Unité de recherche : U1177
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M2SV : Médicaments et molécules pour les systèmes vivants

Université de Lille – Inserm – Institut Pasteur de Lille

Directeur : Benoît DEPREZ

Le Drug Discovery Center réalise les phases amont du processus de R&D pharmaceutique, en lien avec les chercheurs qui étudient les mécanismes des maladies.

Nos équipes ont pour mission de concevoir, synthétiser des prototypes de médicament possédant un mode d’action innovant et visant un progrès thérapeutique marqué dans des indications où le besoin médical est faiblement satisfait. A l’issue de ce processus de recherche, ces prototypes ou « candidats-médicaments » sont suffisamment caractérisés pour entrer en développement préclinique et clinique, le plus souvent en collaboration avec un partenaire industriel, du secteur pharmaceutique ou biotechnologique.

Ce travail d’invention moléculaire interdisciplinaire est inspiré par les découvertes les plus récentes réalisées sur les maladies infectieuses, les maladies du métabolisme, du système immunitaire et le cancer. La découverte des molécules permet à la fois de proposer de nouvelles solutions thérapeutiques et de valider l’implication des mécanismes mis en évidence par les biologistes dans les processus physiopathologiques.

La conception de nouveaux médicaments

La conception et l’optimisation de nouveaux médicaments requièrent une compétence interdisciplinaire couvrant la chimie, la physique, la biologie et la modélisation in silico et l’intelligence artificielle. En effet, le principe actif des médicaments modernes, qu’il soit d’origine synthétique ou biologique est toujours défini à l’échelle moléculaire, voire atomique.

Cette structure moléculaire particulière -mise au point par les chercheurs du Drug Discovery center- est la clé de toutes les propriétés du médicament. Elle conditionne son aptitude à franchir les barrières physiques et chimiques entre les différentes biophases (intestin, sang, tissus, cerveau…) de l’organisme et à atteindre la cible visée. Elle est aussi à la clé de son interaction avec la cible visée et la réalisation de l’effet désiré. Au-delà de l’objectif thérapeutique, les molécules servent également d’outils précieux qui aident les biologistes à mieux comprendre le fonctionnement de la cellule et des organismes vivants et à vérifier que les cibles proposées pour soigner les maladies sont pertinentes.

Nos équipes travaillent sur la résistance aux antibiotiques, le diabète de type 2, certaines formes de cancers, la reconnaissance des antigènes cellulaires par le système immunitaire.

Publications 2022-2026

Vasconcelos, F., Lesire, L., Herledan, A., Piveteau, C., Deprez, B., Iatrou, H., & Deprez-Poulain, R. ERAP2 inhibitor −incorporated nanofibers: Characterization and biological assessment. International Journal of Pharmaceutics,2026 126555. 10.1016/j.ijpharm.2026.126555,  OPEN ACCESS 

Deprez, B. Les « petites » molécules de synthèse : une réserve d’innovation thérapeutique inépuisable, accessible et aisément déployable. L’actualité chimique.,2025 10.63133/scf.act-chim.2025.505.06

Leib, J., Waeckel-Énée, E., Fabrega, S., Keelan, N., Senni, A., Mauvais, F. X., Deprez-Poulain, R., Bertocci, B., & van Endert, P. ERAP1-dependent extreme antigen processing efficacy can govern MHC class I expression hierarchy. J. Immunol.,2025 10.1093/jimmun/vkaf013.

He, B., Karroum, N. B., Gealageas, R., Mauvais, F.-X., Warenghem, S., Roignant, M., Kraupner, N., Lam, B. V., Azaroual, N., Ultré, V., Rech, A., Lesire, L., Couturier, C., Leroux, F., van Endert, P., Deprez, B., & Deprez-Poulain, R. Discovery of New Nanomolar Selective IRAP Inhibitors. J. Med. Chem.,2025.10.1021/acs.jmedchem.4c01744.OPEN ACCESS 

Ponzoni, A., Speca, S., Hartle, M., Gerstenberg, A., Tomezyk, A., Senec, V., Karnik, S., Dubuquoy, L., Launay, D., Deprez-Poulain, R., Gaudin, M., Ramos, C., & Deprez, B. An untargeted metabolomic study using MALDI-mass spectrometry imaging reveals region-specific biomarkers associated with bowel inflammation. Metabolomics,2024, 21(1): 5. 10.1007/s11306-024-02200-4 OPEN ACCESS

Paquot, A., Deprez, B., & Beghyn, T. Drug repurposing and phenotypic screening: innovative strategies for treating ultra-rare disorders. Frontiers in Medicine,2024, 11.10.3389/fmed.2024.1489094.

Gedeon, A., Yab, E., Dinut, A., Sadowski, E., Capton, E., Dreneau, A., Petit, J., Gioia, B., Piveteau, C., Djaout, K., Lecat, E., Wehenkel, A. M., Gubellini, F., Mecy, A., Alzari, P. M., Deprez, B., Baulard, A., Aubry, A., Willand, N., & Petrella, S. Molecular mechanism of a triazole-containing inhibitor of Mycobacterium tuberculosis DNA gyrase. iScience,2024, 27(10): 110967.10.1016/j.isci.2024.110967.

Fougiaxis, V., Barcherini, V., Petrovic, M. M., Sierocki, P., Warenghem, S., Leroux, F., Bou Karroum, N., Petit-Cancelier, F., Rodeschini, V., Roche, D., Deprez, B., & Deprez-Poulain, R. First fragment-based screening identifies new chemotypes inhibiting ERAP1-metalloprotease. Eur. J. Med. Chem.,2024, 280: 116926. 10.1016/j.ejmech.2024.116926. OPEN ACCESS   

Deprez-Poulain, R., Duca, M., George, N., Deprez, B., Ortholand, J.-Y. The French Medicinal Chemistry Society–Sct, an Historical Member of EFMC. ChemMedChem 2024, e202400437. 10.1002/cmdc.202400437 OPEN ACCESS

Lakli, M., Dumont, J., Vauthier, V., Charton, J., Crespi, V., Banet, M., Riahi, Y., Ben Saad, A., Mareux, E., Lapalus, M., Gonzales, E., Jacquemin, E., Di Meo, F., Deprez, B., Leroux, F., & Falguières, T. Identification of new correctors for traffic-defective ABCB4 variants by a high-content screening approach. Communications Biology,2024, 7(1): 898.10.1038/s42003-024-06590-y.

Caradec, T., Plé, C., Sicoli, G., Petrov, R., Pradel, E., Sobieski, C., Antoine, R., Orio, M., Herledan, A., Willand, N., & Hartkoorn, R. C. Small molecule MarR modulators potentiate metronidazole antibiotic activity in aerobic E. coli by inducing activation by the nitroreductase NfsA. J. Biol. Chem.,2024, 300(7): 107431.10.1016/j.jbc.2024.107431.

Chaibi, F.-Z., Brier, L., Carré, P., Landry, V., Desmarets, L., Tarricone, A., Cantrelle, F.-X., Moschidi, D., Herledan, A., Biela, A., Bourgeois, F., Ribes, C., Ikherbane, S., Malessan, M., Dubuisson, J., Belouzard, S., Hanoulle, X., Leroux, F., Deprez, B., & Charton, J. N-acylbenzimidazoles as selective Acylators of the catalytic cystein of the coronavirus 3CL protease. Eur. J. Med. Chem.,2024, 276: 116707.10.1016/j.ejmech.2024.116707.  

De Spiegeleer, B., Deprez, B., Hak, E., Markuszewski, M., & Wynendaele, E. On the pivotal role of drug discovery in sustainable EU pharma reform. Drug Discovery Today,2024, 29(10): 104097.10.1016/j.drudis.2024.104097.

Fougiaxis, V., He, B., Khan, T., Vatinel, R., Koutroumpa, N. M., Afantitis, A., Lesire, L., Sierocki, P., Deprez, B., & Deprez-Poulain, R. ERAP Inhibitors in Autoimmunity and Immuno-Oncology: Medicinal Chemistry Insights. J. Med. Chem.,2024. 10.1021/acs.jmedchem.4c00840. OPEN ACCESS   

Andres, M., Hennuyer, N., Zibar, K., Bicharel-Leconte, M., Duplan, I., Enée, E., Vallez, E., Herledan, A., Loyens, A., Staels, B., Deprez, B., van Endert, P., Deprez-Poulain, R., & Lancel, S. Insulin-degrading enzyme inhibition increases the unfolded protein response and favours lipid accumulation in the liver. Br. J. Pharmacol.,2024, 181(19): 3610-3626. 10.1111/bph.16436.

Aguilar-Ayala, D. A., Sanz-García, F., Rabodoarivelo, M. S., Susanto, B. O., Bailo, R., Eveque-Mourroux, M. R., Willand, N., Simonsson, U. S. H., Ramón-García, S., & Lucía, A. Evaluation of critical parameters in the hollow-fibre system for tuberculosis: A case study of moxifloxacin. Br. J. Clin. Pharmacol.,2024, 90(7): 1711-1727.10.1111/bcp.16068.

Grosse, C., Sigoillot, M., Megalizzi, V., Tanina, A., Willand, N., Baulard, A. R., & Wintjens, R. Crystal structure of the Mycobacterium tuberculosis VirS regulator reveals its interaction with the lead compound SMARt751. J. Struct. Biol.,2024, 216(2): 108090.10.1016/j.jsb.2024.108090.

Mosheim, J. R., Ruggieri, F., Humeau, C., Hance, P., Willand, N., Hilbert, J. L., Heuson, E., & Froidevaux, R. Biocatalytic Regioselective O-acylation of Sesquiterpene Lactones from Chicory: A Pathway to Novel Ester Derivatives. Chembiochem,2024, 25(6): e202300722.10.1002/cbic.202300722.

Brier, L., Furman, C., Charton, J., Deprez, B., & Lipka, E. Capillary electrokinetic chromatography for chiral separation of potential SARS-CoV-2 3CL protease inhibitors. Electrophoresis,2024.10.1002/elps.202300178.

Jiménez-Castellanos, J.-C., Pradel, E., Compagne, N., Vieira Da Cruz, A., Flipo, M., & Hartkoorn, R. C. Characterization of pyridylpiperazine-based efflux pump inhibitors for Acinetobacter baumannii. JAC-Antimicrobial Resistance,2023, 5(5): dlad112. 10.1093/jacamr/dlad112.

Vieira Da Cruz, A., Jiménez-Castellanos, J.-C., Börnsen, C., Van Maele, L., Compagne, N., Pradel, E., Müller, R. T., Meurillon, V., Soulard, D., Piveteau, C., Biela, A., Dumont, J., Leroux, F., Deprez, B., Willand, N., Pos, K. M., Frangakis, A. S., Hartkoorn, R. C., & Flipo, M. Pyridylpiperazine efflux pump inhibitor boosts in vivo antibiotic efficacy against K. pneumoniae. EMBO Molecular Medicine,2023, 16: 93-111.10.1038/s44321-023-00007-9.

