2022

• 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., Haupenthal, J., Lesire, L., Hirsch, A. K., Deprez, B., Stratikos, E., Bouvier, M., & Deprez-Poulain, R. Discovery of the First Selective Nanomolar Inhibitors of Endoplasmic Reticulum Aminopeptidase 2 by Kinetic Target-Guided Synthesis. Angewandte Chemie International Edition,2022, n/an/a.10.1002/anie.202203560. 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.

2021

• Deprez-Poulain, R., Schmidt, F., & Lesur, B. Chimie thérapeutique et chémobiologie. Actualité Chimique,2021, 468: 49.
• Kraupner, N., Dinh, C. P., Wen, X., Landry, V., Herledan, A., Leroux, F., Bosc, D., Charton, J., Maillard, C., Warenghem, S., Duplan, I., Piveteau, C., Hennuyer, N., Staels, B., Deprez, B., & Deprez-Poulain, R. Identification of indole-based activators of insulin degrading enzyme. European Journal of Medicinal Chemistry,2021: 113982.10.1016/j.ejmech.2021.113982.
• Deprez, B., Bosc, D., Charton, J., Couturier, C., Deprez-Poulain, R., Flipo, M., Leroux, F., Villemagne, B., & Willand, N. Molecular Design in Practice: A Review of Selected Projects in a French Research Institute That Illustrates the Link between Chemical Biology and Medicinal Chemistry. Molecules,2021, 2619: 6083.10.3390/molecules26196083.

• 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

2020

• Medve, L., Gealageas, R., Lam, B. V., Guillaume, V., Castillo-Aguilera, O., Camberlein, V., 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: 113053.10.1016/j.ejmech.2020.113053
• 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: in press.http://doi.org/10.1021/acs.jmedchem.9b01183
• 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: in press.http://doi.org/10.1177/2472555219897256

2019

• 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.https://doi.org/10.1016/j.ejmech.2019.06.057

2018

• 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. The Lancet,2018, 391(10115): 59–69.https://doi.org/10.1016/s0140-6736(17)32132-3
• 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 https://dx.doi.org/10.7554/eLife.33572

2017

• 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 Med. Chem. Lett.,2017, 8(3): 333-337.http://doi.org/10.1021/acsmedchemlett.6b00505
• 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. J. Med. Chem.,2017, 60(21): 9067–9089.http://doi.org/10.1021/acs.jmedchem.7b01444

2016

• 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 Med. Chem.,2016, 8(4): 381-404.http:\\dx.doi.org\10.4155/fmc-2015-0007     OPEN ACCESS
• Bauters, D., Scroyen, I., Deprez-Poulain, R., & Lijnen, H. R. ADAMTS5 promotes murine adipogenesis and visceral adipose tissue expansion. Thromb. Haemost.,2016, 116(4): 694-704.10.1160/th16-01-0015
• 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: 278–292.10.1016/j.ebiom.2016.06.002

2015

• 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,2015, 90: 547-567.10.1016/j.ejmech.2014.12.005
• Deprez-Poulain, R., Nathalie, H., Bosc, D., Liang, W. G., Enee, E., Marechal, X., Julie, C., Totobenazara, J., Berte, G., Jakhlal, 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 Commun.,2015, 6(Article number 9250).10.1038/ncomms9250 OPEN ACCESS

2014

• 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. Eur. J. Med. Chem.,2014, 79: 184-193.http://dx.doi.org/10.1016/j.ejmech.2014.04.009
• 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 Med. Chem.,2014, 6(12): 1399-1412. 10.4155/FMC.14.84

2013

• 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 Lett.,2013, 54(6): 562-567.10.1016/j.tetlet.2012.11.082
• Maingot, L., Elbakali, J., Dumont, J., Bosc, D., Cousaert, N., Urban, A., Deglane, G., Villoutreix, B., Nagase, H., Sperandio, O., Leroux, F., Deprez, B., & Deprez-Poulain, R. Aggrecanase-2 Inhibitors Based on the Acylthiosemicarbazide Zinc-Binding Group. Eur J Med Chem,2013, 69: 244-261. 10.1016/j.ejmech.2013.08.027

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. J. Med. Chem.,2012, 55(24): 10909-10917.doi: 10.1021/jm301506h
• Bousquet, T., Jida, M., Soueidan, M., Deprez-Poulain, R., Agbossou-Niedercorn, F., & Pelinski, L. Fast and Efficient solvent-free Passerini reaction. Tetrahedron Lett.,2012, 53(3): 306-308.doi: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 Lett.,2012, 53: 458-461.doi:10.1016/j.tetlet.2011.11.077
• 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
• Wen, X., Bakali, J. E., Deprez-Poulain, R., & Deprez, B. Efficient propylphosphonic anhydride (®T3P) mediated synthesis of benzothiazoles, benzoxazoles and benzimidazoles. Tetrahedron Lett.,2012, 53(19): 2440-2443.doi:10.1016/j.tetlet.2012.03.007
• 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
• 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 Lett.,2012, 53(39): 5215–5218.doi: 10.1016/j.tetlet.2012.07.031

2011

• 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
• 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 Lett.,2011, 52(14): 1705-1708.DOI:10.1016/j.tetlet.2011.02.011

2010

• 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
• 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 Lett.,2010, 51(22): 2983-2985.doi:10.1016/j.tetlet.2010.03.120
• 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 Lett.,2010, 51(39): 5109-5111.doi:10.1016/j.tetlet.2010.07.021
• 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. Bioorg. Med. Chem. Lett.,2010, 21: 6213-6216.doi:10.1016/j.bmcl.2010.08.108

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. Nat. Med.,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. Bioorg. Med. Chem. Lett.,2009, 19(2): 489-492.doi:10.1016/j.bmcl.2008.11.040

