Search Results - "Coté, Jérôme"

Expression of endogenous nuclear bradykinin B2 receptors mediating signaling in immediate early gene activation by Savard, Martin, Barbaz, David, Bélanger, Simon, Müller-Esterl, Werner, Bkaily, Ghassan, D'orléans-Juste, Pedro, Coté, Jérôme, Bovenzi, Veronica, Gobeil Jr, Fernand

“…Bradykinin (BK) represents a pro‐inflammatory mediator that partakes in many inflammatory diseases. The mechanism of action of BK is thought to be primarily…”
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Discovery and Structure–Activity Relationship of a Bioactive Fragment of ELABELA that Modulates Vascular and Cardiac Functions by Murza, Alexandre, Sainsily, Xavier, Coquerel, David, Côté, Jérôme, Marx, Patricia, Besserer-Offroy, Élie, Longpré, Jean-Michel, Lainé, Jean, Reversade, Bruno, Salvail, Dany, Leduc, Richard, Dumaine, Robert, Lesur, Olivier, Auger-Messier, Mannix, Sarret, Philippe, Marsault, Éric

“…ELABELA (ELA) was recently discovered as a novel endogenous ligand of the apelin receptor (APJ), a G protein-coupled receptor. ELA signaling was demonstrated…”
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Design, Structural Optimization, and Characterization of the First Selective Macrocyclic Neurotensin Receptor Type 2 Non-opioid Analgesic by Chartier, Magali, Desgagné, Michael, Sousbie, Marc, Côté, Jérôme, Longpré, Jean-Michel, Marsault, Eric, Sarret, Philippe

“…Neurotensin (NT) receptor type 2 (NTS2) represents an attractive target for the development of new NT-based analgesics. Here, we report the synthesis and…”
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Multitarget ligands that comprise opioid/nonopioid pharmacophores for pain management: Current state of the science by Breault, Émile, Desgagné, Michael, Neve, Jolien De, Côté, Jérôme, Barlow, Thomas M.A., Ballet, Steven, Sarret, Philippe

“…Chronic pain, which affects more than one-third of the world’s population, represents one of the greatest medical challenges of the 21st century, yet its…”
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Modulation of the Passive Permeability of Semipeptidic Macrocycles: N- and C‑Methylations Fine-Tune Conformation and Properties by Comeau, Christian, Ries, Benjamin, Stadelmann, Thomas, Tremblay, Jacob, Poulet, Sylvain, Fröhlich, Ulrike, Côté, Jérôme, Boudreault, Pierre-Luc, Derbali, Rabeb Mouna, Sarret, Philippe, Grandbois, Michel, Leclair, Grégoire, Riniker, Sereina, Marsault, Éric

“…Incorporating small modifications to peptidic macrocycles can have a major influence on their properties. For instance, N-methylation has been shown to impact…”
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C‑Terminal Modifications of Apelin-13 Significantly Change Ligand Binding, Receptor Signaling, and Hypotensive Action by Murza, Alexandre, Besserer-Offroy, Élie, Côté, Jérôme, Bérubé, Patrick, Longpré, Jean-Michel, Dumaine, Robert, Lesur, Olivier, Auger-Messier, Mannix, Leduc, Richard, Sarret, Philippe, Marsault, Éric

“…Apelin is the endogenous ligand of the APJ receptor, a member of the G protein-coupled receptor family. This system plays an important role in the regulation…”
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Development of Macrocyclic Neurotensin Receptor Type 2 (NTS2) Opioid‐Free Analgesics by Desgagné, Michael, Chartier, Magali, Lagard, Camille, Ferková, Sára, Choquette, Mathieu, Longpré, Jean‐Michel, Côté, Jérôme, Boudreault, Pierre‐Luc, Sarret, Philippe

