (SLuc) Département de pédiatrie, UCL - (SLuc) Service de biochimie médicale, and UCL - (SLuc) Centre de référence pour la mucoviscidose

Published
2011

29. Vardenafil corrects transrectal chloride transport in CF mice

Author

Dhooghe, Barbara, Bouckaert, Charlotte, Wallemacq, Pierre, Leal, Teresinha, Autumn Meeting of the Belgian Society of Fundamental and Clinical Physiology and Pharmacology, UCL - SSS/IREC/LTAP - Louvain Centre for Toxicology and Applied Pharmacology, and UCL - (SLuc) Service de biochimie médicale

Abstract

We have previously shown that characteristic transepithelial ion transport defects in cystic fibrosis (CF), namely increased sodium absorption and reduced or abolished chloride transport, can be assessed at the intestinal level, a clinically relevant CF target organ, by means of the rectal potential difference test (RPD). The aim of this work is to test the efficacy of vardenafil, an inhibitor of phosphodiesterase type 5, to correct CFTR-dependent transrectal ion transport in CF mice homozygous for the F508del mutation as compared to heterozygous (HTZ) and wild-type homozygous (WT) animals from the same 129/FVB genetic background. RPD was performed 1 h after a single ip injection of vardenafil (0.14 mg/kg). Total chloride secretion across the rectal mucosa (TCS) was monitored under perfusion of a Ringer’s solution without chloride (replaced by gluconate) and with 10- 5 M forskolin, and containing 10-4 M amiloride and 5 x 10-3 M barium, to block sodium and potassium movement. Vardenafil significantly stimulated TCS in CF mice when values obtained in the absence of vardenafil (-4.2  0.5 mV; mean  SEM; n:5) reached -9.3  1.1mV (n:7; p:0.0054) after vardenafil treatment. Intermediately reduced TCS values in the HTZ group were also significantly increased by vardenafil treatment. The corrector effect of vardenafil was mainly due to the contribution of forskolin sensitivity that was increased by 4-fold in the HTZ group and by 5-fold in the CF group. These data indicate that RPD is a powerful tool to assess efficacy of therapeutic strategies in CF. Our findings confirm that vardenafil corrects CFTR-dependent chloride transport in CF intestinal tissue.

Published
2011

30. Resveratrol Improves Chloride Secretion In CF Mice Homozygous For the F508del Mutation

Author

Palem, Alain, Bouckaert, Charlotte, Dhooghe, Barbara, Leonard, Anissa, Lubamba, Bob, Wallemacq, Pierre, Lebecque, Patrick, Leal, Teresinha, 34th European Cystic Fibrosis Conference, UCL - SSS/IREC/LTAP - Louvain Centre for Toxicology and Applied Pharmacology, UCL - (SLuc) Département de pédiatrie, and UCL - (SLuc) Centre de référence pour la mucoviscidose

Published
2011

32. Le Resveratrol Améliore La Sécrétion Chlorure Chez La Souris F508del

Author

Palem, Alain, Bouckaert, Charlotte, Dhooghe, Barbara, Leonard, Anissa, Lubamba, Bob, Wallemacq, Pierre, Lebecque, Patrick, Leal, Teresinha, 12ème Colloque des Jeunes chercheurs – Vaincre la Mucoviscidose, UCL - SSS/IREC/LTAP - Louvain Centre for Toxicology and Applied Pharmacology, UCL - (SLuc) Service de biochimie médicale, and UCL - (SLuc) Centre de référence pour la mucoviscidose

Published
2011

33. Resveratrol corrects refractory adrenergic pathway in saliva secretion of cystic fibrosis mice

Author

Bouckaert, Charlotte, Palem, Alain, Dhooghe, Barbara, Wallemacq, Pierre, Leal, Teresinha, Autumn Meeting of the Belgian Society of Fundamental and Clinical Physiology and Pharmacology, UCL - SSS/IREC/LTAP - Louvain Centre for Toxicology and Applied Pharmacology, and UCL - (SLuc) Service de biochimie médicale

Subjects
Resveratrol, Salivary secretion, Cystic fibrosis
Published
2011

35. Le Resveratrol Améliore La Sécrétion Chlorure Chez La Souris F508del

Author

UCL - SSS/IREC/LTAP - Louvain Centre for Toxicology and Applied Pharmacology, UCL - (SLuc) Service de biochimie médicale, UCL - (SLuc) Centre de référence pour la mucoviscidose, Palem, Alain, Bouckaert, Charlotte, Dhooghe, Barbara, Leonard, Anissa, Lubamba, Bob, Wallemacq, Pierre, Lebecque, Patrick, Leal, Teresinha, 12ème Colloque des Jeunes chercheurs – Vaincre la Mucoviscidose, UCL - SSS/IREC/LTAP - Louvain Centre for Toxicology and Applied Pharmacology, UCL - (SLuc) Service de biochimie médicale, UCL - (SLuc) Centre de référence pour la mucoviscidose, Palem, Alain, Bouckaert, Charlotte, Dhooghe, Barbara, Leonard, Anissa, Lubamba, Bob, Wallemacq, Pierre, Lebecque, Patrick, Leal, Teresinha, and 12ème Colloque des Jeunes chercheurs – Vaincre la Mucoviscidose