Gioia, B., Ruggieri, F., Biela, A., Landry, V., Roussel, P., Piveteau, C., Leroux, F., Hartkoorn, R. C., & Willand, N. Regioselective and Stereoselective Synthesis of Parthenolide Analogs by Acyl Nitroso-Ene Reaction and Their Biological Evaluation against Mycobacterium tuberculosis. International journal of molecular sciences,2023, 24(24).10.3390/ijms242417395.

Songue Same, O., Nobosse, P., Ngolong Ngea, G. L., Piveteau, C., Lemdani, M., Kamga, R., & Deprez, B. Migration study of phtates from non-food plastic containers used in food preservation. Heliyon,2023, 99: e20002.10.1016/j.heliyon.2023.e20002.

Picon, S., Boulahjar, R., Hoguet, V., Baron, M., Duplan, I., Vallez, E., Hennuyer, N., Dumont, J., Touche, V., Dorchies, E., Lasalle, M., Descat, A., Piveteau, C., Biela, A., Chaput, L., Villoutreix, B. O., Lipka, E., Sevin, E., Culot, M., Gosselet, F., Lestavel, S., Roussel, P., Deprez-Poulain, R., Leroux, F., Staels, B., Deprez, B., Tailleux, A., & Charton, J. Discovery, Structure–Activity Relationships, and In Vivo Activity of Dihydropyridone Agonists of the Bile Acid Receptor TGR5. Journal of Medicinal Chemistry,2023.10.1021/acs.jmedchem.2c01881.

Compagne, N., Jiménez-Castellanos, J.-C., Meurillon, V., Pradel, E., Vieira Da Cruz, A., Piveteau, C., Biela, A., Eveque, M., Leroux, F., Deprez, B., Willand, N., Hartkoorn, R. C., & Flipo, M. Optimization of pyridylpiperazine-based inhibitors of the Escherichia coli AcrAB-TolC efflux pump. European Journal of Medicinal Chemistry,2023, 259: 115630.10.1016/j.ejmech.2023.115630.

Villemagne, B., Faion, L., Tangara, S., & Willand, N. Recent advances in Fragment-based strategies against tuberculosis. European Journal of Medicinal Chemistry,2023, 258: 115569.10.1016/j.ejmech.2023.115569.

Ruggieri, F., Hance, P., Gioia, B., Biela, A., Roussel, P., Hilbert, J.-L., & Willand, N. A Three-Step Process to Isolate Large Quantities of Bioactive Sesquiterpene Lactones from Cichorium intybus L. Roots and Semisynthesis of Chicory STLs Standards. Pharmaceuticals,2023, 165.10.3390/ph16050771.

Maingot, M., Bourotte, M., Vetter, A. C., Schellhorn, B., Antraygues, K., Scherer, H., Gitzinger, M., Kemmer, C., Dale, G. E., Defert, O., Lociuro, S., Brönstrup, M., Willand, N., & Trebosc, V. Structure-activity relationships of actively FhuE transported rifabutin derivatives with potent activity against Acinetobacter baumannii. European Journal of Medicinal Chemistry,2023, 252: 115257.10.1016/j.ejmech.2023.115257.

Ruggieri, F., Compagne, N., Antraygues, K., Eveque, M., Flipo, M., & Willand, N. Antibiotics with novel mode of action as new weapons to fight antimicrobial resistance. European Journal of Medicinal Chemistry,2023, 256: 115413.10.1016/j.ejmech.2023.115413.

Zubiaga, L., Briand, O., Auger, F., Touche, V., Hubert, T., Thevenet, J., Marciniak, C., Quenon, A., Bonner, C., Peschard, S., Raverdy, V., Daoudi, M., Kerr-Conte, J., Pasquetti, G., Koepsell, H., Zdzieblo, D., Mühlemann, M., Thorens, B., Delzenne, N. D., Bindels, L. B., Deprez, B., Vantyghem, M. C., Laferrère, B., Staels, B., Huglo, D., Lestavel, S., & Pattou, F. Oral metformin transiently lowers post-prandial glucose response by reducing the apical expression of sodium-glucose co-transporter 1 in enterocytes. iScience,2023, 264: 106057.10.1016/j.isci.2023.106057.

Tangara, S., Faïon, L., Piveteau, C., Capet, F., Godelier, R., Michel, M., Flipo, M., Deprez, B., Willand, N., & Villemagne, B. Rapid and Efficient Access to Novel Bio-Inspired 3-Dimensional Tricyclic SpiroLactams as Privileged Structures via Meyers’ Lactamization. Pharmaceuticals,2023, 163.10.3390/ph16030413.

Delannoy, C. P., Heuson, E., Herledan, A., Oger, F., Thiroux, B., Chevalier, M., Gromada, X., Rolland, L., Froguel, P., Deprez, B., Paul, S., & Annicotte, J.-S. High-Throughput Quantitative Screening of Glucose-Stimulated Insulin Secretion and Insulin Content Using Automated MALDI-TOF Mass Spectrometry. Cells,2023, 126.10.3390/cells12060849.

Brier, L., Hassan, H., Hanoulle, X., Landry, V., Moschidi, D., Desmarets, L., Rouillé, Y., Dumont, J., Herledan, A., Warenghem, S., Piveteau, C., Carré, P., Ikherbane, S., Cantrelle, F.-X., Dupré, E., Dubuisson, J., Belouzard, S., Leroux, F., Deprez, B., & Charton, J. Novel dithiocarbamates selectively inhibit 3CL protease of SARS-CoV-2 and other coronaviruses. European Journal of Medicinal Chemistry,2023, 250: 115186. 10.1016/j.ejmech.2023.115186.

Faïon, L., Djaout, K., Pintiala, C., Piveteau, C., Leroux, F., Biela, A., Slupek, S., Antoine, R., Záhorszká, M., Cantrelle, F.-X., Hanoulle, X., Korduláková, J., Deprez, B., Willand, N., Baulard, A. R., & Flipo, M. Exploring the Antitubercular Activity of Anthranilic Acid Derivatives: From MabA (FabG1) Inhibition to Intrabacterial Acidification. Pharmaceuticals,2023, 163.10.3390/ph16030335.

Compagne, N., Vieira Da Cruz, A., Müller, R. T., Hartkoorn, R. C., Flipo, M., & Pos, K. M. Update on the Discovery of Efflux Pump Inhibitors against Critical Priority Gram-Negative Bacteria. Antibiotics,2023, 121.10.3390/antibiotics12010180.

Dam, S., Tangara, S., Hamela, C., Hattabi, T., Faïon, L., Carre, P., Antoine, R., Herledan, A., Leroux, F., Piveteau, C., Eveque, M., Flipo, M., Deprez, B., Kremer, L., Willand, N., Villemagne, B., & Hartkoorn, R. C. Tricyclic SpiroLactams Kill Mycobacteria In Vitro and In Vivo by Inhibiting Type II NADH Dehydrogenases. Journal of Medicinal Chemistry,2022, 65(24): 16651-16664.10.1021/acs.jmedchem.2c01493.

Songue-Same, O., Piveteau, C., Biela, A., Kamga, R., & Deprez, B. Evaluation of the exposure to bisphenols from baby bottles and non-food containers used for food preservation in Cameroon. Journal of Hazardous Materials Advances,2022: 100212.10.1016/j.hazadv.2022.100212.

Legru, A., Verdirosa, F., Vo-Hoang, Y., Tassone, G., Vascon, F., Thomas, C. A., Sannio, F., Corsica, G., Benvenuti, M., Feller, G., Coulon, R., Marcoccia, F., Devente, S. R., Bouajila, E., Piveteau, C., Leroux, F., Deprez-Poulain, R., Deprez, B., Licznar-Fajardo, P., Crowder, M. W., Cendron, L., Pozzi, C., Mangani, S., Docquier, J.-D., Hernandez, J.-F., & Gavara, L. Optimization of 1,2,4-Triazole-3-thiones toward Broad-Spectrum Metallo-β-lactamase Inhibitors Showing Potent Synergistic Activity on VIM- and NDM-1-Producing Clinical Isolates. Journal of Medicinal Chemistry,2022: in press.10.1021/acs.jmedchem.2c01257.

Antraygues, K., Maingot, M., Schellhorn, B., Trebosc, V., Gitzinger, M., Deprez, B., Defert, O., Dale, G. E., Bourotte, M., Lociuro, S., & Willand, N. Design and synthesis of water-soluble prodrugs of rifabutin for intraveneous administration. European Journal of Medicinal Chemistry,2022, 238: 114515.10.1016/j.ejmech.2022.114515.

Camberlein, V., Fleau-Tabey, C., Sierocki, P., Li, L., Gealageas, R., Bosc, D., Guillaume, V., Warenghem, S., Leroux, F., Rosell, M., Cheng, K., Medve, L., Prigent, M., Decanter, M., Piveteau, C., Biela, A., Eveque, M., Dumont, J., Mpakali, A., Giastas, P., Herledan, A., Couturier, C., Haupent, J., Lesire, L., Hirsch, A. K., Deprez, B., Stratikos, E., Bouvier, M., & Deprez-Poulain, R. Discovery of the First Selective Nanomolar Inhibitors of Endoplasmic Reticulum Aminopeptidase 2 by Kinetic Target-Guided Synthesis. Angewandte Chemie International Edition,2022, n/an/a.10.1002/anie.202203560.

Belouzard, S., Machelart, A., Sencio, V., Vausselin, T., Hoffmann, E., Deboosere, N., Rouillé, Y., Desmarets, L., Séron, K., Danneels, A., Robil, C., Belloy, L., Moreau, C., Piveteau, C., Biela, A., Vandeputte, A., Heumel, S., Deruyter, L., Dumont, J., Leroux, F., Engelmann, I., Alidjinou, E. K., Hober, D., Brodin, P., Beghyn, T., Trottein, F., Deprez, B., & Dubuisson, J. Clofoctol inhibits SARS-CoV-2 replication and reduces lung pathology in mice. PLOS Pathogens,2022, 185: e1010498.10.1371/journal.ppat.1010498.

Flipo, M., Frita, R., Bourotte, M., Martínez-Martínez María, S., Boesche, M., Boyle Gary, W., Derimanov, G., Drewes, G., Gamallo, P., Ghidelli-Disse, S., Gresham, S., Jiménez, E., de Mercado, J., Pérez-Herrán, E., Porras-De Francisco, E., Rullas, J., Casado, P., Leroux, F., Piveteau, C., Kiass, M., Mathys, V., Soetaert, K., Megalizzi, V., Tanina, A., Wintjens, R., Antoine, R., Brodin, P., Delorme, V., Moune, M., Djaout, K., Slupek, S., Kemmer, C., Gitzinger, M., Ballell, L., Mendoza-Losana, A., Lociuro, S., Deprez, B., Barros-Aguirre, D., Remuiñán Modesto, J., Willand, N., & Baulard, A. The small-molecule SMARt751 reverses Mycobacterium tuberculosis resistance to ethionamide in acute and chronic mouse models of tuberculosis. Science Translational Medicine,2022 14643: eaaz6280. 10.1126/scitranslmed.aaz6280.

