Lesire, L., Deprez-Poulain, R., Bosc, D., Leroux, F., Landry, V., Ourabah, S., Tardy, M., Maillard, C., Gealageas, R., Dumont, J., Herledan, A., Warenghem, S., Cruette, M., Lenglart, C., Biela, A., Piveteau, C., De Smedt, E., Muylaert, C., Liang, W., De Paco, EG, Alaterre, E., Ovejero, S., Robert, N., Delahaye, F., Tang, W.-J., van Endert, P., De Bruyne, E., Moreaux, J., & Deprez, B. Enhancing antitumor response to proteasome inhibitors with inhibitors of insulin-degrading enzyme, a new molecular vulnerability in multiple myeloma. British Journal of Pharmacology, 2026, .10.1111/bph.70407,  HAL OPEN ACCESS

El Bakali, J., Ronco, C., Landry, V., Papavasileiou, KD, Papadourakis, M., Warenghem, S., Leroux, F., Charton, J., Dumont, J., Piveteau, C., Staels, B., Afantitis, A., Hennuyer, N., Deprez, B., Bosc, D., & Deprez-Poulain, R. Discovery of pyrimidine-based small activators of Insulin Degrading Enzyme. European Journal of Medicinal Chemistry,2026:118740. 10.1016/j.ejmech.2026.118740 ; HAL OPEN ACCESS

Valderrama, K., Horlacher, O., Publicola, G., Eisenring, P., Kienle, M., Boarbi, S., Kiass, M., Korduláková, J., Chatagnon, J., Piveteau, C., Leroux, F., Savková, K., Záhorszká, M., Cantrelle, FX, Lherbet, C., Mourey, L., Mikušová, K., Mathys, V., Aichholz, R., Maveyraud, L., Altmann, KH, & Hartkoorn, RC Optimizing the Antibiotic Potency and Metabolic Stability of Pyridomycin Using a Semisynthetic Approach. J Med Chem,2026, 69(3):2496–2508.10.1021/acs.jmedchem.5c02409

Mourot, L., Chaibi, F.-Z., Bou-Karroum, N., Carré, P., Abengozar Munoz, A., Landry, V., Tarricone, A., Biela, A., Piveteau, C., Novikov, G., Dupré, E., Dubuisson, J., Belouzard, S., Leroux, F., Deprez, B., Hanoulle, X., & Charton, J. A new chemotype that opens the S2∗ pocket of the 3CL protease exhibits antiviral activity against SARS-CoV-2. European Journal of Medicinal Chemistry,2026, 302:118277. 10.1016/j.ejmech.2025.118277,   HAL OPEN ACCESS

Pochet, A., Bourguignon, T., Grandé, A., Godinez-Leon, JA, Li, J Control Release,2026,389:114415.10.1016/j.jconrel.2025.114415 

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 Pharmaceuticals,2026 126555. 10.1016 / j.ijpharm.2026.126555,  OPEN ACCESS 

Deprez, B. "Small" synthetic molecules: an inexhaustible, accessible and easily deployable reserve of therapeutic innovation. Chemical news.2025 10.63133/scf.act-chim.2025.505.06

Leib, J., Waeckel-Énée, E., Fabrega, S., Keelan, N., Senni, A., Mauvais, FX, 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, NB, Gealageas, R., Mauvais, F.-X., Warenghem, S., Roignant, M., Kraupner, N., Lam, BV, 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, AM, Gubellini, F., Mecy, A., Alzari, PM, 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, MM, 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, RC 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, 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, NM, 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 favors lipid accumulation in the liver. Br. J. Pharmacol.,2024, 181(19):3610-3626. 10.1111/bph.16436.

Aguilar-Ayala, DA, Sanz-García, F., Rabodoarivelo, MS, Susanto, BO, Bailo, R., Eveque-Mourroux, MR, Willand, N., Simonsson, USH, Ramón-García, S., & Lucía, A. Evaluation of critical parameters in the hollow-fiber 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, AR, & 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, RC 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, RT, Meurillon, V., Soulard, D., Piveteau, C., Biela, A., Dumont, J., Leroux, F., Deprez, B., Willand, N., Pos, KM, Frangakis, AS, Hartkoorn, RC, & 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, RC, & 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, GL, 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, BO, 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, RC, & 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, AC, Schellhorn, B., Antraygues, K., Scherer, H., Gitzinger, M., Kemmer, C., Dale, GE, 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, ND, Bindels, LB, Deprez, B., Vantyghem, MC, 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, CP, Heuson, E., Herledan, A., Oger, F., Thiroux, B., Chevalier, M., Gromada, X., Rolland, L., Froguel, P., Deprez, B., Paul, S., & Annicotte, J.-S. MALDI-TOF Mass Spectrometry. Cells,2023, 126.10.3390/cells 12060849.

