Publications
• Laniel A, Marouseau E, Nguyen DT, Froehlich, U, McCartney C, Boudreault PL*, Lavoie C* (2023) Characterization of PGua4, a Guanidinium-Rich Peptoid that Delivers IgGs to the Cytosol via Macropinocytosis. Molecular Pharmaceutics, just accepted.
• Théroux L, Van Den Hauwe R, Trân K, Fournier J, Desgagné M, Meneboo N, Lavallée A, Fröhlich U, Côté J, Hollanders C, Longpré JM, Murza A, Marsault E, Sarret P*, Boudreault PL*, Ballet S*, (2023) Signaling Modulation via Minimal C-Terminal Modifications of Apelin-13. ACS Pharmacology & Translational Science., just accepted.
• Pérez-Vargas J, Shapira T, Olmstead AD, Villanueva I, Thompson CAH, Ennis S, Gao1 G, DeGuzman J, Williams DE, Wang M, Chin A, Bautista-Sánchez A, Agafitei O, Levett P, Xie X, Nuzzo G, Freire VF, Quintana-Bulla JI, Bernardi DI, Gubiani JR, Suthiphasilp V, Raksat A, Meesakul P, Polbuppha P, Cheenpracha S, Jaidee W, Kanokmedhakul K, Yenjai C, Chaiyosang B, Teles HL, Manzo E, Fontana A, Leduc R, Boudreault PL, Berlinck RGS, Laphookhieo S, Kanokmedhakul S, Tietjen I, Cherkasov A, Krajden M, Nabi IR, Niikura M, Shi PY, Andersen RJ*, Jean F*, (2022) Discovery of lead natural products for developing pan-SARS-CoV-2 therapeutics. Antiviral Research. 209:105484.
• Binette R, Desgagné M, Theaud C, Boudreault PL, (2022) Efficient Fmoc-Protected Amino Ester Hydrolysis Using Green Calcium(II) Iodide as a Protective Agent. Molecules. 27(9):2788
• Shapira T, Monreal IA, Jager M, Dion SP, Buchholz DW, Imbiakha B, Olmstead AD, Jager M, Désilets A, Gao G, Martins M, Vandal T, Thompson CAH, Chin A, Rees WD, Steiner T, Nabi IR, Marsault E, Sahler J, Diel GD, Van de Walle GR, August A, Whittaker GR, Boudreault PL, Leduc R, Aguilar HC, Jean F. (2022) A TMPRSS2 inhibitor acts as a pan-SARS-Cov-2 prophylactic and therapeutic. Nature. 605(7909):340-348.
• Trân K, Sainsily X, Côté J, Coquerel D, Couvineau P, Saibi S, Haroune L, Besserer-Offroy E, Flynn-Robitaille J, Resua Rojas M, Murza A, Longpré JM, Auger-Messier M, Lesur O, Bouvier M, Marsault E, Boudreault PL, Sarret P. (2022) Size-Reduced Macrocyclic Analogues of [Pyr1]-apelin-13 Showing Negative Gα12 Bias Still Produce Prolonged Cardiac Effects. Journal of Medicinal Chemistry. 65(1):531-551.
• Normandin C, Boudreault PL. (2021) Concise Large-Scale Synthesis of Tomatidine, A Potent Antibiotic Natural Product. Molecules. 26(19):6008.
• Chartier, M; Desgagné, M; Sousbie, M; Rumsby, C; Chevillard, L; Théroux, L; Haroune, L; Côté, J;-Longpré, JM; Boudreault, PL; Marsault, E; Sarret, P;. (2021). Pharmacodynamic and Pharmacokinetic Profiles of a Neurotensin Receptor Type 2 (NTS2) Analgesic Macrocyclic Analog. Biomedicine & Pharmacotherapy. 141: 111861.
• Comeau, C*; Ries, B, Stadelmann, T; Tremblay, J*; Poulet, S*; Froehlich, U; Côté, J; Boudreault, PL; Derbali, RM; Sarret, P; Grandbois, M; Leclair, G; Riniker, S; Marsault, E. (2021). Modulation of the passive permeability of semi-peptidic macrocycles – N-and C-methylations fine-tune conformation and properties. Journal of Medicinal Chemistry. 64(9): 5365-5383.