Lesire, L., Leroux, F., Deprez-Poulain, R., & Deprez, B. Insulin-Degrading Enzyme, an Under-Estimated Potential Target to Treat Cancer? Cells,2022, 117. 10.3390/cells11071228.

Antraygues, K., Compagne, N., Ruggieri, F., Djaout, K., Edoo, Z., Eveque, M., Faïon, L., Gioia, B., Tangara, S., Vieira Da Cruz, A., Villemagne, B., Flipo, M., Baulard, A., & Willand, N. On the Hunt for Next-Generation Antimicrobial Agents: An Online Symposium Organized Jointly by the French Society for Medicinal Chemistry (Société de Chimie Thérapeutique) and the French Microbiology Society (Société Française de Microbiologie) on 9-10 December 2021. Pharmaceuticals,2022, 154. 10.3390/ph15040388.

Plé, C., Tam, H.-K., Vieira Da Cruz, A., Compagne, N., Jiménez-Castellanos, J.-C., Müller, R. T., Pradel, E., Foong, W. E., Malloci, G., Ballée, A., Kirchner, M. A., Moshfegh, P., Herledan, A., Herrmann, A., Deprez, B., Willand, N., Vargiu, A. V., Pos, K. M., Flipo, M., & Hartkoorn, R. C. Pyridylpiperazine-based allosteric inhibitors of RND-type multidrug efflux pumps. Nature Communications,2022, 131: 115. 10.1038/s41467-021-27726-2 

Publications 2018-2021

Deprez-Poulain, R., Schmidt, F., & Lesur, B. Chimie thérapeutique et chémobiologie. Actualité Chimique,2021, 468: 49

Kraupner, N., Dinh, C. P., Wen, X., Landry, V., Herledan, A., Leroux, F., Bosc, D., Charton, J., Maillard, C., Warenghem, S., Duplan, I., Piveteau, C., Hennuyer, N., Staels, B., Deprez, B., & Deprez-Poulain, R. Identification of indole-based activators of insulin degrading enzyme. European Journal of Medicinal Chemistry,2021: 113982.10.1016/j.ejmech.2021.113982.

Deprez, B., Bosc, D., Charton, J., Couturier, C., Deprez-Poulain, R., Flipo, M., Leroux, F., Villemagne, B., & Willand, N. Molecular Design in Practice: A Review of Selected Projects in a French Research Institute That Illustrates the Link between Chemical Biology and Medicinal Chemistry. Molecules,2021, 2619: 6083.10.3390/molecules26196083.

Cantrelle, F.-X., Boll, E., Brier, L., Moschidi, D., Belouzard, S., Landry, V., Leroux, F., Dewitte, F., Landrieu, I., Dubuisson, J., Deprez, B., Charton, J., & Hanoulle, X. NMR spectroscopy of the main protease of SARS-CoV-2 and fragment-based screening identify three protein hotspots and an antiviral fragment. Angewandte Chemie International Edition,2021, in press. 10.1002/anie.202109965.

Wynendaele, E., Furman, C., Wielgomas, B., Larsson, P., Hak, E., Block, T., Van Calenbergh, S., Willand, N., Markuszewski, M., Odell, L. R., Poelarends, G. J., & De Spiegeleer, B. Sustainability in Drug Discovery. Medicine in Drug Discovery,2021:100107.10.1016/j.medidd.2021.100107.

Moureu, S., Caradec, T., Trivelli, X., Drobecq, H., Beury, D., Bouquet, P., Caboche, S., Desmecht, E., Maurier, F., Muharram, G., Villemagne, B., Herledan, A., Hot, D., Willand, N., & Hartkoorn, R. C. Rubrolone production by Dactylosporangium vinaceum: biosynthesis, modulation and possible biological function. Applied Microbiology and Biotechnology,2021, 10513: 5541-5551.10.1007/s00253-021-11404-w.

La, Z., Charton, J., Etienne, L., Bourey, J., & Lipka, E. Supercritical fluid chromatography and liquid chromatography for isomeric separation of a multiple chiral centers analyte. Journal of Chromatography A,2021: 462270.10.1016/j.chroma.2021.462270.

Camberlein, V., Kraupner, N., Bou Karroum, N., Lipka, E., Deprez-Poulain, R., Deprez, B., & Bosc, D. Multi-Component Reaction for the Preparation of 1,5-Disubstituted 1,2,3-Triazoles by In-Situ Generation of Azides and Nickel-Catalyzed Azide-Alkyne Cycloaddition. Tetrahedron Letters,2021: 153131.10.1016/j.tetlet.2021.153131.

Castellanos-Jankiewicz, A., Guzmán-Quevedo, O., Fénelon, V. S., Zizzari, P., Quarta, C., Bellocchio, L., Tailleux, A., Charton, J., Fernandois, D., Henricsson, M., Piveteau, C., Simon, V., Allard, C., Quemener, S., Guinot, V., Hennuyer, N., Perino, A., Duveau, A., Maitre, M., Leste-Lasserre, T., Clark, S., Dupuy, N., Cannich, A., Gonzales, D., Deprez, B., Mithieux, G., Dombrowicz, D., Bäckhed, F., Prevot, V., Marsicano, G., Staels, B., Schoonjans, K., & Cota, D. Hypotamic bile acid-TGR5 signaling protects from obesity. Cell Metabolism,2021, 337: 1483-1492.10.1016/j.cmet.2021.04.009

Hoguet, V., Lasalle, M., Maingot, M., Dequirez, G., Boulahjar, R., Leroux, F., Piveteau, C., Herledan, A., Biela, A., Dumont, J., Chávez-Talavera, O., Belloy, L., Duplan, I., Hennuyer, N., Butruille, L., Lestavel, S., Sevin, E., Culot, M., Gosselet, F., Staels, B., Deprez, B., Tailleux, A., & Charton, J. Beyond the Rule of 5: Impact of PEGylation with Various Polymer Sizes on Pharmacokinetic Properties, Structure–Properties Relationships of mPEGylated Small Agonists of TGR5 Receptor. Journal of Medicinal Chemistry,2021.10.1021/acs.jmedchem.0c01774

Medve, L., Gealageas, R., Lam, B. V., Guillaume, V., Castillo-Aguilera, O., Camberlein, V., Piveteau, C., Rosell, M., Fleau, C., Warenghem, S., Charton, J., Dumont-Ryckembusch, J., Bosc, D., Leroux, F., van Endert, P., Deprez, B., & Deprez-Poulain, R. Modulators of hERAP2 discovered by High-Throughput Screening. Eur. J. Med. Chem.,2020, 211: 113053.10.1016/j.ejmech.2020.113053

Guieu, B., Jourdan, J.-P., Dreneau, A., Willand, N., Rochais, C., & Dallemagne, P. Desirable drug–drug interactions or when a matter of concern becomes a renewed therapeutic strategy. Drug Discovery Today,2020, 10.1016/j.drudis.2020.11.026

Faïon, L., Djaout, K., Frita, R., Pintiala, C., Cantrelle, F.-X., Moune, M., Vandeputte, A., Bourbiaux, K., Piveteau, C., Herledan, A., Biela, A., Leroux, F., Kremer, L., Blaise, M., Tanina, A., Wintjens, R., Hanoulle, X., Déprez, B., Willand, N., Baulard, A. R., & Flipo, M. Discovery of the first Mycobacterium tuberculosis MabA (FabG1) inhibitors through a fragment-based screening. European Journal of Medicinal Chemistry,2020, 200: 112440.10.1016/j.ejmech.2020.112440

Lesire, L., Chaput, L., Cruz De Casas, P., Rousseau, F., Piveteau, C., Dumont, J., Pointu, D., Déprez, B., & Leroux, F. High-Throughput Image-Based Aggresome Quantification. SLAS DISCOVERY: Advancing the Science of Drug Discovery,2020, 257: 783-791.10.1177/2472555220919708

Villemagne, B., Machelart, A., Tran, N. C., Flipo, M., Moune, M., Leroux, F., Piveteau, C., Wohlkönig, A., Wintjens, R., Li, X., Gref, R., Brodin, P., Deprez, B., Baulard, A. R., & Willand, N. Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity. ACS Infect Dis,2020, 6(3): 366-378 .10.1021/acsinfecdis.9b00277

Singh, N., Chaput, L., & Villoutreix, B. O. Virtual screening web servers: designing chemical probes and drug candidates in the cyberspace. Brief Bioinform,2020, 2(2): 1790-1818.10.1093/bib/bbaa034

Lu, Y., Giri, H., Villoutreix, B. O., Ding, Q., Wang, X., & Rezaie, A. R. Gly197Arg mutation in protein C causes recurrent thrombosis in a heterozygous carrier. Journal of Thrombosis and Haemostasis,2020, 18(5): 1141-1153.10.1111/jth.14777

Herledan, A., Andres, M., Lejeune-Dodge, A., Leroux, F., Biela, A., Piveteau, C., Warenghem, S., Couturier, C., Deprez, B., & Deprez-Poulain, R. Drug Target Engagement Using Coupled Cellular Thermal Shift Assay—Acoustic Reverse-Phase Protein Array. SLAS DISCOVERY: Advancing Life Sciences R&D,2020, 25(2): 207–214.10.1177/2472555219897256

Gyulkhandanyan, A., Rezaie, A. R., Roumenina, L., Lagarde, N., Fremeaux-Bacchi, V., Miteva, M. A., & Villoutreix, B. O. Analysis of protein missense alterations by combining sequence- and structure-based methods. Mol Genet Genomic Med,2020: e1166.10.1002/mgg3.1166

Bosc, D., Camberlein, V., Gealageas, R., Castillo-Aguilera, O., Deprez, B., & Deprez-Poulain, R. Kinetic Target-Guided Synthesis: reaching the age of maturity. J. Med. Chem.,2020: 3817−3833.10.1021/acs.jmedchem.9b01183

Valderrama, K., Pradel, E., Firsov, A. M., Drobecq, H., Bauderlique-le Roy, H., Villemagne, B., Antonenko, Y. N., & Hartkoorn, R. C. Pyrrolomycins Are Potent Natural Protonophores. Antimicrob. Agents Chemother.,2019, 63(10): e01450-01419. 10.1128/AAC.01450-19

Willand, N., Flipo, M., Villemagne, B., Baulard, A., & Deprez, B. 2019. Chapter Five – Recent advances in the design of inhibitors of mycobacterial transcriptional regulators to boost thioamides anti-tubercular activity and circumvent acquired-resistance. In K. Chibale (Ed.), Annual Reports in Medicinal Chemistry, Vol. 52: 131-152: Academic Press. 10.1016/bs.armc.2019.06.003

