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Pharmacologie

Pharmacologie

Beyond arginine count: Rational engineering of amphipathic macrocyclic CPPs with enhanced intracellular delivery and endosomal escape

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Auteurs et autrices

Duc Tai Nguyen, Michael Desgagné, Ulrike Froehlich, Andréanne Laniel, Christine Lavoie, Pierre-Luc Boudreault

Docking of virtual libraries identifies small-molecule agonists of neurotensin receptors with analgesic activity

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Auteurs et autrices

Nicolas Panel, Duy Duc Vo, Harald Hübner, Mattia Deluigi, Szymon Pach, Félix Bélair, Dorothee Weikert, Christoph Klenk, Mark Hilge, Niharika Shiva, Isabelle Brochu, Jean-Michel Longpré, Frida Bällgren, Aljona Saleh, Huabin Hu, Jon Kapla, Stefanie Kampen, Israel Cabeza de Vaca, Jan Kihlberg, Nina Wettschureck, Philippe Sarret, Andreas Plückthun, Peter Gmeiner, Jens Carlsson

High thrombin activity associated with crohn’s disease induces microbiota pathogenicity contributing to mucosal inflammation

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Auteurs et autrices

Guillaume Le Cosquer, Melissa Pannier, Julie Thevenin, Laura Guiraud, Melissa David, Alexia Dumas, Elodie Meunier, Perrine Rousset, Simone Palese, Carmine Giorgio, Louis Buscail, Barbara Bournet, Cyrielle Gilletta, Adrian Culetto, Cindy Canivet, Etienne Buscail, Caroline Camaré, Laurent Alric, Céline Deraison, Nathalie Vergnolle, &Jean-Paul Motta

Improved brain penetration of neurotensin(8–13) via blood-brain barrier shuttle conjugation underlies strong analgesia

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Auteurs et autrices

Camille Lagard, Jérôme Côté, Nathan Meneboo, Shauna Barreto, Michael Desgagné, Sabrina Beaulieu, Alain Larocque, Élie Besserer-Offroy, Karine Belleville, Karyn Kirby, Jean-Michel Longpré, Michel Demeule, Philippe Sarret

Dual-target opioid/neurotensin ligands drive potent and safer analgesia in vivo

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Auteurs et autrices

Émile Breault, Jolien De Neve, Amirmohammad Ranjbaran, Alexandre Tremblay, Ines Robberechts, Frédérique Lussier, Félix Bélair, Victoria Tremblay, Brian J Holleran, Isabelle Brochu, Nicolò Bisi, Jérôme Côté, Jean-Michel Longpré, Louis Gendron, Steven Ballet, Philippe Sarret

Crosslinking-free preparation of thermoplastic triblock liquid crystal elastomer actuators

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Auteurs et autrices

Ting Liu, Jiaxin Yang, Jie Jiang, Lu Yin, Hongwei Ma, Yue Zhao, Yang Lia  and  Li Han

Trifluoromethylthio and Trifluoromethyl Functionalization of Endomorphin-1 Enhances its Hydrophobicity and Plasma Stability while Preserving its Affinity for the μ-Opioid Receptor

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Auteurs et autrices

Jure Gregorc, Jolien De Neve, Karine Guitot, Brian J Holleran, Nathalie Lensen, Louis Gendron, Thierry Brigaud, Jernej Iskra, Steven Ballet, Grégory Chaume

Biosensor-guided discovery of peptide inhibitors targeting the ribosomal protein uS5-PDCD2 chaperone interaction

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Auteurs et autrices

Zabih Mir Hassani, Frédérique Goulet, Duc Tai Nguyen, Anne-Marie Landry-Voyer, Lauren Kwiatek, Shany Gaudet, Pierre-Luc Boudreault, Taha Azad, François Bachand

Adhesion GPCR ADGRL1/Latrophilin-1 mobilizes β-arrestins as a prerequisite for endosomal restriction of G protein activation and splice-dependent scaffolds

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Auteurs et autrices

Sheila Ribalta-Mena, Ana Lilia Moreno-Salinas, Judith Hernández-Aranda, Juana Calderón-Amador, Kerlys Correoso-Braña, Vincent Vialou, Jesús Alberto Olivares-Reyes, Richard Leduc, Antony A Boucard

Using a bioluminescence resonance energy transfer (BRET2) caspase biosensor to study caspase-3 cleavage site specificity

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Auteurs et autrices

Véronique Blais, Jean-Bernard Denault

A neurotensin receptor type 1-derived pepducin acts as a biased allosteric modulator to regulate target receptor function