• Marsault E, Boudreault PL, Traboulsi H, Sarret P, Nepveu-Traversy ME, Gaudreau S, Leduc F, Larrivee JF, Arcand M. (2020) Anti-human NTSR1 (neurotensin receptor type )1 antibodies and conjugates for diagnosis and treatment of NTSR1-associated metabolic or neoplastic disease. Patent WO 2020041896.
• A Murza, SP Dion, PL Boudreault, A Désilets, R Leduc, E Marsault. (2020). Inhibitors of Type II transmembrane serine proteases in treatment of diseases of the respiratory tract. Expert Opinion on Therapeutic Patents. 30(11): 807-824.
• Le Roux, A; Blaise, E; Boudreault, PL; Comeau, C; Doucet, A; Giarrusso, M; Collin, MP; Neubauer, T; Koelling, F; Goeller, A; Seep, A; Tshitenge, D; Wittwer, M; Kullmann, M; Hillisch, A; Mittendorf, J; Marsault, E. (2020). Structure-Permeability Relationship of Semi-Peptidic Macrocycles – Understanding and Optimizing Passive Permeability and Efflux Ratio. Journal of Medicinal Chemistry. 63(13): 6774-6783.
• Béliveau F; Tarkar A; Ghinet MG; Dion SP; Boudreault PL; Désilets A; StGeorges C; Marsault E; Paone D; Collins J; Macphee CH; Campobasso N; Groy A; Cottom J; Ouellette M; Pope AJ; Leduc R. (2019). TMPRSS6 inhibitors increase hepcidin levels in hepatocytes. Cell Chemical Biology. 26(11): 1559-1572.
• K Klarskov, H Gagnon, PL Boudreault*, C Normandin*, B Plancq*, E Marsault, GJ Gleich, S Naylor. (2018). Structure determination of disease-associated peak AAA from L-tryptophan implicated inthe eosinophiliamyalgia syndrome.Toxicology Letters. 282: 71-80.
• Boulet M, Lamontagne C, Guay I, Brouillette E, Langlois JP, Jacques PE, Rodrigue S, Brzezinski R;, Beauregard P, Bouarab K, Boyapelly K, Boudreault PL, Marsault E, Malouin F. (2018) Tomatidine is a lead antibiotic molecule that targets Staphylococcus aureus ATP synthase subunit C. Antimicrobial Agents and Chemotherapy, 62(6), e02197-17/1-e02197-17/18.
• Klarskov K; Gagnon H; Boudreault PL; Racine M; Boudreault PL; Normandin C; Marsault E; Gleich GJ; Naylor S. (2018). Peak AAA fatty acid contaminants present in the dietary supplementL-Tryptophan associated with the onset of Eosinophilia-Myalgia syndrome. Toxicology Letters. 294: 193-204.
• Lamontagne Boulet M, Isabelle C, Guay I, Brouillette E, Langlois JP, Jacques PÉ, Rodrigue S, Brzezinski R, Beauregard PB, Bouarab K, Boyapelly K, Boudreault PL, Marsault É, Malouin F. (2018). Tomatidine, a lead antibiotic molecule that targetsStaphylococcus aureus ATP synthase subunit C. Antimicrobial Agents and Chemotherapy. 62(6): e02197-17.
• Leyton JF, Marsault E, Beaudoin S, Boudreault PL, Bonin MA, Lopez A. (2018) Antibody conjugate for treating and detecting bladder cancer. Patent WO 2018165752.
• Boudreault PL, Colombo E, Leduc R, Marsault E, Plancq B, Richter M. (2018) Matriptase inhibitors and therapeutic uses thereof. Patent WO 2018112648.
• C St-Georges*, A Désilets, F Béliveau, M Ghinet, SP Dion, É Colombo*, PL Boudreault, RJ Najmanovich, R Leduc, E Marsault. (2017). Modulating the selectivity of matriptase-2 inhibitors with unnatural amino acids.European Journal of Medicinal Chemistry. 129: 110-123.