Lagarde, N., Goldwaser, E., Pencheva, T., Jereva, D., Pajeva, I., Rey, J., Tuffery, P., Villoutreix, B. O., & Miteva, M. A. A Free Web-Based Protocol to Assist Structure-Based Virtual Screening Experiments. Int. J. Mol. Sci.,2019, 20(18): 4648.10.3390/ijms20184648

Sartori, M., Mendes, T., Desai, S., Lasorsa, A., Herledan, A., Malmanche, N., Mäkinen, P., Marttinen, M., Malki, I., Chapuis, J., Flaig, A., Vreulx, A.-C., Ciancia, M., Amouyel, P., Leroux, F., Deprez, B., Cantrelle, F.-X., Maréc, D., Pradier, L., Hiltunen, M., Landrieu, I., Kilinc, D., Herault, Y., Laporte, J., & Lambert, J.-C. BIN1 recovers tauopathy-induced long-term memory deficits in mice and interacts with Tau through Thr348 phosphorylation. Acta Neuropathol. (Berl).2019, 138(4): 631-652.10.1007/s00401-019-02017-9

Leroux, F., Bosc, D., Beghyn, T., Hermant, P., Warenghem, S., Landry, V., Pottiez, V., Guillaume, V., Charton, J., Herledan, A., Urata, S., Liang, W., Sheng, L., Tang, W.-J., Deprez, B., & Deprez-Poulain, R. Identification of ebselen as a potent inhibitor of insulin degrading enzyme by a drug repurposing screening. Eur. J. Med. Chem.,2019, 179: 557-566.10.1016/j.ejmech.2019.06.057

Prevet, H., Moune, M., Tanina, A., Kemmer, C., Herledan, A., Frita, R., Wohlkönig, A., Bourotte, M., Villemagne, B., Leroux, F., Gitzinger, M., Baulard, A. R., Déprez, B., Wintjens, R., Willand, N., & Flipo, M. A fragment-based approach towards the discovery of N-substituted tropinones as inhibitors of Mycobacterium tuberculosis transcriptional regulator EthR2. Eur. J. Med. Chem.,2019, 167: 426-438.10.1016/j.ejmech.2019.02.023

Colin, B., Deprez, B., & Couturier, C. High-throughput DNA plasmid transfection using acoustic droplet ejection technology. SLAS Discovery,2019, 24(4): 492-500.10.1177/2472555218803064

Tanina, A., Wohlkönig, A., Soror, S. H., Flipo, M., Villemagne, B., Prevet, H., Déprez, B., Moune, M., Perée, H., Meyer, F., Baulard, A. R., Willand, N., & Wintjens, R. A comprehensive analysis of the protein-ligand interactions in crystal structures of Mycobacterium tuberculosis EthR. Biochimica et Biophysica Acta (BBA) – Proteins and Proteomics,2019, 1867(3): 248-258.10.1016/j.bbapap.2018.12.003

Colin, B., Rocq, N., Deprez, B., & Couturier, C. High-Throughput DNA Plasmid Multiplexing and Transfection Using Acoustic Nanodispensing Technology. J. Vis. Exp.,2019, 150: e59570.10.3791/59570

Machelart, A., Salzano, G., Li, X., Demars, A., Debrie, A.-S., Menendez-Miranda, M., Pancani, E., Jouny, S., Hoffmann, E., Deboosere, N., Belhaouane, I., Rouanet, C., Simar, S., Talahari, S., Giannini, V., Villemagne, B., Flipo, M., Brosch, R., Nesslany, F., Deprez, B., Muraille, E., Locht, C., Baulard, A. R., Willand, N., Majlessi, L., Gref, R., & Brodin, P. Intrinsic Antibacterial Activity of Nanoparticles Made of β-Cyclodextrins Potentiates Their Effect as Drug Nanocarriers against Tuberculosis. ACS Nano,2019, 13(4): 3992-4007.10.1021/acsnano.8b07902

Pastor, A., Machelart, A., Li, X., Willand, N., Baulard, A., Brodin, P., Gref, R., & Desmaële, D. A novel codrug made of the combination of ethionamide and its potentiating booster: synthesis, self-assembly into nanoparticles and antimycobacterial evaluation. Org. Biomol. Chem.,2019, 17(20): 5129-5137.10.1039/C9OB00680J

Prieri, M., Frita, R., Probst, N., Sournia-Saquet, A., Bourotte, M., Déprez, B., Baulard, A. R., & Willand, N. Efficient analoging around ethionamide to explore thioamides bioactivation pathways triggered by boosters in Mycobacterium tuberculosis. Eur. J. Med. Chem.,2018, 159: 35-46.10.1016/j.ejmech.2018.09.038

Zhang, Z., Liang, W. G., Bailey, L. J., Tan, Y. Z., Wei, H., Wang, A., Farcasanu, M., Woods, V. A., McCord, L. A., Lee, D., Shang, W., Deprez-Poulain, R., Deprez, B., Liu, D. R., Koide, A., Koide, S., Kossiakoff, A. A., Li, S., Carragher, B., Potter, C. S., & Tang, W.-J. Ensemble cryoEM elucidates the mechanism of insulin capture and degradation by human insulin degrading enzyme. eLife,2018, 7: e33572. 10.7554/eLife.33572

Hoguet, V., Charton, J., Hecquet, P.-E., Lakhmi, C., & Lipka, E. Supercritical fluid chromatography versus high performance liquid chromatography for enantiomeric and diastereoisomeric separations on coated polysaccharides-based stationary phases: Application to dihydropyridone derivatives. J. Chromatogr. A,2018, 1549: 39-50.10.1016/j.chroma.2018.03.035

Kussau, T., Flipo, M., Van Wyk, N., Viljoen, A., Olieric, V., Kremer, L., & Blaise, M. Structural rearrangements occurring upon cofactor binding in the Mycobacterium smegmatis beta-ketoacyl-acyl carrier protein reductase MabA. Acta crystallographica. Section D, Structural biology,2018, 74(Pt 5): 383-393. 10.1107/s2059798318002917

Hering, Y., Berthier, A., Duez, H., Lefebvre, P., Deprez, B., Gribbon, P., Wolf, M., Reinshagen, J., ley, F., Hannemann, J., Böger, R., Staels, B., & Gul, S. Development and implementation of a cell-based assay to discover agonists of the nuclear receptor REV-ERBα. 2018,2018. 10.14440/jbm.2018.244

Publications 2013-2017

Wohlkönig, A., Remaut, H., Moune, M., Tanina, A., Meyer, F., Desroses, M., Steyaert, J., Willand, N., Baulard, A. R., & Wintjens, R. Structural analysis of the interaction between spiroisoxazoline SMARt-420 and the Mycobacterium tuberculosis repressor EthR2. Biochem. Biophys. Res. Commun.,2017, 487(2): 403-408.10.1016/j.bbrc.2017.04.074

Tatum, N. J., Liebeschuetz, J. W., Cole, J. C., Frita, R., Herledan, A., Baulard, A. R., Willand, N., & Pohl, E. New active leads for tuberculosis booster drugs by structure-based drug discovery. Org. Biomol. Chem.,2017, 15(48): 10245-10255.10.1039/C7OB00910K

Salzano, G., Wankar, J., Ottani, S., Villemagne, B., Baulard, A. R., Willand, N., Brodin, P., Manet, I., & Gref, R. Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs. Int. J. Pharm.,2017, 531(2): 577-587.10.1016/j.ijpharm.2017.05.030

Montaigne, D., Marec, X., Modine, T., Coisne, A., Mouton, S., Fayad, G., Ninni, S., Klein, C., Ortmans, S., Seunes, C., Potelle, C., Berthier, A., Gheeraert, C., Piveteau, C., Deprez-Poulain, R., Eeckhoute, J., Duez, H., Lacroix, D., Deprez, B., Jegou, B., Koussa, M., Edme, J. L., Lefebvre, P., & Staels, B. Daytime variation of perioperative myocardial injury in cardiac surgery and its prevention by Rev-Erbalpha antagonism: a single-centre propensity-matched cohort study and a randomised study. Lancet,2017 391(10115): 59–69 .10.1016/s0140-6736(17)32132-3

Hermant, P., Bosc, D., Piveteau, C., Gealageas, R., Lam, B. V., Ronco, C., Roignant, M., Tolajanahary, H., Jean, L., Renard, P.-Y., Lemdani, M., Bourotte, M., Herledan, A., Bedart, C., Biela, A., Leroux, F., Deprez, B., & Deprez-Poulain, R. Controlling Plasma Stability of Hydroxamic Acids: A MedChem Toolbox. Journal of Medicinal Chemistry,2017, 60(21): 9067–9089. 10.1021/acs.jmedchem.7b01444

Costa-Gouveia, J., Pancani , E., Jouny, S., Machelart, A., Delorme, V., Salzano, G., Iantomasi, R., Piveteau, C., Queval, C., Song, O.-R., Flipo, M., Deprez, B., Saint-André, J.-P., Hureaux, J., Majlessi, L., Willand, N., Baulard, A., Brodin, P., & Gref, R. Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles. Scientific Reports,2017, 7: Article number: 5390 10.1038/s41598-017-05453-3

Dequirez, G., Bourotte, M., Porras de Francisco, E., Remuiñan, Blanco, M. J., Deprez, B., & Willand, N. Microwave-Assisted Suzuki-Miyaura Cross Coupling using Nickel as Catalyst to Rapidly Access to 3-Arylazetidine. ChemistrySelect,2017, 2(28): 8841-8846.10.1002/slct.201702101. 10.1002/slct.201702101

Boiteau, J.-G., Ouvry, G., Arlabosse, J.-M., Astri, S., Beillard, A., Bhurruth-Alcor, Y., Bonnary, L., Bouix-Peter, C., Bouquet, K., Bourotte, M., Cardinaud, I., Comino, C., Deprez, B., Duvert, D., Féret, A., Hacini-Rachinel, F., Harris, C. S., Luzy, A.-P., Mathieu, A., Millois, C., Orsini, N., Pascau, J., Pinto, A., Piwnica, D., Polge, G., Reitz, A., Reversé, K., Rodeville, N., Rossio, P., Spiesse, D., Tabet, S., Taquet, N., Tomas, L., Vial, E., & Hennequin, L. F. Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis. Bioorganic & Medicinal Chemistry,2017, 264: 945-956. 10.1016/j.bmc.2017.07.054

Lasalle, M., Hoguet, V., Hennuyer, N., Leroux, F., Piveteau, C., Belloy, L., Lestavel, S., Vallez, E., Dorchies, E., Duplan, I., Sevin, E., Culot, M., Gosselet, F., Boulahjar, R., Herledan, A., Staels, B., Deprez, B., Tailleux, A., & Charton, J. Topical Intestinal Aminoimidazole Agonists of G-Protein-Coupled Bile Acid Receptor 1 Promote Glucagon Like Peptide-1 Secretion and Improve Glucose Tolerance. Journal of Medicinal Chemistry,2017, 60(10): 4185-4211. 10.1021/acs.jmedchem.6b01873

