Pierre-Luc Boudreault

Prix et distinctions

• FQRNT - Master's (B1X) Research Scholarships. Fonds de recherche du Québec - Nature et technologies (FRQNT). (Prize / Award).
• FQRNT Postdoctoral Research Scholarship. Fonds de recherche du Québec - Nature et technologies (FRQNT). (Prize / Award).
• NSERC - Canada Graduate Scholarships-Doctoral program. Natural Sciences and Engineering Research Council of Canada (NSERC). (Prize / Award).

Financement

• Grant. (Awarded). Co-investigator. Journey to the Center of the Cell: Reprogramming intracellular transport to the nucleus enhances HER2+ tumor killing for trastuzumab conjugated to payloads active in the nucleus. Canadian Institutes of Health Research (CIHR). Project Grant. 581 400 $. (2021-2026)
• Grant. (Awarded). Co-investigator. Functional and structural understanding of angiotensin II type 1 receptor biased signaling. Canadian Institutes of Health Research (CIHR). Project Grant. 1 189 576 $. (2021-2025)
• Grant. (Awarded). Co-investigator. Acuité-Qc Consortium: predicting and visualizing drug action. Québec Consortium for Drug Discovery (CQDM). Fonds d’Accélération des Collaborations en Santé. 26 398 352 $. (2021-2024)
• Grant. (Awarded). Co-investigator. Cell-based plasmonic biosensor for the quantification of SARS-CoV-2 incorporation in live cells.. Institut de Pharmacologie de Sherbrooke. IPS-Innovation fund. 40 000 $. (2021-2023)
• Grant. (Awarded). Co-applicant. Exploiting ELABELA and analogues to protect from septic shock. Canadian Institutes of Health Research (CIHR). 318 431 $. (2021-2023)
• Grant. (Awarded). Co-applicant. Structure-fonction et dynamique du récepteur à l'apeline, une cible prometteuse pour les maladies cardiovasculaires. Fonds de recherche du Québec - Santé (FRQS). 381 000 $. (2021-2023)
• Grant. (Awarded). Principal Applicant. Start-up Grant. FMSS and CRCHUS. Fonds de démarrage. 40 000 $. (2021-2023)
• Grant. (Awarded). Co-investigator. Role, regulation, and functions of the delta opioid receptor in the treatment of pain. Canadian Institutes of Health Research (CIHR). 967 725 $. (2021-2023)
• Grant. (Awarded). Co-applicant. Preventing SARS-CoV-2 infection by targeting human type II transmembrane serine protease activity. Canadian Institutes of Health Research (CIHR). 856 000 $. (2020-2022)
• Grant. (Awarded). Co-applicant. Targeting TMPRSS6 to treat hepcidin-deficiency disorders. Canadian Institutes of Health Research (CIHR). 192 015 $. (2021-2022)
• Grant. (Awarded). Principal Investigator. Use of the peptide transporter Angiopep-2 for the passage of non-permeable radiotracers across the blood-brain barrier. L’Axe d’imagerie médicale (AIM) du Centre de recherche du CHUS (CRCHUS) et le Centre d’imagerie médi. Programme d’Aide aux Jeunes Chercheurs (AJC) de l’AIM/CIMUS. 15 000 $. (2021-2022)
• Grant. (Awarded). Co-investigator. Development of a new class of antibiotics specific for Staphylococcus and bovine mastitis. Regroupement FRQNT pour un lait de qualité optimale Op+Lait. Nouvelle Initiative. 22 500 $. (2021-2022)
• Grant. (Awarded). Principal Applicant. Targeting Endogenous Repair: A Novel Mutation Independent Pharmacological Approach for the Treatment of Muscular Dystrophy. Stem Cell Ntework. Stem Cell Network research award. 62 233 $. (2021-2022)
• Grant. (Awarded). Co-investigator. Bacterial ATP synthase inhibitors – A novel approach toward antibiotics targeting difficult-to-treat Gram-positive and Gram-negative bacterial infections. Amorchem Therapeutics and CQDM. SynergiQc. 1 459 041 $. (2020-2021)
• Contract. (Awarded). Principal Investigator. Immune Biosolution - Generation of spatial epitopes for membrane targets (GPCR). Immune Bioslolution. Service Cotract. 30 690 $. (2020-2021)
• Grant. (Awarded). Co-investigator. New antibiotic combination for MRSA and Pseudomonas aeruginosa in cystic fibrosis. Cystic Fibrosis Canada. Strategic Projects. 300 000 $. (2018-2021)
• Contract. (Awarded). Principal Investigator. Synthesis of macrocycles - proprietary molecules. Bayer AG. Bayer Ag Research Contract. 1 300 000 $. (2021-2021)