2008

• 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 Lett.,2008, 49: 2743-2747.doi:10.1016/j.tetlet.2008.02.147
• Charton, J., Charruault, L., Deprez-Poulain, R., & Deprez, B. Alkylsquarates as key intermediates for the rapid preparation of original drug-inspired compounds. Comb. Chem. High Throughput Screen.,2008, 11(4): 294-303 10.2174/138620708784246013
• 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. Bioorg. Med. Chem. Lett.,2008, 18(18): 4968-4971.doi:10.1016/j.bmcl.2008.08.025
• Beghyn, T., Deprez-Poulain, R., Willand, N., Foleas, B., & Deprez, B. Natural compounds: leads or ideas? Bioinspired molecules for drug discovery. Chem. Biol. Drug Des.,2008, 72: 3-15.doi:10.1111/j.1747-0285.2008.00673.x

2007

• 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. J. Med. Chem.,2007, 50(6): 1322-1334 10.1021/jm061169b
• 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. Bioorg. Med. Chem.,2007, 15(1): 63-76.doi:10.1016/j.bmc.2006.10.010  
• 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 Lett.,2007, 48(46): 8157-8162.doi:10.1016/j.tetlet.2007.09.094
• 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 Lett.,2007, 48(8): 1479-1483.doi:10.1016/j.tetlet.2006.12.050

2005

• Deprez-Poulain, R., & Melnyk, P. 1,4-bis(3-aminopropyl)piperazine libraries: from the discovery of classical chloroquine-like antimalarials to the identification of new targets. Comb. Chem. High Throughput Screen.,2005, 8(1): 39-48 10.2174/1386207053328165
• Guillon, J., Grellier, P., Labaied, M., Sonnet, P., Leger, J. M., Deprez-Poulain, R., Forfar-Bares, I., Dallemagne, P., Lemaitre, N., Pehourcq, F., Rochette, J., Sergheraert, C., & Jarry, C. Synthesis, antimalarial activity, and molecular modeling of new pyrrolo[1,2-a]quinoxalines, bispyrrolo[1,2-a]quinoxalines, bispyrido[3,2-e]pyrrolo[1,2-a]pyrazines, and bispyrrolo[1,2-a]thieno[3,2-e]pyrazines. J. Med. Chem.,2004, 47(8): 1997-2009 10.1021/jm0310840

2004

• Deprez-Poulain, R., Willand, N., Boutillon, C., Nowogrocki, G., Azaroual, N., & Deprez, B. A simple reaction to produce small structurally complex and diverse molecules. Tetrahedron Lett.,2004, 45(27): 5287-5290.doi:10.1016/j.tetlet.2004.05.008
• Deprez-Poulain, R., & Deprez, B. Facts, figures and trends in lead generation. Curr. Top. Med. Chem.,2004, 4(6): 569-580

2003

• Ryckebusch, A., Deprez-Poulain, R., Maes, L., Debreu-Fontaine, M. A., Mouray, E., Grellier, P., & Sergheraert, C. Synthesis and in vitro and in vivo antimalarial activity of N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives. J. Med. Chem.,2003, 46(4): 542-557
• Ryckebusch, A., Deprez-Poulain, R., Debreu-Fontaine, M.-A., Vandaele, R., Mouray, E., Grellier, P., & Sergheraert, C. Synthesis and antimalarial evaluation of new 1,4-bis(3-aminopropyl)piperazine derivatives. Bioorg. Med. Chem. Lett.,2003, 13(21): 3783-3787
• Flipo, M., Florent, I., Grellier, P., Sergheraert, C., & Deprez-Poulain, R. Design, synthesis and antimalarial activity of novel, quinoline-Based, zinc metallo-aminopeptidase inhibitors. Bioorg. Med. Chem. Lett.,2003, 13(16): 2659-2662

2002

• Ryckebusch, A., Deprez-Poulain, R., Debreu-Fontaine, M. A., Vandaele, R., Mouray, E., Grellier, P., & Sergheraert, C. Parallel Synthesis and Anti-Malarial Activity of a Sulfonamide Library. Bioorg. Med. Chem. Lett.,2002, 12(18): 2595-2598

2001

• Poulain, R. F., Tartar, A. L., & Deprez, B. P. Parallel synthesis of 1,2,4-oxadiazoles from carboxylic acids using an improved, uronium-based, activation. Tetrahedron Lett.,2001, 42(8): 1495-1498
• Poulain, R., Horvath, D., Bonnet, B., Eckhoff, C., Chapelain, B., Bodinier, M. C., & Deprez, B. From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands. J. Med. Chem.,2001, 44(21): 3378-3390
• Poulain, R., Horvath, D., Bonnet, B., Eckhoff, C., Chapelain, B., Bodinier, M. C., & Deprez, B. From hit to lead. Analyzing structure-profile relationships. J. Med. Chem.,2001, 44(21): 3391-3401

2000

• Yu, N., Poulain, R., & Gesquiere, J.-C. A One-Pot Synthesis of Tetrahydroisoquinolonic Acids from Aldehydes and Amines in Trimethylorthoformate. Synlett,2000, 3: 355-350

1999

• Yu, N., Poulain, R., Tartar, A., & Gesquiere, J.-C. Cycloaddition of homophthalic anhydrides with aldehydes and ketones: a route to 3,4-dihydroisocoumarin-4-carboxylic acid derivatives. Tetrahedron,1999, 55(48): 13735-13740

1997

• Baudelle, R., Bourel, L., Poulain, R., Vendeville, S., & Tartar, A. Premier Symposium français sur la chimie combinatoire, Rennes, 29-30 octobre 1996. Act. Chimique,1997, 1: 13-19