Delplanques, T., Boulahjar, R., Charton, J., Houze, C., Howsam, M., Servais, A.-C., Fillet, M., & Lipka, E. Single and dual cyclodextrins systems for the enantiomeric and diastereoisomeric separations of structurally related dihydropyridone analogues. Electrophoresis 2017, 38(15): 1922-1931.10.1002/elps.201600536

Blondiaux, N., Moune, M., Desroses, M., Frita, R., Flipo, M., Mathys, V., Soetaert, K., Kiass, M., Delorme, V., Djaout, K., Trebosc, V., Kemmer, C., Wintjens, R., Wohlkönig, A., Antoine, R., Huot, L., Hot, D., Coscolla, M., Feldmann, J., Gagneux, S., Locht, C., Brodin, P., Gitzinger, M., Déprez, B., Willand, N., & Baulard, A. R. Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420. Science,2017, 355(6330): 1206-1211. http://dx.doi.org/10.1126/science.aag1006

Wohlkönig, A., Remaut, H., Moune, M., Tanina, A., Meyer, F., Desroses, M., Steyaert, J., Willand, N., Baulard, A. R., & Wintjens, R. Structural analysis of the interaction between spiroisoxazoline SMARt-420 and the Mycobacterium tuberculosis repressor EthR2. Biochemical and Biophysical Research Communications,2017, 487(2): 403-408.http://dx.doi.org/10.1016/j.bbrc.2017.04.074

Mpakali, A., Giastas, P., Deprez-Poulain, R., Papakyriakou, A., Koumantou, D., Gealageas, R., Tsoukalidou, S., Vourloumis, D., Mavridis, I. M., Stratikos, E., & Saridakis, E. Crystal Structures of ERAP2 Complexed with Inhibitors Reveal Pharmacophore Requirements for Optimizing Inhibitor Potency. ACS Medicinal Chemistry Letters,2017, 8(3): 333-337.http://dx.doi.org/10.1021/acsmedchemlett.6b00505

Ouvry, G., Berton, Y., Bhurruth-Alcor, Y., Bonnary, L., Bouix-Peter, C., Bouquet, K., Bourotte, M., Chambon, S., Comino, C., Deprez, B., Duvert, D., Duvert, G., Hacini-Rachinel, F., Harris, C. S., Luzy, A.-P., Mathieu, A., Millois, C., Pascau, J., Pinto, A., Polge, G., Reitz, A., Reversé, K., Rosignoli, C., Taquet, N., & Hennequin, L. F. Identification of novel TACE inhibitors compatible with topical application. Bioorganic & Medicinal Chemistry Letters,2017, 278: 1848-1853.doi.org/10.1016/j.bmcl.2017.02.035.

Chapuis, J., Flaig, A., Grenier-Boley, B., Eysert, F., Pottiez, V., Deloison, G., Vandeputte, A., Ayral, A.-M., Mendes, T., Desai, S., Goate, A. M., Kauwe, J. S. K., Leroux, F., Herledan, A., Demiautte, F., Bauer, C., Checler, F., Petersen, R. C., Blennow, K., Zetterberg, H., Minthon, L., Van Deerlin, V. M., Lee, V. M.-Y., Shaw, L. M., Trojanowski, J. Q., Albert, M., Moghekar, A., O’Brien, R., Peskind, E. R., Malmanche, N., Schellenberg, G. D., Dourlen, P., Song, O.-R., Cruchaga, C., Amouyel, P., Deprez, B., Brodin, P., & Lambert, J.-C. Genome-wide, high-content siRNA screening identifies the Alzheimer’s genetic risk factor FERMT2 as a major modulator of APP metabolism. Acta Neuropathologica,2016. http://dx.doi.org/1-12.10.1007/s00401-016-1652-z

Bauters, D., Scroyen, I., Deprez-Poulain, R., & Lijnen, H. R. ADAMTS5 promotes murine adipogenesis and visceral adipose tissue expansion. Thromb Haemost,2016, 116(4). http://dx.doi.org/10.1160/th16-01-0015

Prevet, H., Flipo, M., Roussel, P., Deprez, B., & Willand, N. Microwave-assisted synthesis of functionalized spirohydantoins as 3-D privileged fragments for scouting the chemical space. Tetrahedron Letters,2016, 57(26): 2888-2894.http://dx.doi.org/10.1016/j.tetlet.2016.05.065

Letronne, F., Laumet, G., Ayral, A. M., Chapuis, J., Demiautte, F., Laga, M., Vandenberghe, M. E., Malmanche, N., Leroux, F., Eysert, F., Sottejeau, Y., Chami, L., Flaig, A., Bauer, C., Dourlen, P., Lesaffre, M., Delay, C., Huot, L., Dumont, J., Werkmeister, E., Lafont, F., Mendes, T., Hansmannel, F., Dermaut, B., Deprez, B., Herard, A. S., Dhenain, M., Souedet, N., Pasquier, F., Tulasne, D., Berr, C., Hauw, J. J., Lemoine, Y., Amouyel, P., Mann, D., Deprez-Poulain, R., Checler, F., Hot, D., Delzescaux, T., Gevaert, K., & Lambert, J. C. ADAM30 Downregulates APP-Linked Defects Through Cathepsin D Activation in Alzheimer’s Disease. EBioMedicine,2016, 9: 278–292. http://dx.doi.org/10.1016/j.ebiom.2016.06.002 OPEN ACCESS

Probst, N. P., Deprez, B., & Willand, N. Palladium-free Sonogashira-type cross-coupling reaction of bromoisoxazolines or N-alkoxyimidoyl bromides and alkynes. Tetrahedron Letters,2016, 57(10): 1066-1070. http://dx.doi.org/10.1016/j.tetlet.2016.01.070

Bosc, D., Jakhlal, J., Deprez, B., & Deprez-Poulain, R. Kinetic target-guided synthesis in drug discovery and chemical biology: a comprehensive facts and figures survey. Future Medicinal Chemistry,2016, 84: 381-404. http://dx.doi.org/10.4155/fmc-2015-0007 OPEN ACCESS

Broeders, E. M., Nascimento, E. M., Havekes, B., Brans, B., Roumans, K. M., Tailleux, A., Schaart, G., Kouach, M., Charton, J., Deprez, B., Bouvy, N., Mottaghy, F., Staels, B., van Marken Lichtenbelt, W. D., & Schrauwen, P. The Bile Acid Chenodeoxycholic Acid Increases Human Brown Adipose Tissue Activity. Cell Metabolism,2015, 22(3): 418-426. http://dx.doi.org/10.1016/j.cmet.2015.07.002

Deprez-Poulain, R., Natie, H., Bosc, D., Liang, W. G., Enee, E., Marec, X., Julie, C., Totobenazara, J., Berte, G., Jahklal, J., Verdelet, T., Dumont, J., Dassonneville, S., Woitrain, E., Gauriot, M., Paquet, C., Duplan, I., Hermant, P., Cantrelle, F.-X., Sevin, E., Culot, M., Landry, V., Herledan, A., Piveteau, C., Lippens, G., Florence, L., Tang, W. J., Van Endert, P., Staels, B., & Deprez, B. Catalytic site inhibition of insulin-degrading enzyme by a small molecule induces glucose intolerance in mice. Nature Communications,2015, 6. http://dx.doi.org/10.1038/ncomms9250 OPEN ACCESS

Henninot, A., Terrier, A., Charton, J., Urbain, R., Fontayne, A., Deprez, B., & Beghyn, T. Characterization of monoclonal antibodies by a fast and easy LC- MS ToF analysis on culture supernatant. Analytical Biochemistry,2015, 491: 52-54. http://dx.doi.org/10.1016/j.ab.2015.08.006

Tran, N. C., Dhondt, H., Flipo, M., Deprez, B., & Willand, N. Synthesis of functionalized 2-isoxazolines as three-dimensional fragments for fragment-based drug discovery. Tetrahedron Letters,2015, 56(27): 4119-4123. http://dx.doi.org/10.1016/j.tetlet.2015.05.035

Bonner, C., Kerr-Conte, J., Gmyr, V., Queniat, G., Moerman, E., Thevenet, J., NBeaucamps, C., Delalleau, N., Popescu, I., Malaisse, W., Sener, A., Deprez, B., Abderrahmani, A., Staels, B., & Pattou, F. Inhibition of the glucose transporter SGLT2 with dapagliflozin in pancreatic alpha cells triggers glucagon secretion. Nature Medicine,2015, 21: 512-517. http://dx.doi.org/10.1038/nm.3828

Lasalle, M., Picon, S., Boulahjar, R., Hoguet, V., Van Obbergen, J., Roussel, P., Deprez, B., & Charton, J. Access to newly functionalized imidazole derivatives: efficient synthesis of novel 5-amino-2-thioimidazoles using propylphosphonic anhydride (®T3P). Tetrahedron Letters,2015, 56(8): 1011-1014. http://dx.doi.org/10.1016/j.tetlet.2015.01.046

Charton, J., Gauriot, M., Totobenazara, J., Hennuyer, N., Dumont, J., Bosc, D., Marec, X., Elbakali, J., Herledan, A., Wen, X., Ronco, C., Gras-Masse, H., Heninot, A., Pottiez, V., Landry, V., Staels, B., Liang, W. G., Leroux, F., Tang, W. J., Deprez, B., & Deprez-Poulain, R. Structure-activity relationships of Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, dual binders of human Insulin-Degrading Enzyme. Eur J Med Chem. 90: 547-567 http://dx.doi.org/10.1016/j.ejmech.2014.12.005

Corbel, C., Zhang, B., Le Parc, A., Baratte, B., Colas, P., Couturier, C., Kosik, K. S., Landrieu, I., Le Tilly, V., & Bach, S. Tamoxifen Inhibits CDK5 Kinase Activity by Interacting with p35/p25 and Modulates the Pattern of Tau Phosphorylation. Chemistry & Biology,2015, 22(4): 482.http://dx.doi.org/10.1016/j.chembiol.2015.03.009

Karrout, Y., Dubuquoy, L., Piveteau, C., Siepmann, F., Moussa, E., Wils, D., Beghyn, T., Neut, C., Flament, M. P., Guerin-Deremaux, L., Dubreuil, L., Deprez, B., Desreumaux, P., & Siepmann, J. In vivo efficacy of microbiota-sensitive coatings for colon targeting: A promising tool for IBD therapy. Journal of Controlled Release,2015, 197: 121-130. http://dx.doi.org/ 10.1016/ j.jconrel. 2014.11.006

Elbakali, J., Gras, H., Maingot, L., Deprez, B., Dumont, J., Leroux, F., & Deprez-Poulain, R. Inhibition of aggrecanase as a therapeutic strategy in osteoarthritis. Future Medicinal Chemistry,2014, 6(12): 1399-1412. 10.4155/FMC.14.84