“…The opioid crisis has highlighted the urgent need to develop non‐opioid alternatives for managing pain, with an effective, safe, and non‐addictive…”
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Size-Reduced Macrocyclic Analogues of [Pyr1]‑apelin-13 Showing Negative Gα12 Bias Still Produce Prolonged Cardiac Effects by Tran, Kien, Sainsily, Xavier, Côté, Jérôme, Coquerel, David, Couvineau, Pierre, Saibi, Sabrina, Haroune, Lounès, Besserer-Offroy, Élie, Flynn-Robitaille, Joël, Resua Rojas, Martin, Murza, Alexandre, Longpré, Jean-Michel, Auger-Messier, Mannix, Lesur, Olivier, Bouvier, Michel, Marsault, Éric, Boudreault, Pierre-Luc, Sarret, Philippe

“…We previously reported a series of macrocyclic analogues of [Pyr1]-apelin-13 (Ape13) with increased plasma stability and potent APJ agonist properties. Based…”
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ELABELA Improves Cardio-Renal Outcome in Fatal Experimental Septic Shock by Coquerel, David, Chagnon, Frédéric, Sainsily, Xavier, Dumont, Lauralyne, Murza, Alexandre, Côté, Jérôme, Dumaine, Robert, Sarret, Philippe, Marsault, Éric, Salvail, Dany, Auger-Messier, Mannix, Lesur, Olivier

“…OBJECTIVES:Apelin-13 was recently proposed as an alternative to the recommended β-adrenergic drugs for supporting endotoxin-induced myocardial dysfunction…”
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A Systematic Exploration of Macrocyclization in Apelin-13: Impact on Binding, Signaling, Stability, and Cardiovascular Effects by Trân, Kien, Murza, Alexandre, Sainsily, Xavier, Coquerel, David, Côté, Jérôme, Belleville, Karine, Haroune, Lounès, Longpré, Jean-Michel, Dumaine, Robert, Salvail, Dany, Lesur, Olivier, Auger-Messier, Mannix, Sarret, Philippe, Marsault, Éric

“…The apelin receptor generates increasing interest as a potential target across several cardiovascular indications. However, the short half-life of its cognate…”
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Constraining the Side Chain of C‑Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile by Trân, Kien, Van Den Hauwe, Robin, Sainsily, Xavier, Couvineau, Pierre, Côté, Jérôme, Simard, Louise, Echevarria, Marco, Murza, Alexandre, Serre, Alexandra, Théroux, Léa, Saibi, Sabrina, Haroune, Lounès, Longpré, Jean-Michel, Lesur, Olivier, Auger-Messier, Mannix, Spino, Claude, Bouvier, Michel, Sarret, Philippe, Ballet, Steven, Marsault, Éric

“…Side-chain-constrained amino acids are useful tools to modulate the biological properties of peptides. In this study, we applied side-chain constraints to…”
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Antitumor activity of cell‐penetrant kinin B1 receptor antagonists in human triple‐negative breast cancer cells by Dubuc, Céléna, Savard, Martin, Bovenzi, Veronica, Lessard, Andrée, Côté, Jérôme, Neugebauer, Witold, Geha, Sameh, Chemtob, Sylvain, Gobeil, Fernand

“…High nuclear expression of G protein‐coupled receptors, including kinin B1 receptors (B1R), has been observed in several human cancers, but the clinical…”
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Structure-Activity Relationship and Bioactivity of Short Analogues of ELABELA as Agonists of the Apelin Receptor by Trân, Kien, Murza, Alexandre, Sainsily, Xavier, Delile, Eugénie, Couvineau, Pierre, Côté, Jérôme, Coquerel, David, Peloquin, Maude, Auger-Messier, Mannix, Bouvier, Michel, Lesur, Olivier, Sarret, Philippe, Marsault, Éric