Publications

Articles de revue

• Shapira, T; Monreal, IA; Dion, SP; Jager, M; Desilets, A; Olmstead, AD; Vandal, T; Buchholz, DW; Imbiakha, B; Gao, G; Chin, A; Rees, WD; Steiner, T; Nabi, IR; Marsault, E; Sahler, J; August, A; Van de Walle, G.Whittaker, GR; Boudreault, PL; Aguilar, HC; Leduc, R: Jean, F. (2021). A Novel highly potent inhibitor of TMPRSS2-like proteases blocks SARS-CoV-2 variants of concern and is broadly protective against infection and mortality in mice. bioRxiv (Published).
• Normandin, C*; Boudreault, PL. (2021). Concise Large-Scale Synthesis of Tomatidine, A Potent Antibiotic Natural Product. Molecules 26 (19), 6008. DOI. (Published).
• Binette, R*; Desgagné, M*; Theaud, C*; Boudreault, PL. (2021). Efficient Fmoc-protected amino ester hydrolysis using green calcium(II) iodide as a protective agent. The Journal of Organic Chemistry jo-2021-02465w (Submitted).
• 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. (Published).
• Shapira, T; Monreal, IA; Dion, SP; Jager, M; Dion, SP; Buchholz, D; Imbiakha, B; Mason, J; Désilets, A; Olmstead, AD; Vandal, T*; Buchholz, DW; Imbiakha, B; Gao, G; Chin, A; Rees, WD; Steiner, T; Marsault, E; August, A; Van de Walle, G; Whittaker, GR; Aguilar, HC; Boudreault, PL; Leduc, R; Jean, F;. (2021). Novel highly potent inhibitor of TMPRSS2-like proteases acts as a pan-SARS-CoV-2 prophylactic and therapeutic. Nature (Revision Requested).
• 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. (Published).
• Tran, K*; Sainsily, X; Côté, J; Coquerel, D; Couvineau, P; Saibi, S; Haroune, L; Besserer-Offroy, E; Flynn-Robitaille, J*; Resua Rojas, M; Longpré, JM; Auger-Messier, M; Lesur, O; Bouvier, M; Marsault, E; Sarret, P, Boudreault, PL. (2021). Size-reduced macrocyclic analogs of[Pyr1]-apelin-13 showing negative Gα12 bias still produce prolonged cardiac effects. Journal of Medicinal Chemistry (Submitted).
• Murza, A*; Dion, SP; Boudreault, PL, Désilets, A; Leduc, R; Marsault, E. (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. (Published).
• 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. (Published).
• Béliveau F; Tarkar A; Ghinet MG; Dion SP; Boudreault PL; Désilets A; St-Georges 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. (Published).
• Klarskov K; Gagnon H; 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. (Published).
• Klarskov, K; Gagnon, H; Boudreault, PL; Normandin, C*; Plancq, B; Marsault, E; Gleich, GJ; Naylor, S. (2018). Structure determination of disease-associated peak AAA from L-tryptophan implicated inthe eosinophiliamyalgia syndrome. Toxicology Letters 282 71-80. (Published).
• Lamontagne-Boulet, M; Isabelle, C; Guay, I; Brouillette, E; Langlois, JP; Jacques, PE; Rodrigue, S; Brzezinski, R; Beauregard, PB; Bouarab K, Boyapelly K*, Boudreault PL, Marsault E, Malouin F. (2018). Tomatidine, a lead antibiotic molecule that targets Staphylococcus aureus ATP synthase subunit C. Antimicrobial Agents and Chemotherapy 62 (6), e02197-17. (Published).
• Berube, C; Barbeau, X; Cardinal, S; Boudreault, PL; Bouchard, C; Delcey, N; Lague, P; Voyer, N. (2017). Interfacial supramolecular biomimetic epoxidation catalyzed by cyclic dipeptides. Supramolecular Chemistry 29 (5), 330-349. (Published).
• 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. (Accepted).
• Paquette, M; Vilera-Perez, LG; Beaudoin, S; Ekindi-Ndongo, N; Boudreault, PL; Bonin, MA; Battista, MC; Bentourkia, M; Lopez, AF; Lecomte, R; Marsault, E; Guérin, B; Sabbagh, R; Leyton, JV. (2017). Targeting IL5Ra with antibody-conjugates reveals a strategy for imaging and therapy for invasive bladder cancer. Oncoimmunology 6 (10), e1331195. (Published).
• Berube, C; Cardinal, S; Boudreault, PL; Barbeau, X; Delcey, N; Giguere, M; Gleeton, D; Voyer, N. (2015). Novel chiral N,​N'-​dimethyl-​1,​4-​piperazines with metal binding abilities. Tetrahedron 71 (42), 8077-8084. (Published).
• 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. (Published).
• Duchêne D, Colombo E*, Désilets A, Boudreault PL, Leduc R, Marsault E, Najmanovich R. (2014). Analysis of subpocket selectivity and identification of potent selective inhibitors for matriptaseand matriptase-2. Journal of Medicinal Chemistry 57 (23), 10198-204. (Published).