Mathieu, A. L., Sperandio, O., Pottiez, V., Balzarin, S., Herledan, A., Elkaim, J. O., Fogeron, M. L., Piveteau, C., Dassonneville, S., Deprez, B., Villoutreix, B. O., Bonnefoy, N., & Leroux, F. Identification of Small Inhibitory Molecules Targeting the Bfl-1 Anti-Apoptotic Protein That Alleviates Resistance to ABT-737. J Biomol Screen,2014, 19(7): 1035-1046. 10.1177/1087057114534070

Villemagne, B., Flipo, M., Blondiaux, N., Crauste, C., Malaquin, S., Leroux, F., Piveteau, C., Villeret, V., Brodin, P., Villoutreix, B. O., Sperandio, O., Soror, S. H., Wohlkonig, A., Wintjens, R., Deprez, B., Baulard, A. R., & Willand, N. Ligand efficiency driven design of new inhibitors of Mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging and linking approaches. Journal of Medicinal Chemistry,2014 57(11): 4876-4888.10.1021/jm500422b

Charton, J., Gauriot, M., Guo, Q., Hennuyer, N., Marec, X., Dumont, J., Hamdane, M., Pottiez, V., Landry, V., Sperandio, O., Flipo, M., Buee, L., Staels, B., Leroux, F., Tang, W.-J., Deprez, B., & Deprez-Poulain, R. Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-b hydrolysis. European Journal of Medicinal Chemistry,2014, 79, 184-193. 10.1016/j.ejmech.2014.04.009

Crauste, C., Willand, N., Villemagne, B., Flipo, M., Willery, E., Carette, X., Moune Dimala, M., Drucbert, A. S., Danze, P. M., Deprez, B., & Baulard, A. Unconventional Surface Plasmon Resonance signals reveal quantitative inhibition of transcriptional repressor EthR by synthetic ligands. Analytical Biochemistry,2014, 452: 54–66. 10.1016/j.ab.2014.02.011

Malaquin, S., Jida, M., Courtin, J., Laconde, G., Willand, N., Deprez, B., & Deprez-Poulain, R. Water-based conditions for the microscale parallel synthesis of bicyclic lactams. Tetrahedron Letters,2013, 54(6): 562–567. 10.1016/j.tetlet.2012.11.082

 

Maingot, L., Elbakali, J., Dumont, J., Bosc, D., Cousaert, N., Urban, A., Deglane, G., Villoutreix, B., Nagase, H., Sperandio, O., Leroux, F., Deprez, B., & Deprez-Poulain, R. Aggrecanase-2 Inhibitors Based on the Acylthiosemicarbazide Zinc-Binding Group. Eur J Med Chem,2013, 69: 244–261. 10.1016/j.ejmech.2013.08.027

Wiśniewski, K., Finnman, J., Flipo, M., Galyean, R., & Schteingart, C. D. On the mechanism of degradation of oxytocin and its analogues in aqueous solution. Biopolymers (Peptide Science),2013, 100(4): 408–421. 10.1002/bip.22260

Tatum, N. J., Villemagne, B., Willand, N., Deprez, B., Liebeschuetz, J. W., Baulard, A. R., & Pohl, E. Structural and docking studies of potent ethionamide boosters. Acta Crystallographica Section C,2013, 69(11): 1243–1250. 10.1107/S0108270113028126

Couturier, C., & Deprez, B. Setting up a Bioluminescence Resonance Energy Transfer high throughput screening assay to search for protein/protein interaction inhibitors in mammalian cells. Frontiers in Endocrinology,2013, 3: 100. 10.3389/fendo.2012.00100

Lipka, E., Charton, J., & Vaccher, C. Development of HPLC/fluorescence detection method for chiral resolution of dansylated benzimidazoles derivatives. Biomedical Chromatography,2013, 28(1): 4–9. 10.1002/bmc.2992

Publications 2008-2012

Bousquet, T., Jida, M., Soueidan, M., Deprez-Poulain, R., Agbossou-Niedercorn, F., & Pelinski, L. Fast and Efficient solvent-free Passerini reaction. Tetrahedron Letters,2012, 53(3): 306–308. 10.1016/j.tetlet.2011.11.028

Aknin, K., Gauriot, M., Totobenazara, J., Deguine, N., Deprez-Poulain, R., Deprez, B., & Charton, J. Squaric acid is a suitable building-block in 4C-Ugi reaction: access to original bivalent compounds. Tetrahedron Letters,2012, 53: 458–461. 10.1016/j.tetlet.2011.11.077

Carette, X., Blondiaux, N., Willery, E., Hoos, S., Lecat-Guillet, N., Lens, Z., Wohlkonig, A., Wintjens, R., Soror, S., Frenois, F., Dirié, B., Villeret, V., England, P., Lippens, G., Deprez, B., Locht, C., Willand, N., & Baulard, A. Structural activation of the transcriptional repressor EthR from M.tuberculosis by single amino-acid change mimicking natural and synthetic ligands Nucleic Acids Res,2012, 40(7): 3018–3030. 10.1093/nar/gkr1113

Flipo, M., Desroses, M., Lecat-Guillet, N., Villemagne, B., Blondiaux, N., Leroux, F., Piveteau, C., Mathys, V., Flament, M.-P., Siepmann, J., Villeret, V., Wohlkönig, A., Wintjens, R., Soror, S. H., Christophe, T., Jeon, H. K., Locht, C., Brodin, P., Deprez, B., Baulard, A. R., & Willand, N. Ethionamide Boosters. 2. Combining Bioisosteric Replacement and Structure-Based Drug Design To Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors. Journal of Medicinal Chemistry,2012, 55(1): 68–83. 10.1021/jm200825u

Beghyn, T., Julie, C., Leroux, F., Henninot, A., Reboule, I., Cos, P., Maes, L., & Deprez, B. P. Drug-to-Genome-to-Drug, Step 2: Reversing Selectivity in a Series of Antiplasmodial Compounds. Journal of Medicinal Chemistry,2012, 55(3): 1274–1286. 10.1021/jm201422e

Elbakali, J., Maingot, L., Dumont, J., Host, H., Hocine, A., Cousaert, N., Dassonneville, S., Leroux, F., Deprez, B., & Deprez-Poulain, R. Novel Selective Inhibitors of Neutral Endopeptidase: Discovery by Screening and Hit-to-Lead Optimisation. Med.Chem.Comm.,2012, 3: 469–474. 10.1039/C2MD00287F

Wen, X., Bakali, J. E., Deprez-Poulain, R., & Deprez, B. Efficient propylphosphonic anhydride (®T3P) mediated synthesis of benzothiazoles, benzoxazoles and benzimidazoles. Tetrahedron Letters,2012, 53(19): 2440–2443. 10.1016/j.tetlet.2012.03.007

Villemagne, B., Crauste, C., Flipo, M., Baulard, A. R., Deprez, B., & Willand, N. Tuberculosis: The drug development pipeline at a glance. European Journal of Medicinal Chemistry,2012, 51: 1–16. 10.1016/j.ejmech.2012.02.033

Jida, M., & Deprez, B. Friedlander synthesis of polysubstituted quinolines and naphthyridines promoted by propylphosphonic anhydride (T3PR) under mild conditions. New Journal of Chemistry,2012, 36(4): 869–873 10.1039/C2NJ21043F

Jida, M., Soueidan, O.-M., Deprez, B., Laconde, G., & Deprez-Poulain, R. Racemic and diastereoselective construction of indole alkaloids under solvent- and catalyst-free microwave-assisted Pictet-Spengler condensation. Green Chemistry,2012, 14(4): 909–911 10.1039/C2GC16596A

Flipo, M., Willand, N., Lecat-Guillet, N., Hounsou, C., Desroses, M., Leroux, F., Lens, Z., Villeret, V., Wohlkönig, A., Wintjens, R., Christophe, T., Jeon, H. K., Locht, C., Brodin, P., Baulard, A., & Deprez, B. Discovery of novel N-phenyl-phenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining High-Throughput Screening and Synthesis. Journal of Medicinal Chemistry,2012, 55(14): 6391–6402. 10.1021/jm300377g

Jida, M., Laconde, G., Soueidan, O.-M., Lebegue, N., Revelant, G., Pelinski, L., Agbossou-Niedercorn, F., Deprez, B., & Deprez-Poulain, R. Stereoselective synthesis of enantiopure N-protected-3-arylpiperazines from keto-esters. Tetrahedron Letters,2012, 53(39): 5215–5218. 10.1016/j.tetlet.2012.07.031

Gonzalez, S., Beghyn, T., Jia, J., Debreuck, N., Berte, G., Mamchaoui, K., Mouly, V., Gruenert, D., Deprez, B., & Lejeune, F. Rescue of nonsense mutations by amlexanox in human cells. Orphanet Journal of Rare Diseases,2012, 7(1): 58. 10.1186/1750-1172-7-58

Deprez, B. Sciences chimiques et sciences de la vie : une coalescence prometteuse pour la pharmacie. L’actualité chimique,2012, 369: 5–7

Deprez-Poulain, R., Flipo, M., Piveteau, C., Leroux, F., Dassonneville, S., Florent, I., Maes, L., Cos, P., & Deprez, B. Structure-Activity Relationships and Blood Distribution of Antiplasmodial Aminopeptidase-1 Inhibitors. Journal of Medicinal Chemistry,2012, 55(24): 10909–10917. 10.1021/jm301506h

Zhang, B., Corbel, C., Gueritte, F., Couturier, C., Bach, S., & Tan, V. An in silico approach for the discovery of CDK5/p25 interaction inhibitors. . Biotechnol J. ,2011 6(7): 871–881. 10.1002/biot.201100139

Jida, M., Soueidan, M., Willand, N., Agbossou-Niedercorn, F., Pelinski, L., Laconde, G., Deprez-Poulain, R., & Deprez, B. A facile and rapid synthesis of N-benzyl-2-substituted piperazines. Tetrahedron Letters,2011, 52(14): 1705–1708. 10.1016/j.tetlet.2011.02.011

Beghyn, T. B., Charton, J., Leroux, F., Laconde, G., Bourin, A., Cos, P., Maes, L., & Deprez, B. Drug to Genome to Drug: Discovery of New Antiplasmodial Compounds. Journal of Medicinal Chemistry,2011, 54(9): 3222–3240. 10.1021/jm1014617

Flipo, M., Desroses, M., Lecat-Guillet, N., Dirié, B., Carette, X., Leroux, F., Piveteau, C., Demirkaya, F., Lens, Z., Rucktooa, P., Villeret, V., Christophe, T., Jeon, H. K., Locht, C., Brodin, P., Déprez, B., Baulard, A. R., & Willand, N. Ethionamide Boosters: Synthesis, Biological Activity, and Structure-Activity Relationships of a Series of 1,2,4-Oxadiazole EthR Inhibitors. Journal of Medicinal Chemistry,2011, 54(8): 2994–3010. 10.1021/jm200076a

