Publications
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• Desgagné M, Chartier M, Lagard C, Ferková S, Choquette M, Longpré JM, Côté J, Boudreault PL, Sarret P. (2024) Development of Macrocyclic Neurotensin Receptor Type 2 (NTS2) Opioid-Free Analgesics. Angew Chem Int Ed Engl. Aug 7:e202405941.
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• Desgagné M, Désilets A, Ferková S, Lepage M, Perreault O, Joushomme A, Lemieux G, Guerrab W, Froehlich U, Comeau C, Sarret P, Leduc R, Boudreault PL. (2024) Rational In Silico Design of Selective TMPRSS6 Peptidomimetic Inhibitors via Exploitation of the S2 Subpocket. J Med Chem. Aug 8;67(15):12969-12983.
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• Shkreta L, Toutant J, Delannoy A, Durantel D, Salvetti A, Ehresmann S, Sauvageau M, Delbrouck JA, Gravel-Trudeau A, Comeau C, Huard C, Coulombe-Huntington J, Tyers M, Grierson D, Boudreault PL, Chabot B (2024) The anticancer potential of the CLK kinases inhibitors 1C8 and GPS167 revealed by their impact on the epithelial-mesenchymal transition and the antiviral immune response. Oncotarget. May 16:15:313-325.
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• Pérez-Vargas J, Lemieux G, Thompson CAH, Désilets A, Ennis S, Gao G, Gordon DG, Schulz AL, Niikura M, Nabi IR, Krajden M, Boudreault PL, Leduc R, Jean F (2024) Nanomolar anti-SARS-CoV-2 Omicron activity of the host-directed TMPRSS2 inhibitor N-0385 and synergistic action with direct-acting antivirals. Antiviral Res. Mar 26:225:105869.
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• Le Moal E, Liu Y, Collerette-Tremblay J, Dumontier S, Fabre P, Molina T, Dort J, Orfi Z, Denault N, Boutin J, Michaud J, Giguère H, Desroches A, Trân K, Ellezam B, Vézina F, Bedard S, Raynaud C, Balg F, Sarret P, Boudreault PL, Scott MS, Denault JB, Marsault E, Feige JN, Auger-Messier M, Dumont NA, Bentzinger CF (2024) Apelin stimulation of the vascular skeletal muscle stem cell niche enhances endogenous repair in dystrophic mice. Sci Transl Med. Mar 20;16(739):eabn8529.
• Huy ML, Desgagné M, Nguyen DT, Comeau Froehlich U, Marsault E, Boudreault P-L* (2024) Insights on Structure-Passive Permeability Relationship in Pyrrole and Furan-Containing Macrocycles. J Med Chem Mar 14;67(5):3711-3726.
• Langlois J-P, Larose A, Brouillette E, Delbrouck JA, Boudreault P-L, Malouin F* (2024) Mode of Antibacterial Action of Tomatidine C3-Diastereoisomers. Molecules Jan 10:29(2):343.
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• Colombo E, Désilets A, Hassanzadeh H, Lemieux G, Marois I, Cliche D, Delbrouck JA, Murza A, Jean F, Marsault E, Richter MV, Leduc R, Boudreault PL* (2024) Optimization of Ketobenzothiazole-Based Type II Transmembrane Serine Protease Inhibitors to Block H1N1 Influenza Virus Replication. ChemMedChem Jan15:19(2):e202300458.
Cover Page ChemMedChem Volume 19, Issue 2, January 15, 2024 (PDF)
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• Langlois J-P, Larose A, Brouillette E, Delbrouck JA, Boudreault P-L, Malouin F* (2024) Mode of Antibacterial Action of Tomatidine C3-Diastereoisomers. Molecules Jan 10:29(2):343.
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• Ferková S, Froehlich U, Nepveu-Traversy M-E, Murza A, Azad T, Grandbois M, Sarret P, Lavigne P, Boudreault PL* (2023) Comparative Analysis of Cyclization Techniques in Stapled Peptides: Structural Insights into Protein-Protein Interactions in a SARS-CoV-2 Spike RBD/hACE2 Model System. Int J Mol Sci Dec 21:25(1):166.
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• Delbrouck JA, Murza A, Diachenko I, Ben Jamaa A, Devi R, Larose A, Chamberland S, Malouin F*, Boudreault PL* (2023) From garden to lab: C-3 chemical modifications of tomatidine unveil broad-spectrum ATP synthase inhibitors to combat bacterial resistance. Eur J Med Chem Dec 15:262:115886.
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• 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*, (2023) A novel class of broad-spectrum active-site-directed 3C-like protease inhibitors with nanomolar antiviral activity against highly immune-evasive SARS-CoV-2 Omicron subvariants. Emerging Microbes & Infections. 12:2246594.
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• Robillard S, Trân K, Lachance MS, Brazeau T, Boisvert E, Lizotte E, Auger-Messier M, Boudreault PL, Marsault E, Geraldes P (2023) Apelin prevents diabetes-induced poor collateral vessel formation and blood flow reperfusion in ischemic limb. Frontiers in Cardiovascular Medicine, 10:1191891
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• Millette G, Lacasse E, Binette R, Belley V, Chaumont LP, Ster C, Beaudry F, Boyapelly K, Boudreault PL, Malouin F (2023) Rationally Designed Pyrimidine Compounds: Promising Novel Antibiotics for the Treatment of Staphylococcus aureus-Associated Bovine Mastitis. Antibiotics, 12(8):1344
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• Loubane G, Robert G, Firdaus SB, Venne P, Comeau C, Boudreault PL, Komba JE, Wagner JR, Naylor S, Klarskov K (2023) Conundrum of dehydroascorbic acid and homocysteine thiolactone reaction products: Structural characterization and effect on peptide and protein N-homocysteinylation. Free Radic Biol Med, 206:111-124
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• Delbrouck JA, Desgagné M, Comeau C, Bouarab K, Malouin F, Boudreault PL (2023) The Therapeutic Value of Solanum Steroidal (Glyco)Alkaloids: A 10-Year Comprehensive Review. Molecules, 28(13):4957
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• L'Exact M, Comeau C, Bourhis A, Boisvert O, Froehlich U, Létourneau D, Marsault E, Lavigne P, Grandbois M, Boudreault PL (2023) Beyond Rule-of-five: Permeability Assessment of Semipeptidic Macrocycles. Biochim Biophys Acta Biomembr, 1865(7):184196
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• 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, 20(3):1577-1590.
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• 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, 6(2):290-305.
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• 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*, (2023) Discovery of lead natural products for developing pan-SARS-CoV-2 therapeutics. Antiviral Research. 209:105484.
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• 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
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• 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.
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• 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.
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• 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.
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• 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.
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• Leyton JF, Marsault E, Beaudoin S, Boudreault PL, Bonin MA, Lopez A. (2018) Antibody conjugate for treating and detecting bladder cancer. Patent WO 2018165752.
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• 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.
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• 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.
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