Chapitres de livre

• Boudreault, PL; Comeau, C; Marsault, E. (2021). Macrocycles as Inhibitors of Protein–Protein Interactions. Ali Tavassoli. Inhibitors of Protein–Protein Interactions: Small Molecules, Peptides and Macrocycles (The Royal Society of Chemistry, 17, 200-276). United Kingdom : Ali Tavassoli. (Published).

Propriétés intellectuelles

Patents

• Boudreault PL; Marsault E; Traboulsi H; Sarret P; Neveu-Traversy ME; Gaudreau S; Leduc F; Larrivé JF; Arcan M. Antibodies specific for NTSR1 and uses thereof. PCT/CA2019/051216. United States. (Pending).
• Boudreault PL; Leyton JV; Beaudoin S; Bonin MA; Lopez A. Antibody conjugate for treating and detecting bladder cancer. PCT/CA2017/051575. Canada. (Pending).
• Boudreault PL; Leyton JV; Beaudoin S; Bonin MA; Lopez A. Antibody conjugate for treating and detecting bladder cancer. 16/493845. United States. (Pending).
• Boudreault PL; Marsault E; Planc B, Colombo E; Leduc R; Richter M. Matriptase Inhibitor and uses thereof. 20190337981. Canada. (Pending).
• Boudreault PL; Marsault E; Planc B, Colombo E; Leduc R; Richter M. Matriptase inhibitors and therapeutic uses thereof. CA3085853. Canada. (Pending).
• Boudreault PL; Marsault E; Planc B, Colombo E; Leduc R; Richter M. Matriptase inhibitors and therapeutic uses thereof. 16/471979. United States. (Allowed).
• Boudreault PL; Marsault E; Planc B, Colombo E; Leduc R; Richter M. Matriptase inhibitors and uses thereof. PCT/CA2017/051575. United States. (Pending).
• Prostratin analogs, bryostatin analogs, prodrugs, synthetic methods, and methods of use. United States. (Pending).

Licenses

• License agreement with Amorchem Therapeutics, Inc. related to patents on steroid alkaloids as inhibitors of bacterial ATP synthase. (Granted).
• Research agreement with licence: matriptase inhibitors for the treatment of influenza. (Granted).
• TTSP inhibitors for the treatment of SARS-CoV-2 (Ebvia). (In Negotiation).

Autres contributions

Cours enseignés

• Biochimie. BCM300. (45CR).
• Chimie Médicinale Avancé. PHR714.

Activités de collaboration internationale

• Collaborator - Jen Carlsson. Sweden. Synthesis and characterization of Neurotensin modulators.
• Collaborator - Gary Whittaker. United States. Test TMPRSS2 inhibitors on mice.
• Collaborator - Tom Maier. United Kingdom. Crystallization of the ATP synthase.
• Collaborator - Hector Aguilar-Carreno. United States. Test small molecule inhibitors SARS-Cov-2.

