Review
Biochemistry & Molecular Biology
Qingyu Wu, Shuo Li, Xianrui Zhang, Ningzheng Dong
Summary: TTSPs play a crucial role in regulating adipose tissue phenotype, energy metabolism, and thermoregulation through various signaling mechanisms.
Article
Chemistry, Medicinal
Eloic Colombo, Antoine Desilets, Malihe Hassanzadeh, Gabriel Lemieux, Isabelle Marois, Dominic Cliche, Julien A. Delbrouck, Alexandre Murza, Francois Jean, Eric Marsault, Martin V. Richter, Richard Leduc, Pierre-Luc Boudreault
Summary: This study aims to develop novel antiviral drugs and innovative therapeutic strategies for influenza by modifying the peptidomimetic ketobenzothiazole protease inhibitor RQAR-Kbt. The modifications significantly improved the inhibitory potency against matriptase and the ability to block influenza virus replication in human lung cells. Targeting host cell enzymes may provide a solution to overcome the challenges of high mutational rate and drug resistance in influenza viruses.
Article
Multidisciplinary Sciences
Darius O. O. Gaymon, Robert Barndt, Hillary Stires, Rebecca B. B. Riggins, Michael. D. Johnson
Summary: Matriptase activation in breast cancer cells is mediated by ROS, which can be inhibited by the ROS inhibitor NAC, resulting in apoptosis of breast cancer cells.
Review
Biochemistry & Molecular Biology
Noora Barzkar, Zahoor Khan, Saeid Tamadoni Jahromi, Sajjad Pourmozaffar, Mohsen Gozari, Reza Nahavandi
Summary: Marine organisms are valuable sources of enzymes and their inhibitors with great therapeutic potential, particularly serine proteases and their inhibitors showing promise in biomedical applications. The uncontrolled activity of these proteases can lead to diseases, but their actions are regulated by serine protease inhibitors to maintain physiological functions.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Article
Chemistry, Medicinal
Patrick Gonschorek, Alessandro Zorzi, Tamara Maric, Mathilde Le Jeune, Mischa Schuettel, Mathilde Montagnon, Rebeca Gomez-Ojea, Denis Patrick Vollmar, Chantal Whitfield, Luc Reymond, Vanessa Carle, Hitesh Verma, Oliver Schilling, Alain Hovnanian, Christian Heinis
Summary: In this study, selective and high-affinity inhibitors of KLK5 and KLK7 were identified using phage display. The stability and half-life of the inhibitors were improved by eliminating proteaseprone sites and conjugating them to an albumin-binding peptide. These inhibitors were shown to reach the target KLKs in mouse epidermis and have the potential to control deregulated protease activity in Netherton syndrome.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Fisheries
Chen Feng, Xiaofeng Liu, Niewen Hu, Yiyang Tang, Mengzhe Feng, Zejun Zhou
Summary: The secretory serine protease Ssp1 in Aeromonas hydrophila plays a crucial role in its pathogenicity by increasing intestinal permeability and disrupting tight junctions. The mutant strain delta Ssp1 exhibited reduced virulence, but showed no differences in biofilm formation, swimming motility, and resistance to environmental stress.
FISH & SHELLFISH IMMUNOLOGY
(2022)
Correction
Biology
Gonzalo Villapalos-Garcia, Pablo Zubiaur, Rebeca Rivas-Duran, Pilar Campos-Norte, Cristina Arevalo-Roman, Marta Fernnandez-rico, Lucio Garcia-Fraile Fraile, Paula Fernandez-Campos, Paula Soria-Chacartegui, Sara Fernandez de Cordoba-Onate, Pablo Delgado-Wicke, Elena Fernandez-Ruiz, Isidoro Gonzalez-Alvaro, Jesus Sanz, Francisco Abad-Santos, Ignacio de los Santos
Summary: This study aimed to evaluate predictors of COVID-19 severity. The results showed that the TMPRSS2 genotype, dyslipidemia, sex, and the Charlson Comorbidity Index were identified as the main predictors of disease severity.
LIFE SCIENCE ALLIANCE
(2022)
Article
Immunology
Ruobing Guan, Shaoru Hu, Xiang Li, Shiheng An, Xuexia Miao, Haichao Li
Summary: This study focused on the transcriptome sequence of the Asian corn borer and identified several protease and protease inhibitor genes. One novel serine protease inhibitor gene, ACB-TIL, was found to be involved in the insect's immune response to Gram-negative bacteria and viruses. This gene has the potential to be a target for pest control.