Bonnel, D., Legouffe, R., Willand, N., Baulard, A., Hamm, G., Deprez, B., & Stauber, J. MALDI imaging techniques dedicated to drug-distribution studies. Bioanalysis,2011, 3(12): 1399–1406. 10.4155/bio.11.88

Deprez-Poulain, R., Cousaert, N., Toto, P., Willand, N., & Deprez, B. Application of Ullmann and Ullmann-Finkelstein reactions for the synthesis of N-aryl-N-(1H-pyrazol-3-yl) acetamide or N-(1-aryl-1H-pyrazol-3-yl) acetamide derivatives and pharmacological evaluation. . Eur J Med Chem,2011, 46: 3867–3876. 10.1016/j.ejmech.2011.05.056

Corbel, C., Wang, Q., Bousserouel, H., Hamdi, A., Zhang, B., Lozach, O., Ferandin, Y., Tan, V., Gueritte, F., Colas, P., Couturier, C., & Bach, S. First BRET-based screening assay performed in budding yeast leads to the discovery of CDK5/p25 interaction inhibitors. Biotechnol J.,2011, 6(7): 860–870. 10.1002/biot.201100138

Seron, K., Couturier, C., Belouzard, S., Bacart, J., Monte, D., Corset, L., Bocquet, O., Dam, J., Vauthier, V., Lec Oelig Ur, C., Bailleul, B., Hoflack, B., Froguel, P., Jockers, R., & Rouille, Y. Endospanins regulate a postinternalization step of the leptin receptor endocytic pathway. . Journal of Biological Chemistry,2011, (286): 17968–17981. 10.1074/jbc.m111.224857

Soueidan, M., Jida, M., Bousquet, T., Niedercorn, F. A., & Pelinski, L. Efficient access to new chiral ferrocenyl [gamma]-lactams from amino alcohols. New Journal of Chemistry,2011, 35(5): 991–993. 10.1039/C1NJ20059C

Grellier, E., Lecolle, K., Rogee, S., Couturier, C., D’Halluin, J.-C., Hong, S.-S., Fender, P., Boulanger, P., Quesnel, B., & Colin, M. A fiber-modified adenoviral vector interacts with immunoevasion molecules of the B7 family at the surface of murine leukemia cells derived from dormant tumors. Molecular Cancer,2011, 10(1): 105. 10.1186/1476-4598-10-105

Willand, N., Desroses, M., Toto, P., Dirie, B., Lens, Z., Villeret, V., Rucktooa, P., Locht, C., Baulard, A., & Deprez, B. Exploring Drug Target Flexibility Using in Situ Click Chemistry: Application to a Mycobacterial Transcriptional Regulator. ACS Chemical Biology,2010, 5(11): 1007–1013. http://dx.doi.org/10.1021/cb100177g

Maingot, L., Leroux, F., Landry, V., Dumont, J., Nagase, H., Villoutreix, B., Sperandio, O., Deprez-Poulain, R., & Deprez, B. New non-hydroxamic ADAMTS-5 inhibitors based on the 1,2,4-triazole-3-thiol scaffold. Bioorganic & Medicinal Chemistry Letters,2010, 21: 6213-6216. http://dx.doi.org/10.1016/j.bmcl.2010.08.108

Jida, M., Malaquin, S., Deprez-Poulain, R., Laconde, G., & Deprez, B. Synthesis of five- and six-membered lactams via solvent-free microwave Ugi reaction. Tetrahedron Letters,2010, 51(39): 5109-5111. http://dx.doi.org/10.1016/j.tetlet.2010.07.021

Lipka, E., Folly-Klana, M., Charton, J., Vaccher, M.-P., Bonte, J.-P., & Vaccher, C. Determination of pKa values of benzimidazole derivatives from mobility obtained by capillary electrophoresis. Journal of Pharmaceutical and Biomedical Analysis,2010, 53: 1267-1271. http://dx.doi.org/10.1016/j.jpba.2010.07.023

Malaquin, S., Jida, M., Gesquiere, J.-C., Deprez-Poulain, R., Deprez, B., & Laconde, G. Ugi reaction for the synthesis of 4-aminopiperidine-4-carboxylic acid derivatives. Application to the synthesis of carfentanil and remifentanil. Tetrahedron Letters,2010, 51(22): 2983-2985. http://dx.doi.org/10.1016/j.tetlet.2010.03.120

Jida, M., Deprez-Poulain, R., Malaquin, S., Roussel, P., Agbossou-Niedercorn, F., Deprez, B., & Laconde, G. Solvent-free microwave-assisted Meyers’ lactamization. Green Chemistry,2010, 12: 961 – 964. http://dx.doi.org/10.1039/B924111F

Reynes, C., Host, H., Camproux, A.-C., Laconde, G., Leroux, F., Mazars, A., Deprez, B., Fahraeus, R., Villoutreix, B. O., & Sperandio, O. Designing Focused Chemical Libraries Enriched in Protein-Protein Interaction Inhibitors using Machine-Learning Methods. Plos Computational Biology,2010, 6(3): e1000695. http://dx.doi.org/10.1371/journal.pcbi.1000695

Flipo, M., Charton, J., Hocine, A., Dassonneville, S., Deprez, B., & Deprez-Poulain, R. Hydroxamates: Relationships between structure and plasma-stability. J Med Chem,2009, 52(21): 6790-6802. http://dx.doi.org/10.1021/jm900648x

Willand, N., Dirié, B., Carette, X., Bifani, P., Sing, A., Desroses, M., Leroux, F., Déprez-Poulain, R., Frénois, F., Aumercier, M., Locht, C., Villeret, V., Déprez, B., & Baulard, A. Synthetic EthR inhibitors boost anti-tuberculous activity of ethionamide. Nature Medicine,2009, 15: 537-544.http://dx.doi.org/10.1038/nm.1950

Charton, J., Deprez-Poulain, R., Hennuyer, N., Tailleux, A., Staels, B., & Deprez, B. Novel non-carboxylic acid retinoids: 1,2,4-Oxadiazol-5-one derivatives. Bioorganic & Medicinal Chemistry Letters,2009, 19(2): 489-492.http://dx.doi.org/10.1016/j.bmcl.2008.11.040

Klose, D., Laprais, M., Leroux, V., Siepmann, F., Deprez, B., Bordet, R., & Siepmann, J. Fenofibrate-loaded PLGA microparticles: Effects on ischemic stroke. European Journal of Pharmaceutical Sciences,2009, 1:43-52. http://dx.doi.org/10.1016/j.ejps.2008.12.016

Beghyn, T., Deprez-Poulain, R., Willand, N., Foleas, B., & Deprez, B. Natural compounds: leads or ideas? Bioinspired molecules for drug discovery. Chemical Biology and Drug Design,2008, 72: 3-15. http://dx.doi.org/10.1111/j.1747-0285.2008.00673.x

Charton, J., Charruault, L., Deprez-Poulain, R., & Deprez, B. Alkylsquarates as key intermediates for the rapid preparation of original drug-inspired compounds. Combinatorial Chemistry and High Throughput Screening,2008, 11(4): 294-303.

Charton, J., Leroux, F., Delaroche, S., Landry, V., Deprez, B. P., & Deprez-Poulain, R. F. Synthesis of a Library of 200-Member Squaric Acid N-Hydroxylamide Amides. Bioorganic & Medicinal Chemistry Letters,2008, 18(18): 4968-4971. http://dx.doi.org/10.1016/j.bmcl.2008.08.025

Cousaert, N., Willand, N., Gesquiere, J.-C., Tartar, A., Deprez, B., & Deprez-Poulain, R. Original loading and Suzuki conditions for the solid-phase synthesis of biphenyltetrazoles. Application to the first solid-phase synthesis of irbesartan. Tetrahedron Letters,2008, 49: 2743-2747. http://dx.doi.org/10.1016/j.tetlet.2008.02.147

Vaccher, M.-P., Charton, J., Guelzim, A., Caignard, D.-H., Bonte, J.-P., & Vaccher, C.
Preparative Enantiomeric Separation of Potent AMP-Activated Protein Kinase Activator by HPLC on Amylose-Based Chiral Stationary Phase. Determination of Enantiomeric Purity and Assignment of Absolute Configuration.
Journal of Pharmaceutical and Biomedical Analysis,2008, 46(5): 920-928.
http://dx.doi.org/10.1016/j.jpba.2008.01.048

Villoutreix, B. O., Bastard, K., Sperandio, O., Fahraeus, R., Poyet, J. L., Calvo, F., Deprez, B., & Miteva, M. A.
In silico-in vitro screening of protein-protein interactions: towards the next generation of therapeutics.
Current Pharmaceutical Biotechnology,2008, 9(2): 103-122

Publications 2005-2007

Beghyn, T., Deprez-Poulain, R. F., & Willand, N. Drug Discovery and Selection – 43rd Rencontres Internationales de Chimie Thérapeutique, Lille, France.
IDDB Meeting Report ,2007.

Beghyn, T., Hounsou, C., & Deprez, B. P. PDE5 inhibitors: An original access to novel potent arylated analogues of tadalafil.
Bioorganic & Medicinal Chemistry Letters,2007, 17(3): 789-792. http://dx.doi.org/10.1016/j.bmcl.2006.10.069

Charton, J., Cousaert, N., Bochu, C., Willand, N., Deprez, B., & Deprez-Poulain, R. A versatile solid-phase synthesis of 3-aryl-1,2,4-oxadiazolones and analogues. Tetrahedron Letters,2007, 48(8): 1479-1483. http://dx.doi.org/10.1016/j.tetlet.2006.12.050

Deprez-Poulain, R. F., Charton, J., Leroux, V., & Deprez, B. P. Convenient synthesis of 4H-1,2,4-triazole-3-thiols using di-2-pyridylthionocarbonate. Tetrahedron Letters,2007, 48(46): 8157-8162. http://dx.doi.org/10.1016/j.tetlet.2007.09.094

Dubs, P., Bourel-Bonnet, L., Subra, G., Blanpain, A., Melnyk, O., Pinel, A. M., Gras-Masse, H., & Martinez, J.
Parallel synthesis of a lipopeptide library by hydrazone-based chemical ligation. J Comb Chem,2007, 9(6): 973-981.
http://dx.doi.org/ 10.1021/cc070033b

Flipo, M., Beghyn, T., Charton, J., Leroux, V. A., Deprez, B. P., & Deprez-Poulain, R. F. A library of novel hydroxamic acids targeting the metallo-protease family: design, parallel synthesis and screening. Bioorganic and Medicinal Chemistry,2007, 15(1): 63-76. http://dx.doi.org/10.1016/j.bmc.2006.10.010

Flipo, M., Beghyn, T., Leroux, V., Florent, I., Deprez, B. P., & Deprez-Poulain, R. F. Novel Selective Inhibitors of the Zinc Plasmodial Aminopeptidase PfA-M1 as Potential Antimalarial Agents. Journal of Medicinal Chemistry,2007, 50(6): 1322-1334.
http://dx.doi.org/10.1021/jm061169b

Gras-Masse, H., & Willand, N. Neuraminidase inhibitors and risk of H5N1 influenza. Annales Pharmaceutiques Francaises,2007, 65(1): 50-57.