Présentations

• Binette R; Lacasse E; Milette G; Beaudry F; Rico D; Malouin F. (2021). Antibioswitch: Un traitement ciblé contre Staphylococcus aureus en mammite bovine. Op+lait 2021, Rendez-vous scientifique annuel d'Op+lait. St-Hyacinthe, Canada
• T Nguyen Duc, C Lavoie. (2021). Library Synthesis of Peptoid-based Guanidine-rich Transporters. Journée Phare. Orford, Canada
• T Shapira, A Monreal, S P. Dion, M Jager, A Désilets, A D. et al. (2021). L’inhibition de TMPRSS2 empêche l’infection par le SRAS-CoV-2. 9e journée scientifique du DOCC : Les maladies cardiométaboliques. Canada
• T Shapira, A Monreal, S P. Dion, M Jager, A Désilets, A D. et al. (2021). Type II transmembrane serine protease inhibitors prevent SARS-CoV-2 infection. ASBMB – Serine Proteases in Pericellular Proteolysis and Signaling. United States
• C Normandin, F Malouin, E Marsault. (2019). Efforts towards the hemisynthesis of tomatidine – a naturally occurring steroid alkaloid targeting persistant forms of Staphylococcus aureus. Canadian Society for Chemistry National Meeting. Québec, Canada
• MF Oye Mi-mba Mintsa, A Désilets, R Leduc, E Marsault. (2019). Optimization of matriptase-2 inhibitors. Canadian Society for Chemistry National Meeting. Québec, Canada
• Laurent Bruneau-Cossette, Hassan Traboulsi, Marie-Edith Nepveu-Traversy, Djordje Grbic, Simon Gaudreau, Fernand-Pierre Gendron, Fernand Gobeil and Philippe Sarret, Éric Marsault. (2019). Structure-based design of macrocyclic peptide to generate functional antibodies against GPCR. GPCR Retreat. Canada
• C Normandin, K Klarskov, H Gagnon, B Plancq, E Marsault. (2018). Structure determination of disease-associated peak AAA from L-Tryptophan implicated in eosinophikia-myalgia syndrome (EMS). Canadian Society for Chemistry National Meeting. Edmonton, Canada
• Baptiste Plancq, Éloïc Colombo, Pallavi Thakur, Émilie Gravel, Antoine Désilets, Isabelle Marois, Dominic Cliche, Alexandre Cloutier, Richard Leduc, Martin Richter, Éric Marsault. (2018). Tomatidine : vers une nouvelle classe d’antibiotiques prometteurs contre les formes persistantes de S. Auréus. 86e Congrès de l'ACFAS. Canada
• Nepveu-Traversy M.E., Morissette S., Besserer-Offroy É., Kirby K., Longpré J.M., Gendron F.P., Breton B., Marsault E., Gaudreau S, and Sarret P. (2017). Characterization of chicken antibodies targeting the 3D structure of the second extracellular loop of the neurotensinreceptor type 1. 14th Annual Protein and Antibody Engineering Summit. Boston, United States
• ME Nepveu-Traversy, S Morissette, E Besserer-Offroy, K Kirby, JM Longpré, FP Gendron, B Breton, E Marsault, S Gaudreau, P Sarret. (2017). Chicken antibodies engineered to target the 3D structure of extracellular loops of GPCRs. Great Lakes GPCR Retreat. Ottawa, Canada
• E Besserer-Offroy, C Mona, R Brouillette, K Belleville, JM Longpré, R Leduc, E Marsault, P Sarret. (2017). Phosphomimetic lipopeptides as new tools to investigate beta-arrestin functions. Great Lakes GPCR Retreat. Ottawa, Canada
• 31. F Béliveau, SP Dion, C St-Georges, M Ghinet, A Désilets, E Marsault and R Leduc. (2017). Targeting TMPRSS6 activity as a potential treatment for iron-overload disorders. International Proteolysis Society. Banff, Canada
• (2016). 3D-specific IgY antibodies targeting GPCR loops. PEGS Meeting. Boston, United States
• ME Nepveu-Traversy, S Morissette, K Kirby, B Breton, E Marsault, S Gaudreau, P Sarret. (2016). Caractérisation d’anticorps IgY reconnaissant la structure 3D de la deuxième boucle extracellulaire du récepteur NTS1 de la neurotensine. Journée Phare. Bromont, Canada
• E Marsault, A Griffin, B Brown, R Leduc, M Richter. (2016). Host-based inhibitors of type 2 transmembrane serine proteases as a promising approach for the treatment of influenza. Tetrahedron Symposium. Barcelona, Spain
• Élie Besserer-Offroy, Christine Mona, Pierre-Luc Boudreault, Jean-Michel Longpré, Richard Leduc, Éric Marsault, and Philippe Sarret. (2016). Phosphomimetic lipopeptides as new tools to investigate β-arrestin-mediated functions. Neurosciences 2016. San Diego, United States
• C St-Georges, A Désilets, SP Dion, R Najmanovich, R Leduc, E Marsault. (2016). Synthesis and Characterization of Potent and Selective Inhibitors for Matriptase-2. CSC National Meeting. Halifax, Canada
• M Azzi, A Griffin, B Brown, R Leduc, M Richter and E Marsault. (2015). A successful industry-academia collaboration toward the development of new host-based antivirals against influenza. Pacifichem 2015. Honolulu, United States
• E Colombo, P Thakur, E Gravel, A Désilets, I Marois, D Cliche, A Cloutier, A Griffin, B Brown, R Leduc, M Richter and E Marsault. (2015). Host-based serine protease inhibitors as an emerging treatment against influenza. Pacifichem 2015. Honolulu, United States
• E Colombo, P Thakur, E Gravel, A Désilets, I Marois, D Cliche, A Cloutier, R Leduc, M Richter, E Marsault. (2015). Peptidomimetic inhibition of host-targeted serine proteases as a treatment against influenza. CSC National Meeting. Halifax, Canada
• E Marsault, E Colombo, P Thakur, I Marois, A Désilets, R Leduc, M Richter. (2014). New inhibitors of matriptase against influenza. European Peptide Symposium. Sofia, Bulgaria