Brier, L., Hassan, H., Hanoulle, 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, AR, & 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, RT, Hartkoorn, RC, Flipo, M., & Pos, KM 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, RC 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, CA, Sannio, F., Corsica, G., Benvenuti, M., Feller, G., Coulon, R., Marcoccia, F., Devente, SR, Bouajila, E., Piveteau, C., Leroux, F., Deprez-Poulain, R., Deprez, B., Licznar-Fajardo, P., Crowder, MW, 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, GE, 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, AK, 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, EK, 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/cells 11071228.

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, RT, Pradel, E., Foong, WE, Malloci, G., Ballée, A., Kirchner, MA, Moshfegh, P., Herledan, A., Herrmann, A., Deprez, B., Willand, N., Vargiu, AV, Pos, KM, Flipo, M., & Hartkoorn, RC Pyridylpiperazine-based allosteric inhibitors of RND-type multidrug efflux pumps. Nature Communications,2022, 131: 115. 10.1038/s41467-021-27726-2 

Deprez-Poulain, R., Schmidt, F., & Lesur, B. Medicinal Chemistry and Chemobiology. Actualité Chimique,2021, 468: 49

Kraupner, N., Dinh, CP, Wen, 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, 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, LR, Poelarends, GJ, & De Spiegeleer, B. Sustainability in Drug Discovery. Medicine in Drug Discovery,2021: 100107.10.1016/j.medidd.2021.100107.

Moureu, S., Caradec, T., Trivelli, 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, VS, 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, BV, 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, AR, & 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

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Villemagne, B., Machelart, A., Tran, NC, Flipo, M., Moune, M., Leroux, F., Piveteau, C., Wohlkönig, A., Wintjens, R., Li, Vivo Ethionamide Boosting Activity. ACS Infect Dis,2020, 6(3): 366-378 .10.1021/acsinfecdis.9b00277

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

Lu, Y., Giri, H., Villoutreix, BO, Ding, Q., Wang, X., & Rezaie, AR 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, AR, Roumenina, L., Lagarde, N., Fremeaux-Bacchi, V., Miteva, MA, & Villoutreix, BO 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, AM, Drobecq, H., Bauderlique-le Roy, H., Villemagne, B., Antonenko, YN, & Hartkoorn, RC 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, BO, & Miteva, MA A Free Web-Based Protocol to Assist Structure-Based Virtual Screening Experiments. Int. J. Mol. Sci.,2019, 20(18): 4648.10.3390 / ijms20184648

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Prevet, H., Moune, M., Tanina, A., Kemmer, C., Herledan, A., Frita, R., Wohlkönig, A., Bourotte, M., Villemagne, B., Leroux, F., Gitzinger, M., Baulard, AR, 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, SH, Flipo, M., Villemagne, B., Prevet, H., Déprez, B., Moune, M., Perée, H., Meyer, F., Baulard, AR, 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, Flipo, M., Brosch, R., Nesslany, F., Deprez, B., Muraille, E., Locht, C., Baulard, AR, 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

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Salzano, G., Wankar, J., Ottani, S., Villemagne, B., Baulard, AR, 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, H., Lacroix, D., Deprez, B., Jegou, B., Koussa, M., Edme, JL, Lefebvre, P., & Staels, B. Daytime variation of perioperative myocardial injury in cardiac surgery and its prevention by Rev-Erbalpha antagonism: a single-center propensity-matched cohort study and a randomized study. Lancet,2017 391(10115): 59–69.10.1016/s0140-6736(17)32132-3

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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, 7Article number: 5390 10.1038/s41598-017-05453-3

Dequirez, G., Bourotte, M., Porras de Francisco, E., Remuiñan, Blanco, MJ, 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, CS, 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, LF 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 cyclodextrin systems for the enantiomeric and diastereoisomeric separations of structurally related dihydropyridone analogues. Electrophoresis 2017, 38 (15) 1922-1931.10.1002/elps.201600536

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Wohlkönig, A., Remaut, H., Moune, M., Tanina, A., Meyer, F., Desroses, M., Steyaert, J., Willand, N., Baulard, AR, & 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, IM, 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, CS, Luzy, A.-P., Mathieu, A., Millois, C., Pascau, J., Pinto, A., Polge, G., Reitz, A., Reversé, K., Rosignoli, C., Taquet, N., & Hennequin, LF 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.

