Articles & Reviews

 

2022

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. HAL

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. HAL

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 HAL

2021

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

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. HAL

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. HAL

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. HAL

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. HAL

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. Hypothalamic 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

2020

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  HAL

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 HAL

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 HAL

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 HAL

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 HAL

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 HAL

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 HAL

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 HAL

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 HAL

2019

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 HAL

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 HAL

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 HAL

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., Maréchal, 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 HAL

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 HAL

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 HAL

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 HAL

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 HAL

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 HAL

2018

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., Halley, 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

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., Marechal, 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 HAL

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. doi: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.doi: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.doi: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.

2016

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. doi: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). doi: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.doi: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. doi: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. doi: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. doi:10.4155/fmc-2015-0007 OPEN ACCESS

2015

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. doi:10.1016/j.cmet.2015.07.002

Deprez-Poulain, R., Nathalie, H., Bosc, D., Liang, W. G., Enee, E., Marechal, 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. doi: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. doi: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. doi: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. doi: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. doi:10.1016/j.tetlet.2015.01.046

Charton, J., Gauriot, M., Totobenazara, J., Hennuyer, N., Dumont, J., Bosc, D., Marechal, 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 doi: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.doi: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. doi: 10.1016/ j.jconrel. 2014.11.006

2014

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., Marechal, 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

2013

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

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.doi:10.1107/S0108270113028126

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.doi: 10.1016/j.ejmech.2013.08.027

Wieniewski, 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.doi: 10.1002/bip.22260

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. doi:10.1016/j.tetlet.2012.11.082

2012

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. doi: 10.1021/jm301506h

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

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. doi:10.1186/1750-1172-7-58

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. doi: 10.1016/j.tetlet.2012.07.031

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. doi:10.1021/jm300377g

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.. doi:10.1039/C2MD00287F

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. doi: 10.1016/j.ejmech.2012.02.033

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 doi:10.1016/j.tetlet.2012.03.007

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. doi: 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.doi: 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 doi: 10.1021/jm201422e

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. doi:10.1016/j.tetlet.2011.11.077

2011

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. doi: 10.1186/1476-4598-10-105

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. doi: 10.1039/C1NJ20059C

Bousquet, T., Jida, M., Soueidan, M., Deprez-Poulain, R., Agbossou-Niedercorn, F., & Pelinski, L. Fast and Efficient solvent-free Passerini reaction. Tetrahedron Letters,2011, 533: 306-308. doi:10.1016/j.tetlet.2011.11.028

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. doi:10.1016/j.ejmech.2011.05.056

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. doi: 10.1039/C1NJ20059C

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 67: 871-881. doi: 10.1002/biot.201100139

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. doi: 10.4155/bio.11.88

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, 67: 860-870. doi: 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.

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. doi:10.1021/jm200076a

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. doi:10.1021/jm1014617

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. doi:10.1016/j.tetlet.2011.02.011

2010

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. doi: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. doi: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. doi: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. doi: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. doi: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. doi: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. doi:10.1371/journal.pcbi.1000695

2009

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. doi:10.1021/jm900648x

Willand, N., Dirié, B., Carette, X., Bifani, P., Singhal, 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.doi: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.doi: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. doi:10.1016/j.ejps.2008.12.016

2008

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. doi: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. doi: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. doi: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.
doi: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

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. doi: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. doi: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. doi: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.
doi: 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. doi: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.
doi: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. doi: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.doi: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.doi: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. Marechal, S. Roy, & F. Lafanechere (Eds.), Chemogénomique: Des petites molécules pour explorer le vivant: 109-119: EDP Sciences.

2006

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. doi: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. doi: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. doi: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.doi: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 challenged with pathogenic SIVmac251. Virol J,2006, 3: 65.

2005

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 kahalalide 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

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