Published
2011

36. Resveratrol Improves Chloride Secretion In CF Mice Homozygous For the F508del Mutation

Author

UCL - SSS/IREC/LTAP - Louvain Centre for Toxicology and Applied Pharmacology, UCL - (SLuc) Département de pédiatrie, UCL - (SLuc) Centre de référence pour la mucoviscidose, Palem, Alain, Bouckaert, Charlotte, Dhooghe, Barbara, Leonard, Anissa, Lubamba, Bob, Wallemacq, Pierre, Lebecque, Patrick, Leal, Teresinha, 34th European Cystic Fibrosis Conference, UCL - SSS/IREC/LTAP - Louvain Centre for Toxicology and Applied Pharmacology, UCL - (SLuc) Département de pédiatrie, UCL - (SLuc) Centre de référence pour la mucoviscidose, Palem, Alain, Bouckaert, Charlotte, Dhooghe, Barbara, Leonard, Anissa, Lubamba, Bob, Wallemacq, Pierre, Lebecque, Patrick, Leal, Teresinha, and 34th European Cystic Fibrosis Conference

Published
2011

37. Différence de potentiel transrectal chez la souris F508del-CFTR: un outil additionnel d'évaluation in vivo du transport ionique dans la mucoviscidose

Author

UCL - SSS/IREC/LTAP - Louvain Centre for Toxicology and Applied Pharmacology, UCL - (SLuc) Service de biochimie médicale, UCL - (SLuc) Département de pédiatrie, Dhooghe, Barbara, Lubamba, Bob, Palem, Alain, Bouckaert, Charlotte, Leonard, Anissa Marie, Wallemacq, Pierre, Leal, Teresinha, 12ème Colloque des Jeunes Chercheurs - Vaincre la Mucoviscidose, UCL - SSS/IREC/LTAP - Louvain Centre for Toxicology and Applied Pharmacology, UCL - (SLuc) Service de biochimie médicale, UCL - (SLuc) Département de pédiatrie, Dhooghe, Barbara, Lubamba, Bob, Palem, Alain, Bouckaert, Charlotte, Leonard, Anissa Marie, Wallemacq, Pierre, Leal, Teresinha, and 12ème Colloque des Jeunes Chercheurs - Vaincre la Mucoviscidose

Published
2011

38. Transrectal potential difference in F508del-CFTR mice: an additional tool to evaluate in vivo ion transport in cystic fibrosis

Author

UCL - SSS/IREC/LTAP - Louvain Centre for Toxicology and Applied Pharmacology, UCL - (SLuc) Département de pédiatrie, UCL - (SLuc) Service de biochimie médicale, UCL - (SLuc) Centre de référence pour la mucoviscidose, Dhooghe, Barbara, Lubamba, Bob, Palem, Alain, Bouckaert, Charlotte, Leonard, Anissa Marie, Wallemacq, Pierre, Lebecque, Patrick, Leal, Teresinha, 5th European CF Young Meeting, UCL - SSS/IREC/LTAP - Louvain Centre for Toxicology and Applied Pharmacology, UCL - (SLuc) Département de pédiatrie, UCL - (SLuc) Service de biochimie médicale, UCL - (SLuc) Centre de référence pour la mucoviscidose, Dhooghe, Barbara, Lubamba, Bob, Palem, Alain, Bouckaert, Charlotte, Leonard, Anissa Marie, Wallemacq, Pierre, Lebecque, Patrick, Leal, Teresinha, and 5th European CF Young Meeting

Published
2011

39. Vardenafil corrects transrectal chloride transport in CF mice

Author

UCL - SSS/IREC/LTAP - Louvain Centre for Toxicology and Applied Pharmacology, UCL - (SLuc) Service de biochimie médicale, Dhooghe, Barbara, Bouckaert, Charlotte, Wallemacq, Pierre, Leal, Teresinha, Autumn Meeting of the Belgian Society of Fundamental and Clinical Physiology and Pharmacology, UCL - SSS/IREC/LTAP - Louvain Centre for Toxicology and Applied Pharmacology, UCL - (SLuc) Service de biochimie médicale, Dhooghe, Barbara, Bouckaert, Charlotte, Wallemacq, Pierre, Leal, Teresinha, and Autumn Meeting of the Belgian Society of Fundamental and Clinical Physiology and Pharmacology

Abstract

We have previously shown that characteristic transepithelial ion transport defects in cystic fibrosis (CF), namely increased sodium absorption and reduced or abolished chloride transport, can be assessed at the intestinal level, a clinically relevant CF target organ, by means of the rectal potential difference test (RPD). The aim of this work is to test the efficacy of vardenafil, an inhibitor of phosphodiesterase type 5, to correct CFTR-dependent transrectal ion transport in CF mice homozygous for the F508del mutation as compared to heterozygous (HTZ) and wild-type homozygous (WT) animals from the same 129/FVB genetic background. RPD was performed 1 h after a single ip injection of vardenafil (0.14 mg/kg). Total chloride secretion across the rectal mucosa (TCS) was monitored under perfusion of a Ringer’s solution without chloride (replaced by gluconate) and with 10- 5 M forskolin, and containing 10-4 M amiloride and 5 x 10-3 M barium, to block sodium and potassium movement. Vardenafil significantly stimulated TCS in CF mice when values obtained in the absence of vardenafil (-4.2  0.5 mV; mean  SEM; n:5) reached -9.3  1.1mV (n:7; p:0.0054) after vardenafil treatment. Intermediately reduced TCS values in the HTZ group were also significantly increased by vardenafil treatment. The corrector effect of vardenafil was mainly due to the contribution of forskolin sensitivity that was increased by 4-fold in the HTZ group and by 5-fold in the CF group. These data indicate that RPD is a powerful tool to assess efficacy of therapeutic strategies in CF. Our findings confirm that vardenafil corrects CFTR-dependent chloride transport in CF intestinal tissue.

Published
2011

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