• M Paquette, L Guillermo Vilera-Perez, S Beaudoin, N Ekindi-Ndongo, PL Boudreault, MA Bonin, MC Battista, M Bentourkia, AF Lopez, R Lecomte, E Marsault, B Guérin, R Sabbagh, JV Leyton. (2017). Targeting IL5Ra with antibody-conjugates reveals a strategy for imaging and therapy forinvasive bladder cancer. Oncoimmunology. 6(10): e1331195.
• Berube, C; Barbeau, X; Cardinal, S; Boudreault, PL; Bouchard, C; Delcey, N; Lague, P; Voyer, N. (2017). Interfacialsupramolecular biomimetic epoxidation catalyzed by cyclic dipeptides. Supramolecular Chemistry. 29(5): 330-349.
• Berube, C; Cardinal, S; Boudreault, PL; Barbeau, X; Delcey, N; Giguere, M; Gleeton, D; Voyer, N (2015). Novel chiralN,N'-dimethyl-1,4-piperazines with metal binding abilities. Tetrahedron. 71(42): 8077-8084.
• Boudreault, PL; Mattler, JK; Wender, PA. (2015). Studies on the regio-and diastereo-selective epoxidation of daphnanes and tiglianes. Tetrahedron Letters. 56(23): 3423-3427.
• Duchêne D, Colombo E, Désilets A, Boudreault PL, Leduc R, Marsault E, Najmanovich R. (2014). Analysis of subpocketselectivity and identification of potent selective inhibitors for matriptaseand matriptase-2. Journal of Medicinal Chemistry. 57(23): 10198-204.
• Boudreault PL, Arseneault M, Otis F, Voyer N. (2008). Nanoscale tools to selectively destroy cancer cells. Chemical Communications, (18), 2118-20.
• Boudreault PL, Voyer N. (2007). Synthesis, characterization and cytolytic activity of alpha-helical amphiphilic peptide nanostructures containing crown ethers. Organic and Biomolecular Chemistry, 5(9), 1459-65.
Other publications of the group
• Coquerel, D., Lamoureux, J., Chagnon, F., Trân, K., Sage, M., Fortin-Pellerin, E., Delile, E., Sainsily, X., Fournier, J., Dumont, A. A., Auger-Messier, M., Sarret, P., Marsault, E., Praud, J. P., Fülöp, T., & Lesur, O. (2021). Apelin-13 in septic shock: effective in supporting hemodynamics in sheep but compromised by enzymatic breakdown in patients. Scientific reports, 11(1), 22770.
• Sainsily, X., Coquerel, D., Giguère, H., Dumont, L., Tran, K., Noll, C., Ionescu, A. L., Côté, J., Longpré, J. M., Carpentier, A., Marsault, É., Lesur, O., Sarret, P., & Auger-Messier, M. (2021). Elabela Protects Spontaneously Hypertensive Rats From Hypertension and Cardiorenal Dysfunctions Exacerbated by Dietary High-Salt Intake. Frontiers in pharmacology, 12, 709467.
• Trân, K., Van Den Hauwe, R., Sainsily, X., Couvineau, P., Côté, J., Simard, L., Echevarria, M., Murza, A., Serre, A., Théroux, L., Saibi, S., Haroune, L., Longpré, J. M., Lesur, O., Auger-Messier, M., Spino, C., Bouvier, M., Sarret, P., Ballet, S., & Marsault, É. (2021). Constraining the Side Chain of C-Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile. Journal of medicinal chemistry, 64(9), 5345–5364.
• Coquerel, D., Delile, E., Dumont, L., Chagnon, F., Murza, A., Sainsily, X., Salvail, D., Sarret, P., Marsault, E., Auger-Messier, M., & Lesur, O. (2021). Gαi-biased apelin analog protects against isoproterenol-induced myocardial dysfunction in rats. American journal of physiology. Heart and circulatory physiology, 320(4), H1646–H1656.
• Chartier, M., Desgagné, M., Sousbie, M., Côté, J., Longpré, J. M., Marsault, E., & Sarret, P. (2021). Design, Structural Optimization, and Characterization of the First Selective Macrocyclic Neurotensin Receptor Type 2 Non-opioid Analgesic. Journal of medicinal chemistry, 64(4), 2110–2124.