FRONTIERS IN IMMUNOLOGY
(2022)
Review
Medicine, Research & Experimental
E. Burchacka, P. Pieta, A. Lupicka-Slowik
Summary: There are four types of antifungal drugs targeting different aspects of fungi, but increasing resistance poses a challenge to treatment options. Thus, developing new drug strategies is crucial for addressing fungal diseases effectively.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Food Science & Technology
Maram Morjen, Wassim Moslah, Imen Touihri-Baraketi, Najet Srairi-Abid, Jose Luis, Naziha Marrakchi, Jed Jebali
Summary: This study successfully cloned and expressed the first active anti-oncogenic snake venom Kunitz-type protease inhibitor, PIVL. It inhibits the growth of glioblastoma cells and blocks angiogenesis. Both native PIVL and recombinant PIVL modulate the PI3/AKT and MAPK signaling pathways.
Article
Chemistry, Medicinal
Thomas Hanke, Sebastian Mathea, Julia Woortman, Eidarus Salah, Benedict-Tilman Berger, Anthony Tumber, Risa Kashima, Akiko Hata, Bernhard Kuster, Susanne Mueller, Stefan Knapp
Summary: In this study, three highly selective LIMK1/2 inhibitors were characterized, providing potential candidate drugs for the treatment of diseases associated with LIMK dysregulation.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Immunology
Xin Zhang, Miao Li, Layla El Moussawi, Sally Saab, Shasha Zhang, Mike A. Osta, Kristin Michel
Summary: Humoral immune responses in animals are tightly controlled by regulated proteolysis, where extracellular protease cascades activate key immune proteins and enzymes. In mosquitoes, the protease network regulates melanization reactions and affects resistance against microorganisms.
FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY
(2021)
Article
Microbiology
Manon Laporte, Valerie Raeymaekers, Ria Van Berwaer, Julie Vandeput, Isabel Marchand-Casas, Hendrik-Jan Thibaut, Dominique Van Looveren, Katleen Martens, Markus Hoffmann, Piet Maes, Stefan Poehlmann, Lieve Naesens, Annelies Stevaert
Summary: The high transmissibility of SARS-CoV-2 is related to the virus's abundant replication in the upper airways, which differs from other highly pathogenic coronaviruses. The spike protein of SARS-CoV-2 exhibits intrinsic temperature preference, optimizing the virus for the human respiratory tract and enhancing its transmission. Additionally, certain proteases in the human airways play a key role in activating the spike protein for virus entry, further increasing SARS-CoV-2's ability to spread.
Article
Chemistry, Medicinal
Jimin Hwang, Natalie Strange, Rami Mazraani, Matthew J. Phillips, Allan B. Gamble, Wilhelmina M. Huston, Joel D. A. Tyndall
Summary: A new series of CtHtrA inhibitors were developed by proline ring expansion and Cg-substitutions, which showed significantly improved antichlamydial activity in vitro.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Gillian A. Kelly-Robinson, James A. Reihill, Fionnuala T. Lundy, Lorcan P. McGarvey, John C. Lockhart, Gary J. Litherland, Keith D. Thornbury, S. Lorraine Martin
Summary: COPD is a complex disease characterized by unregulated proteolytic destruction of lung tissue mediated via a protease-antiprotease imbalance. Serpins, including AAT, play a crucial role in regulating protease activity in the lungs and understanding their physiological/pathological role could lead to new therapeutic opportunities for COPD and other chronic lung diseases.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemical Research Methods
Matthieu Chartier, Etienne Adriansen, Rafael Najmanovich
Article
Gastroenterology & Hepatology
Natalie J. Ronaghan, Judie Shang, Vadim Iablokov, Raza Zaheer, Pina Colarusso, Sebastien Dion, Antoine Desilets, Richard Leduc, Jerrold R. Turner, Wallace K. MacNaughton
AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY
(2016)
Article
Chemistry, Medicinal
Catherine St-Georges, Antoine Desilets, Francois Beliveau, Mariana Ghinet, Sebastien P. Dion, Eloic Colombo, Pierre-Luc Boudreault, Rafael J. Najmanovich, Richard Leduc, Eric Marsault
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2017)
Article