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Bauters, D., Scroyen, I., Deprez-Poulain, R., & Lijnen, HR 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

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Probst, NP, 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

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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, NC, 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

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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

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Corbel, C., Zhang, B., Le Parc, A., Baratte, B., Colas, P., Couturier, C., Kosik, KS, 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, MP, 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, AL, Sperandio, O., Pottiez, V., Balzarin, S., Herledan, A., Elkaim, JO, Fogeron, ML, Piveteau, C., Dassonneville, S., Deprez, B., Villoutreix, BO, 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

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Crauste, C., Willand, N., Villemagne, B., Flipo, M., Willery, E., Carette, 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( 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

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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 benzimidazole derivatives. Biomedical Chromatography,2013, 28( 10.1002/bmc.2992

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( 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, Baulard, A. Structural activation of the transcriptional repressor EthR from M. tuberculosis by single amino-acid change mimicking natural and synthetic ligands Nucleic Acid Res,2012, 40( 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, SH, Christophe, T., Jeon, HK, Locht, C., Brodin, P., Deprez, B., Baulard, AR, & 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( 10.1021/jm200825u

Beghyn, T., Julie, C., Leroux, F., Henninot, A., Reboule, I., Cos, P., Maes, L., & Deprez, BP Drug-to-Genome-to-Drug, Step 2: Reversing Selectivity in a Series of Antiplasmodial Compounds. Journal of Medicinal Chemistry,2012, 55( 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 Optimization. Med.Chem.Comm.,2012, 3: 469-474. 10.1039/C2MD00287F

Wen, Tetrahedron Letters,2012, 53( 10.1016/j.tetlet.2012.03.007

Villemagne, B., Crauste, C., Flipo, M., Baulard, AR, 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 (T3P^R) 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, HK, 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( 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( 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. Chemical sciences and life sciences: a promising coalescence for pharmacy. Chemical news,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( 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( 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( 10.1016/j.tetlet.2011.02.011

Beghyn, TB, 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( 10.1021/jm1014617

Flipo, M., Desroses, M., Lecat-Guillet, N., DirieÌ , B., Carette, Baulard, AR, & 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( 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( 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( 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, FA, & Pelinski, L. Efficient access to new chiral ferrocenyl [gamma]-lactams from amino alcohols. New Journal of Chemistry,2011, 35( 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, BO, & 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, BP, & Deprez-Poulain, RF 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 Amyloidosis-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, BO, Bastard, K., Sperandio, O., Fahraeus, R., Poyet, JL, Calvo, F., Deprez, B., & Miteva, MA
In silico-in vitro screening of protein-protein interactions: towards the next generation of therapeutics.
Current Pharmaceutical Biotechnology,2008,9(2):103-122

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

Beghyn, T., Hounsou, C., & Deprez, BP 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, RF, Charton, J., Leroux, V., & Deprez, BP 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, AM, 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, VA, Deprez, BP, & Deprez-Poulain, RF 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, BP, & Deprez-Poulain, RF 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, FD 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, BP, 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. High information content screening for forward chemical genetics (phenotypic screening on organisms) and inverse chemical genetics (structural screening by NMR). In E. Marec, S. Roy, & F. Lafanechere (Eds.), Chemogenomics: Small molecules to explore life: 109-119: EDP Sciences.

Ashworth, DM, Batt, AR, Baxter, AJ, Broqua, P., Haigh, R., M., Hudson, P., Heeney, CMS, Laporte, R., Penson, A., Pitt, GRW, Robson, PA, Rooker, DP, Tartar, AL, Ye CM, & Roe, MB
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, JG, & Bourgault-Villada, I.
SIV escape mutants in rhesus macaques vaccinated with NEF-derived lipopeptides and activated 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 feasible 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, JG, 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, KV, Hamann, MT, Ganesan, A. Solid-phase total synthesis of kaalide A and related analogues
J Med Chem, 2005, 48, 5, 1330-5

Bourel-Bonnet, L., Pecheur, EI, 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