• Trân, K., Murza, A., Sainsily, X., Delile, E., Couvineau, P., Côté, J., Coquerel, D., Peloquin, M., Auger-Messier, M., Bouvier, M., Lesur, O., Sarret, P., & Marsault, É. (2021). Structure-Activity Relationship and Bioactivity of Short Analogues of ELABELA as Agonists of the Apelin Receptor. Journal of medicinal chemistry, 64(1), 602–615.
• Langlois, J. P., Millette, G., Guay, I., Dubé-Duquette, A., Chamberland, S., Jacques, P. É., Rodrigue, S., Bouarab, K., Marsault, É., & Malouin, F. (2020). Bactericidal Activity of the Bacterial ATP Synthase Inhibitor Tomatidine and the Combination of Tomatidine and Aminoglycoside Against Persistent and Virulent Forms of Staphylococcus aureus. Frontiers in microbiology, 11, 805.
• Brouillette, R. L., Besserer-Offroy, É., Mona, C. E., Chartier, M., Lavenus, S., Sousbie, M., Belleville, K., Longpré, J. M., Marsault, É., Grandbois, M., & Sarret, P. (2020). Cell-penetrating pepducins targeting the neurotensin receptor type 1 relieve pain. Pharmacological research, 155, 104750.
• Marsault, E., Llorens-Cortes, C., Iturrioz, X., Chun, H. J., Lesur, O., Oudit, G. Y., & Auger-Messier, M. (2019). The apelinergic system: a perspective on challenges and opportunities in cardiovascular and metabolic disorders. Annals of the New York Academy of Sciences, 1455(1), 12–33.
• Simmons, J. R., Murza, A., Lumsden, M. D., Kenward, C., Marsault, É., & Rainey, J. K. (2019). Simultaneous Ligand and Receptor Tracking through NMR Spectroscopy Enabled by Distinct 19F Labels. International journal of molecular sciences, 20(15), 3658.
• Sousbie, M., Vivancos, M., Brouillette, R. L., Besserer-Offroy, É., Longpré, J. M., Leduc, R., Sarret, P., & Marsault, É. (2018). Structural Optimization and Characterization of Potent Analgesic Macrocyclic Analogues of Neurotensin (8-13). Journal of medicinal chemistry, 61(16), 7103–7115.
• Murza, A., Trân, K., Bruneau-Cossette, L., Lesur, O., Auger-Messier, M., Lavigne, P., Sarret, P., & Marsault, É. (2018). Apelins, ELABELA, and their derivatives: Peptidic regulators of the cardiovascular system and beyond. Peptide Science, 111(1), e24064.
• Besserer-Offroy, É., Bérubé, P., Côté, J., Murza, A., Longpré, J. M., Dumaine, R., Lesur, O., Auger-Messier, M., Leduc, R., Marsault, É., & Sarret, P. (2018). The hypotensive effect of activated apelin receptor is correlated with β-arrestin recruitment. Pharmacological research, 131, 7–16.
• Guay, I., Boulanger, S., Isabelle, C., Brouillette, E., Chagnon, F., Bouarab, K., Marsault, E., & Malouin, F. (2018). Tomatidine and analog FC04-100 possess bactericidal activities against Listeria, Bacillus and Staphylococcus spp. BMC pharmacology & toxicology, 19(1), 7.
• Coquerel, D., Sainsily, X., Dumont, L., Sarret, P., Marsault, É., Auger-Messier, M., & Lesur, O. (2018). The apelinergic system as an alternative to catecholamines in low-output septic shock. Critical care (London, England), 22(1), 10.
• Yan, L. H., Le Roux, A., Boyapelly, K., Lamontagne, A. M., Archambault, M. A., Picard-Jean, F., Lalonde-Seguin, D., St-Pierre, E., Najmanovich, R. J., Fortier, L. C., Lafontaine, D., & Marsault, É. (2018). Purine analogs targeting the guanine riboswitch as potential antibiotics against Clostridioides difficile. European journal of medicinal chemistry, 143, 755–768.