“…ELABELA (ELA) is the second endogenous ligand of the apelin receptor (APJ). Although apelin-13 and ELA both target APJ, there is limited information on…”
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Synthesis and Characterization in Vitro and in Vivo of (l)‑(Trimethylsilyl)alanine Containing Neurotensin Analogues by Fanelli, Roberto, Besserer-Offroy, Élie, René, Adeline, Côté, Jérôme, Tétreault, Pascal, Collerette-Tremblay, Jasmin, Longpré, Jean-Michel, Leduc, Richard, Martinez, Jean, Sarret, Philippe, Cavelier, Florine

“…The silylated amino acid (l)-(trimethylsilyl)­alanine (TMSAla) was incorporated at the C-terminal end of the minimal biologically active neurotensin (NT)…”
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The combination of opioid and neurotensin receptor agonists improves their analgesic/adverse effect ratio by Eiselt, Emilie, Côté, Jérôme, Longpré, Jean-Michel, Blais, Véronique, Sarret, Philippe, Gendron, Louis

“…Opioid and neurotensin (NT) receptors are expressed in both central and peripheral nervous systems where they modulate nociceptive responses. Nowadays, opioid…”
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The hypotensive effect of activated apelin receptor is correlated with β-arrestin recruitment by Besserer-Offroy, Élie, Bérubé, Patrick, Côté, Jérôme, Murza, Alexandre, Longpré, Jean-Michel, Dumaine, Robert, Lesur, Olivier, Auger-Messier, Mannix, Leduc, Richard, Marsault, Éric, Sarret, Philippe

“…[Display omitted] The apelinergic system is an important player in the regulation of both vascular tone and cardiovascular function, making this physiological…”
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Pain relief devoid of opioid side effects following central action of a silylated neurotensin analog by Tétreault, Pascal, Besserer-Offroy, Élie, Brouillette, Rebecca L., René, Adeline, Murza, Alexandre, Fanelli, Roberto, Kirby, Karyn, Parent, Alexandre J., Dubuc, Isabelle, Beaudet, Nicolas, Côté, Jérôme, Longpré, Jean-Michel, Martinez, Jean, Cavelier, Florine, Sarret, Philippe

“…Neurotensin (NT) exerts naloxone-insensitive antinociceptive action through its binding to both NTS1 and NTS2 receptors and NT analogs provide stronger pain…”
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Pharmacological Modulation of Blood–Brain Barrier Permeability by Kinin Analogs in Normal and Pathologic Conditions by Sikpa, Dina, Whittingstall, Lisa, Savard, Martin, Lebel, Réjean, Côté, Jérôme, McManus, Stephen, Chemtob, Sylvain, tin, David, Lepage, Martin, Gobeil, Fernand

“…The blood–brain barrier (BBB) is a major obstacle to the development of effective diagnostics and therapeutics for brain cancers and other central nervous…”
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Structure-activity relationship of novel macrocyclic biased apelin receptor agonists by Murza, Alexandre, Sainsily, Xavier, Côté, Jérôme, Bruneau-Cossette, Laurent, Besserer-Offroy, Élie, Longpré, Jean-Michel, Leduc, Richard, Dumaine, Robert, Lesur, Olivier, Auger-Messier, Mannix, Sarret, Philippe, Marsault, Éric

“…Apelin is the endogenous ligand for the G protein-coupled receptor APJ and exerts a key role in regulating cardiovascular functions. We report herein a novel…”
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Signaling Modulation via Minimal C‑Terminal Modifications of Apelin-13 by Théroux, Léa, Van Den Hauwe, Robin, Trân, Kien, Fournier, Justin, Desgagné, Michael, Meneboo, Nathan, Lavallée, Alexis, Fröhlich, Ulrike, Côté, Jérôme, Hollanders, Charlie, Longpré, Jean-Michel, Murza, Alexandre, Marsault, Eric, Sarret, Philippe, Boudreault, Pierre-Luc, Ballet, Steven

“…Apelin is an endogenous peptide that is involved in many diseases such as cardiovascular diseases, obesity, and cancer, which has made it an attractive target…”
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