Host, H., Drobecq, H., Locht, C., & Menozzi, F. D. Enzymatic methylation of the Mycobacterium tuberculosis heparin-binding haemagglutinin. FEMS Microbiology Letters,2007, 268(2): 144-150. http://dx.doi.org/10.1111/j.1574-6968.2007.00 6.x

Willand, N., Folléas, B., Boutillon, C., Verbraeken, L., Gesquiere, J.-C., Tartar, A., & Deprez, B. Efficient, Two-Step Synthesis O N-Substituted Nortropinone Derivatives. Tetrahedron Letters,2007, 48(29): 5007-5011.http://dx.doi.org/10.1016/j.tetlet.2007.05.110

Beghyn, T.; Hounsou, C.; Deprez, B. P., PDE5 inhibitors: An original access to novel potent arylated analogues of tadalafil.
Bioorg. Med. Chem. Lett. 2007, 17, (3), 789-92.http://dx.doi.org/10.1016/j.bmcl.2006.10.069

Deprez, B. 2007. Le criblage à haut contenu d’information pour la génétique chimique directe (criblage phénotypique sur organismes) et inverse (cribl e structural par RMN). In E. Marec, S. Roy, & F. Lafanechere (Eds.), Chemogénomique: Des petites molécules pour explorer le vivant: 109-119: EDP Sciences.

Ashworth, D. M., Batt, A. R., Baxter, A. J., Broqua, P., Haigh, R., M., Hudson, P., Heeney, C. M. S., Laporte, R., Penson, A., Pitt, G. R. W., Robson, P. A., Rooker, D. P., Tartar, A. L., Ye C. M., & Roe, M. B.
Nonpeptide oxytocin agonists.
Drugs of the Future,2006, 31(4): 345-353.

Charton, J., Girault-Mizzi, S., Debreu-Fontaine, M.-A., Foufelle, F., Hainault, I., Bizot-Espiard, J.-G., Caignard, D.-H., & Sergheraert, C. Synthesis and biological evaluation of benzimidazole derivatives as potent AMP-activated protein kinase activators. Bioorganic & Medicinal Chemistry,2006, 14(13): 4490. http://dx.doi.org/10.1016/j.bmc.2006.02.028

Deprez-Poulain, R., & Deprez, B. Trends in Hit-to-Lead: An Update. Frontiers in Medicinal Chemistry,2006, 3(1): 653-673.

Melnyk, P., Leroux, V., Sergheraert, C., & Grellier, P. Design, synthesis and in vitro antimalarial activity of an acylhydrazone library. Bioorg Med Chem Lett.,2006, 16(1): 31-35. http://dx.doi.org/10.1016/j.bmcl.2005.09.058

Toto, P., Gesquiere, J.-C., Cousaert, N., Deprez, B., & Willand, N. UFU (Ullmann-Finkelstein-Ullmann): a new multicomponent reaction. Tetrahedron Letters,2006, 47(28): 4973-4978. http://dx.doi.org/10.1016/j.tetlet.2006.04.041

Toto, P., Gesquiere, J.-C., Deprez, B., & Willand, N. Synthesis of N-(iodophenyl)-amides via an unprecedented Ullmann-Finkelstein tandem reaction. Tetrahedron Letters,2006, 47(7): 1181-1186.http://dx.doi.org/10.1016/j.tetlet.2005.12.022

Villefroy, P., Letourneur, F., Coutsinos, Z., Mortara, L., Beyer, C., Gras-Masse, H., Guillet, J. G., & Bourgault-Villada, I.
SIV escape mutants in rhesus macaques vaccinated with NEF-derived lipopeptides and clenged with pathogenic SIVmac251. Virol J,2006, 3: 65.

Caroline Smet, Jean-Frédéric Duckert, Jean-Michel Wieruszeski, Isabelle Landrieu, Luc Buée, Guy Lippens, and Benoît Déprez.
Control of protein-protein interactions: structure-based discovery of low molecular weight inhibitors of the interactions between Pin1 WW domain and phosphopeptides. J.Med.Chem , 2005, 48, (15), 4815-4823

Nicolas Cousaert, Patrick Toto, Nicolas Willand, and Benoît Déprez. Efficient, Protection-Free Suzuki-Miyaura Synthesis of ortho-biphenyltetrazoles. Tet Let, 2005, 46, 6529-6532.

Jolimaitre, P., Roux, A., Blanpain, A. , Leduc, C., Bassereau, P., Bourel-Bonnet, L. Synthesis and pre inary physical applications of a rhodamin-biotin phosphatidylethanolamine, an easy attainable lipid double probe Chem Phys Lipids, 2005, 133, (2), 215-23

Déprez-Poulain R, Melnyk P. Libraries of 1,4-bis(aminopropyl)piperazine antimalarials : from discovery to the coming generation. Comb. Chem. And High Through. Screen. Review, 2005, 8, (1), 39-48

Coutsinos, Z., Villefroy, P., Gras-Masse, H., Guillet, J. G., Bourgault-Villada, I. Evaluation of SIV-lipopeptide immunizations administered by the intradermal route in their ability to induce antigen specific T-cell responses in rhesus macaques
FEMS Immunol Med Microbiol, 2005, 43, (3), 357-66

Bourel-Bonnet, L., Rao, K. V., Hamann, M. T., Ganesan, A. Solid-phase total synthesis of kaalide A and related analogues
J Med Chem, 2005, 48, 5, 1330-5

Bourel-Bonnet, L., Pecheur, E. I., Grandjean, C., Blanpain, A., Baust, T., Melnyk, O., Hoflack, B., Gras-Masse, H.
Anchorage of synthetic peptides onto liposomes via hydrazone and alpha-oxo hydrazone bonds. preliminary functional investigations Bioconjug Chem, 2005, 16, 2, 450-7

Membres

BAUVOIS Agathe

Doctorant - IPL

Photo de BAUVOIS Agathe

BEGHYN Térence

PhD, PharmD, Maître de Conférences - Université de Lille

Photo de BEGHYN Térence

BIELA Alexandre

Technicien de laboratoire - IPL

N. ORCID : 0000-0001-5749-3262
Photo de BIELA Alexandre

BLANCHART Paul

PharmD, Doctorant - Université de Lille, Université de Saarland

Photo de BLANCHART Paul

BONNET Guillaume

Doctorant - Université de Lille

Photo de BONNET Guillaume

BOSC Damien

PhD, Maître de Conférences , Université de Lille

N. ORCID : 0000-0002-6076-2934
Photo de BOSC Damien

BOU KARROUM Nour

PhD, Maître de Conférences, Université de Lille

N. ORCID : 0000-0002-1516-9090
Photo de BOU KARROUM Nour

CARRE Paul

Ingénieur d’études, Institut Pasteur de Lille

Photo de CARRE Paul

CHARTON Julie

PhD, Maître de Conférences, Université de Lille

N. ORCID : 0000-0001-6895-276X
Photo de CHARTON Julie

Benoît DEPREZ

Directeur UMR1177 Inserm - Professeur PhD, Pharm Université de Lille

N. ORCID : 0000-0002-2777-4538
Photo de Benoît DEPREZ

DEPREZ-POULAIN Rebecca

Professeur, PhD, PharmD Université de Lille

N. ORCID : 0000-0002-3318-5297
Photo de DEPREZ-POULAIN Rebecca

DESGARDIN Clara

Ingénieur d’études , Institut Pasteur de Lille

Photo de DESGARDIN Clara

DUMONT Julie

Ingénieur d’études, Université de Lille

N. ORCID : 0000-0001-5893-0022
Photo de DUMONT Julie

FAURE Camille

Ingénieur d’études, SATTNord

Photo de FAURE Camille

FISCHER Pauline

PhD, Postdoctorant SATTNord

FLIPO Marion

PhD, Maître de Conférences, Université de Lille

N. ORCID : 0000-0003-2863-5721
Photo de FLIPO Marion

FOUGIAXIS Vasileios

PhD, PharmD, Postdoctorant IPL

Photo de FOUGIAXIS Vasileios

GADOTTI Irène

Responsable administratif et des opérations, INSERM

HENNEQUIN Hugo

Doctorant -Université de Lille

Photo de HENNEQUIN Hugo

HERLEDAN Adrien

Ingénieur d’étude Inserm, U1177

N. ORCID : 0000-0001-7258-498X
Photo de HERLEDAN Adrien

KANIECKI Sylvana

Ingénieur d’études SATTNord

Photo de KANIECKI Sylvana

KUBIAK Adrien

Administrateur de bases de données, IPL

Photo de KUBIAK Adrien

LANDRY Valérie

Ingénieur d’études IPL

N. ORCID : 0000-0002-7650-8965
Photo de LANDRY Valérie

LEROUX Florence

PhD, PharmD, Ingénieur de Recherche INSERM

N. ORCID : 0000-0003-0554-873X
Photo de LEROUX Florence

LOUCHET Théo

Doctorant Université de Lille

Photo de LOUCHET Théo

LUCCA Gabriele

Doctorant Université de lille

Photo de LUCCA Gabriele

LY Kim

PhD, Postdoctoral fellow SATTNord

Photo de LY Kim

NDJOGOU Dominique

Ingénieur d’études Institut Pasteur de Lille

Photo de NDJOGOU Dominique

NHARI Mira

Chargée de gestion et de pilotage IPL

Photo de NHARI Mira

PEZINSKI Marcin

PhD, Postdoctorant IPL

Photo de PEZINSKI Marcin

PIVETEAU Catherine

Ingénieur d’études Université de Lille

N. ORCID : 0000-0002-3835-4619

RUGGIERI Francesca

PhD, Postdoctorant Institut Pasteur de Lille

Photo de RUGGIERI Francesca

TARDY Morgane

Ingénieur Institut Pasteur de Lille

Photo de TARDY Morgane

VATINEL Rodolphe

PhD, Postdoctorant Université de Lille

N. ORCID : 0000-0001-8600-3904
Photo de VATINEL Rodolphe

VIGIER Clément

PhD, Postdoctorant Institut Pasteur de Lille

N. ORCID : 0000-0002-6127-0907
Photo de VIGIER Clément

VILLEMAGNE Baptiste

PhD, Maître de Conférences Université de Lille

N. ORCID : 0000-0002-8416-5253
Photo de VILLEMAGNE Baptiste

WARZEE Agathe

Doctorant Université de Lille

Photo de WARZEE Agathe

WILLAND Nicolas

Professeur, PhD Université de Lille

N. ORCID : 0000-0002-0784-0462
Photo de WILLAND Nicolas

Contact d'équipe

Benoît DEPREZ

Directeur UMR1177 Inserm - Professeur PhD, Pharm Université de Lille

N. ORCID : 0000-0002-2777-4538
Photo de Benoît DEPREZ