• Coquerel, D., Chagnon, F., Sainsily, X., Dumont, L., Murza, A., Côté, J., Dumaine, R., Sarret, P., Marsault, É., Salvail, D., Auger-Messier, M., & Lesur, O. (2017). ELABELA Improves Cardio-Renal Outcome in Fatal Experimental Septic Shock. Critical care medicine, 45(11), e1139–e1148.
• Besserer-Offroy, É., Brouillette, R. L., Lavenus, S., Froehlich, U., Brumwell, A., Murza, A., Longpré, J. M., Marsault, É., Grandbois, M., Sarret, P., & Leduc, R. (2017). The signaling signature of the neurotensin type 1 receptor with endogenous ligands. European journal of pharmacology, 805, 1–13.
• Chagnon, F., Coquerel, D., Salvail, D., Marsault, E., Dumaine, R., Auger-Messier, M., Sarret, P., & Lesur, O. (2017). Apelin Compared With Dobutamine Exerts Cardioprotection and Extends Survival in a Rat Model of Endotoxin-Induced Myocardial Dysfunction. Critical care medicine, 45(4), e391–e398.
• Murza, A., Sainsily, X., Côté, J., Bruneau-Cossette, L., Besserer-Offroy, É., Longpré, J. M., Leduc, R., Dumaine, R., Lesur, O., Auger-Messier, M., Sarret, P., & Marsault, É. (2017). Structure-activity relationship of novel macrocyclic biased apelin receptor agonists. Organic & biomolecular chemistry, 15(2), 449–458.
• Mona, C. E., Besserer-Offroy, É., Cabana, J., Leduc, R., Lavigne, P., Heveker, N., Marsault, É., & Escher, E. (2016). Design, synthesis, and biological evaluation of CXCR4 ligands. Organic & biomolecular chemistry, 14(43), 10298–10311.
• Deny, L. J., Traboulsi, H., Cantin, A. M., Marsault, É., Richter, M. V., & Bélanger, G. (2016). Bis-Michael Acceptors as Novel Probes to Study the Keap1/Nrf2/ARE Pathway. Journal of medicinal chemistry, 59(20), 9431–9442.
• Zoratti, G. L., Tanabe, L. M., Hyland, T. E., Duhaime, M. J., Colombo, É., Leduc, R., Marsault, E., Johnson, M. D., Lin, C. Y., Boerner, J., Lang, J. E., & List, K. (2016). Matriptase regulates c-Met mediated proliferation and invasion in inflammatory breast cancer. Oncotarget, 7(36), 58162–58173.
• Mona, C. E., Besserer-Offroy, É., Cabana, J., Lefrançois, M., Boulais, P. E., Lefebvre, M. R., Leduc, R., Lavigne, P., Heveker, N., Marsault, É., & Escher, E. (2016). Structure-Activity Relationship and Signaling of New Chimeric CXCR4 Agonists. Journal of medicinal chemistry, 59(16), 7512–7524.
• Murza, A., Sainsily, X., Coquerel, D., Côté, J., Marx, P., Besserer-Offroy, É., Longpré, J. M., Lainé, J., Reversade, B., Salvail, D., Leduc, R., Dumaine, R., Lesur, O., Auger-Messier, M., Sarret, P., & Marsault, É. (2016). Discovery and Structure-Activity Relationship of a Bioactive Fragment of ELABELA that Modulates Vascular and Cardiac Functions. Journal of medicinal chemistry, 59(7), 2962–2972.
• Boulanger, S., Mitchell, G., Bouarab, K., Marsault, É., Cantin, A., Frost, E. H., Déziel, E., & Malouin, F. (2015). Bactericidal Effect of Tomatidine-Tobramycin Combination against Methicillin-Resistant Staphylococcus aureus and Pseudomonas aeruginosa Is Enhanced by Interspecific Small-Molecule Interactions. Antimicrobial agents and chemotherapy, 59(12), 7458–7464.
• Treder, A. P., Hickey, J. L., Tremblay, M. C., Zaretsky, S., Scully, C. C., Mancuso, J., Doucet, A., Yudin, A. K., & Marsault, E. (2015). Solid-Phase Parallel Synthesis of Functionalised Medium-to-Large Cyclic Peptidomimetics through Three-Component Coupling Driven by Aziridine Aldehyde Dimers. Chemistry (Weinheim an der Bergstrasse, Germany), 21(25), 9249–9255.