Biochemistry & Molecular Biology
Erwan Lanchec, Antoine Desilets, Francois Beliveau, Anthony Flamier, Shaimaa Mahmoud, Gilbert Bernier, Denis Gris, Richard Leduc, Christine Lavoie
JOURNAL OF BIOLOGICAL CHEMISTRY
(2017)
Article
Multidisciplinary Sciences
Kelcie A. Lahey, Natalie J. Ronaghan, Judie Shang, Sebastien P. Dion, Antoine Desilets, Richard Leduc, Wallace K. MacNaughton
Article
Rheumatology
David J. Wilkinson, Angela Habgood, Heather K. Lamb, Paul Thompson, Alastair R. Hawkins, Antoine Desilets, Richard Leduc, Torsten Steinmetzer, Maya Hammami, Melody S. Lee, Charles S. Craik, Sharon Watson, Hua Lin, Jennifer M. Milner, Andrew D. Rowan
ARTHRITIS & RHEUMATOLOGY
(2017)
Article
Cell Biology
Sebastien P. Dion, Francois Beliveau, Antoine Desilets, Mariana Gabriela Ghinet, Richard Leduc
JOURNAL OF CELLULAR AND MOLECULAR MEDICINE
(2018)
Article
Multidisciplinary Sciences
David J. Wilkinson, Antoine Desilets, Hua Lin, Sarah Charlton, Maria del Carmen Arques, Adrian Falconer, Craig Bullock, Yu-Chen Hsu, Kristian Birchall, Alastair Hawkins, Paul Thompson, William R. Ferrell, John Lockhart, Robin Plevin, Yadan Zhang, Emma Blain, Shu-Wha Lin, Richard Leduc, Jennifer M. Milner, Andrew D. Rowan
SCIENTIFIC REPORTS
(2017)
Article
Multidisciplinary Sciences
Sebastien P. Dion, Francois Beliveau, Louis-Philippe Morency, Antoine Desilets, Rafael Najmanovich, Richard Leduc
SCIENTIFIC REPORTS
(2018)
Article
Multidisciplinary Sciences
Erwan Lanchec, Antoine Desilets, Francois Beliveau, Cloe Fontaine-Carbonneau, Andreanne Laniel, Richard Leduc, Christine Lavoie
SCIENTIFIC REPORTS
(2020)
Review
Chemistry, Medicinal
Alexandre Murza, Sebastien P. Dion, Pierre-Luc Boudreault, Antoine Desilets, Richard Leduc, Eric Marsault
EXPERT OPINION ON THERAPEUTIC PATENTS
(2020)
Article
Multidisciplinary Sciences
Tirosh Shapira, I. Abrrey Monreal, Sebastien P. Dion, David W. Buchholz, Brian Imbiakha, Andrea D. Olmstead, Mason Jager, Antoine Desilets, Guang Gao, Mathias Martins, Thierry Vandal, Connor A. H. Thompson, Aaleigha Chin, William D. Rees, Theodore Steiner, Ivan Robert Nabi, Eric Marsault, Julie Sahler, Diego G. Diel, Gerlinde R. Van de Walle, Avery August, Gary R. Whittaker, Pierre-Luc Boudreault, Richard Leduc, Hector C. Aguilar, Francois Jean
Summary: The COVID-19 pandemic caused by the SARS-CoV-2 virus is still a global public health crisis, with reduced efficacy of vaccination campaigns due to emerging variants of concern. Development of host-directed therapeutics and prophylactics can limit resistance and provide urgently needed protection against these variants.
Article
Multidisciplinary Sciences
Sebastien P. Dion, Antoine Desilets, Gabriel Lemieux, Richard Leduc
Summary: TMPRSS6 is a protease involved in iron homeostasis, and its different isoforms can interact and affect the activity of other proteins. Specifically, isoform 2 reduces hepcidin production by cleaving surface proteins, while isoforms 3 and 4 decrease the proteolytic activity of isoform 2 and behave as dominant negative regulators.
Article
Chemistry, Medicinal
Eloic Colombo, Antoine Desilets, Malihe Hassanzadeh, Gabriel Lemieux, Isabelle Marois, Dominic Cliche, Julien A. Delbrouck, Alexandre Murza, Francois Jean, Eric Marsault, Martin V. Richter, Richard Leduc, Pierre-Luc Boudreault
Summary: This study aims to develop novel antiviral drugs and innovative therapeutic strategies for influenza by modifying the peptidomimetic ketobenzothiazole protease inhibitor RQAR-Kbt. The modifications significantly improved the inhibitory potency against matriptase and the ability to block influenza virus replication in human lung cells. Targeting host cell enzymes may provide a solution to overcome the challenges of high mutational rate and drug resistance in influenza viruses.
Article
Biochemistry & Molecular Biology
Francois Beliveau, Aarti Tarkar, Sebastien P. Dion, Antoine Desilets, Mariana Gabriela Ghinet, Pierre-Luc Boudreault, Catherine St-Georges, Eric Marsault, Daniel Paone, Jon Collins, Colin H. Macphee, Nino Campobasso, Arthur Groy, Josh Cottom, Michael Ouellette, Andrew J. Pope, Richard Leduc
CELL CHEMICAL BIOLOGY
(2019)