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Auteurs et autrices 

Rebecca L. Brouillette, Frédérique Lussier, Émile Breault, Nathan Meneboo, Malihe Hassanzadeh, Victoria Tremblay, Magali Chartier, Élora Midavaine, Laurence Ulrich, Jérôme Côté, Véronique Blais, Christine E. Mona, Jean-Michel Longpré, Michel Grandbois, Pierre-Luc Boudreault, Martin Audet, Élie Besserer-Offroy, Philippe Sarret

Unbiased characterization of COVID-19 endotypes leads to prognostication of high-risk individuals using routine blood tests

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Auteurs et autrices

William Ma, Antoine Soulé, Catherine Allard, Madeleine Durand, Karine Tremblay, Simon Rousseau, Amin Emad

Pharmacogenetic association study of cannabis use in chronic pain

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Auteurs et autrices 

William Beauchesne, Jordan Turcotte, Philippe Mercier, Flore Lavoie, Laurence Tessier, Ann-Lorie Gagnon, Catherine Allard, Elliot Fortin, Guillaume Léonard, Louis Gendron, Karine Tremblay

TMPRSS2 inhibitors with broad-spectrum efficacy against SARS-CoV-2 (JN.1) and influenza A (H1N1) viruses protect mice from influenza A infection

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Auteurs et autrices 

Lianne Presley, Jimena Pérez-Vargas, Anaïs Saintigny, Iván Villanueva, Michelle Ho, Jessica Fone, Lara Brinsden, Nidhi Kaushik, Syan Olver, Connor A H Thompson, Diana Bautista-Sánchez, Siobhan Ennis, Mike Chen, Matthew McCallum, Jack T Brown, Sára Ferková, Brian Hetrick, David Veesler, Richard Leduc, Masahiro Niikura, Pierre-Luc Boudreault, Bryce Warner, François Jean

Tunable Biased Signaling of the Angiotensin II Type 1 Receptor for Inotropy via C-Terminal Peptide Engineering and Allosteric Site Targeting

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Auteurs et autrices 

Margot Hadjadj, Malihe Hassanzadeh, Justin Martel, Marie-Frédérique Roy, Hugo Giguère, Alexandre Murza, Brian J Holleran, Yoon Namkung, Ulrike Froehlich, Richard Leduc, Mannix Auger-Messier, Stéphane A Laporte, Pierre-Luc Boudreault

Adhesion G protein-coupled receptors

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Auteurs et autrices

Tobias Langenhan, Garret R Anderson, Demet Araç, Gabriela Aust, Monserrat Avila-Zozaya, Sofie Morsing Bagger, Patrick Barth, Sandra Berndt, Stephen C Blacklow, Beatriz Blanco-Redondo, Antony A Boucard, James P Bridges, Lara-Sophie Brodmerkel, Kathleen M Caron, Yin Kwan Chung, Andrew N Dates, Virginea de Araujo Farias, Daniel Del Toro, Joseph G Duman, Felix B Engel, David M Favara, Caroline J Formstone, Chaoyu Fu, Alain Garcia De Las Bayonas, Anastasia Georgiadi, David E Gloriam, Randy A Hall, Jörg Hamann, Peter W Hildebrand, Cheng-Chih Hsiao, Bill X Huang, Jonathan A Javitch, Hee-Yong Kim, Robert J Kittel, Gunnar Kleinau, Richard Leduc, Ines Liebscher, Hsi-Hsien Lin, Joshua Linnert, Marie-Gabrielle Ludwig, David C Martinelli, Signe Mathiasen, Daniel Matúš, Mariam Melkumyan, Ana L Moreno-Salinas, Jan Mulder, Michael A Nash, Kasturi Pal, Daniel T Pederick, Nicole A Perry-Hauser, Xianhua Piao, Yu-Qi Ping, Dimitris G Placantonakis, Fabian Pohl, Simone Prömel, Mette M Rosenkilde, Laurent Sabbagh, Richard C Sando, Patrick Scheerer, Torsten Schöneberg, Elena Seiradake, Mareike Selcho, Florian Seufert, Abhishek K Singh, Georgios Skiniotis, Katja Spiess, Norbert Sträter, David Strutt, Thomas C Südhof, Jinpeng Sun, Gregory G Tall, Doreen Thor, Douglas G Tilley, Kimberley F Tolias, Mario Vallon, Erwin G Van Meir, Benoit Vanhollebeke, Giselle R Wiggin, Uwe Wolfrum, Jie Yan, Nathan A Zaidman, Yimin Zou, Nicole Scholz