• Zoratti, G. L., Tanabe, L. M., Varela, F. A., Murray, A. S., Bergum, C., Colombo, É., Lang, J. E., Molinolo, A. A., Leduc, R., Marsault, E., Boerner, J., & List, K. (2015). Targeting matriptase in breast cancer abrogates tumour progression via impairment of stromal-epithelial growth factor signalling. Nature communications, 6, 6776.
• Traboulsi, H., Larkin, H., Bonin, M. A., Volkov, L., Lavoie, C. L., & Marsault, É. (2015). Macrocyclic cell penetrating peptides: a study of structure-penetration properties. Bioconjugate chemistry, 26(3), 405–411.
• Murza, A., Besserer-Offroy, É., Côté, J., Bérubé, P., Longpré, J. M., Dumaine, R., Lesur, O., Auger-Messier, M., Leduc, R., Sarret, P., & Marsault, É. (2015). C-Terminal modifications of apelin-13 significantly change ligand binding, receptor signaling, and hypotensive action. Journal of medicinal chemistry, 58(5), 2431–2440.
• Tremblay, H., St-Georges, C., Legault, M. A., Morin, C., Fortin, S., & Marsault, E. (2014). One-pot synthesis of polyunsaturated fatty acid amides with anti-proliferative properties. Bioorganic & medicinal chemistry letters, 24(24), 5635–5638.
• Treder, A. P., Tremblay, M. C., Yudin, A. K., & Marsault, E. (2014). Solid-phase synthesis of piperazinones via disrupted Ugi condensation. Organic letters, 16(17), 4674–4677.
• Murza, A., Belleville, K., Longpré, J. M., Sarret, P., & Marsault, É. (2014). Stability and degradation patterns of chemically modified analogs of apelin-13 in plasma and cerebrospinal fluid. Biopolymers, 102(4), 297–303.
• Chagnon, F., Guay, I., Bonin, M. A., Mitchell, G., Bouarab, K., Malouin, F., & Marsault, É. (2014). Unraveling the structure-activity relationship of tomatidine, a steroid alkaloid with unique antibiotic properties against persistent forms of Staphylococcus aureus. European journal of medicinal chemistry, 80, 605–620.
• Demeule, M., Beaudet, N., Régina, A., Besserer-Offroy, É., Murza, A., Tétreault, P., Belleville, K., Ché, C., Larocque, A., Thiot, C., Béliveau, R., Longpré, J. M., Marsault, É., Leduc, R., Lachowicz, J. E., Gonias, S. L., Castaigne, J. P., & Sarret, P. (2014). Conjugation of a brain-penetrant peptide with neurotensin provides antinociceptive properties. The Journal of clinical investigation, 124(3), 1199–1213.
• Beaulieu, A., Gravel, É., Cloutier, A., Marois, I., Colombo, É., Désilets, A., Verreault, C., Leduc, R., Marsault, É., & Richter, M. V. (2013). Matriptase proteolytically activates influenza virus and promotes multicycle replication in the human airway epithelium. Journal of virology, 87(8), 4237–4251.
• Colombo, E., Désilets, A., Duchêne, D., Chagnon, F., Najmanovich, R., Leduc, R., & Marsault, E. (2012). Design and synthesis of potent, selective inhibitors of matriptase. ACS medicinal chemistry letters, 3(7), 530–534.
• Mitchell, G., Lafrance, M., Boulanger, S., Séguin, D. L., Guay, I., Gattuso, M., Marsault, E., Bouarab, K., & Malouin, F. (2012). Tomatidine acts in synergy with aminoglycoside antibiotics against multiresistant Staphylococcus aureus and prevents virulence gene expression. The Journal of antimicrobial chemotherapy, 67(3), 559–568.
• Murza, A., Parent, A., Besserer-Offroy, E., Tremblay, H., Karadereye, F., Beaudet, N., Leduc, R., Sarret, P., & Marsault, É. (2012). Elucidation of the structure-activity relationships of apelin: influence of unnatural amino acids on binding, signaling, and plasma stability. ChemMedChem, 7(2), 318–325.
