Article
Fisheries
Shun-ichiro Kawabata, Toshio Shibata
Summary: This article discusses the concept of autocatalytic activation, the presence of enzyme cascades in blood coagulation cascade and signal transduction and amplification systems, as well as the autocatalytic activation of prochelicerase C and the evolutionary insights into the hemolymph coagulation and complement systems in horseshoe crabs.
DEVELOPMENTAL AND COMPARATIVE IMMUNOLOGY
(2022)
Article
Fisheries
Wei Li, Wei Dou, Jin-Jun Wang
Summary: Insects rely on their immune system to fight against microbial invaders. The melanization reaction, mediated by PPO and clip serine protease, is an important immune process. This study characterizes the role of BdcSP10, a clip serine protease, in the melanization reaction and defense against microbial infection in Bactrocera dorsalis.
DEVELOPMENTAL AND COMPARATIVE IMMUNOLOGY
(2023)
Article
Chemistry, Multidisciplinary
Timothy E. G. Ferguson, James A. Reihill, S. Lorraine Martin, Brian Walker
Summary: Serine proteases play varied and important roles in biological processes, and activity-based profiling has been instrumental in pinpointing their precise roles. A range of activity-based probes targeting serine proteases have been developed, and their synthesis and application in profiling various serine proteases are described in this study.
FRONTIERS IN CHEMISTRY
(2022)
Article
Biotechnology & Applied Microbiology
Junhua Zhang, Wei Huang, Lanxin Zhang, Xiaokun Tang, Gaoyuan Sun, Lihui Zou
Summary: The research developed a method to determine protease activity by detecting the activity of an engineered zymogen. Specific protease activity, such as caspase-3, could be detected using suitable zymogen constructs. This study provides a new way to directly detect the activities of key human proteases, which could be used to monitor the efficacy and safety of tumor therapy.
APPLIED MICROBIOLOGY AND BIOTECHNOLOGY
(2022)
Article
Chemistry, Medicinal
Dasom Song, Ji-Yu Lee, Eun-Chae Park, Na-Eun Choi, Ho-Yeon Nam, Jiwon Seo, Jiyoun Lee
Summary: HTRA is a serine protease that participates in protein quality control and cellular stress responses, and is associated with several clinical disorders. Recent studies have identified HTRA as an important biomarker and potential therapeutic target, necessitating the development of an effective detection method. We have developed a series of HTRA-targeting activity-based probes with enhanced subtype selectivity and reactivity. These probes are cell-permeable and inhibit HTRA1 and HTRA2, making them valuable for identifying and validating HTRAs as important biomarkers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Biochemistry & Molecular Biology
Joanna Pianka, Natalia Gruba, Adam Lesner
Summary: West Nile Virus (WNV), a member of the flavivirus group, can cause mild or severe forms of infection, with no known medications for prevention. The research aimed to develop specific tools to determine the activity of the WNV serine proteinase.
BIOORGANIC CHEMISTRY
(2023)
Article
Immunology
Tisheng Shan, Yang Wang, Neal T. Dittmer, Michael R. Kanost, Haobo Jiang
Summary: The study reveals the presence of serine protease cascade modules in the extra-embryonic tissues of Manduca sexta eggs, which can stimulate immune responses at different stages of infection. The constitutive and inducible modules play distinct roles and may interact during bacterial inoculation. Similar mechanisms are also observed in other insect species, indicating the protective function of extra-embryonic tissues.
JOURNAL OF INNATE IMMUNITY
(2023)
Article
Chemistry, Medicinal
Adela Simkova, Tereza Ormsby, Natan Sidej, Lenka Postova Slavetinska, Jiri Brynda, Jana Beranova, Pavel Sacha, Pavel Majer, Jan Konvalinka
Summary: Novel FAP inhibitors were synthesized with nanomolar to sub-nanomolar potency, showing selectivity over DPP-IV and minimal cytotoxicity in tissue cultures. The most potent inhibitor had about 36-fold higher inhibition potency compared to previously published compounds. (C) 2021 The Authors. Published by Elsevier Masson SAS.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Carly E. Martin, Andrew S. Murray, Jacob R. Mackinder, Kimberley E. Sala-Hamrick, Michael G. Flynn, Joseph G. Lundgren, Fausto A. Varela, Karin List
Summary: In this study, a novel post-translational mechanism important for the function of TMPRSS13 was characterized. The findings provide further insight into the roles of different post-translational modifications as regulators of TMPRSS13 function and localization.
BIOLOGICAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Alba Ramos-Llorca, Lisse Decraecker, Valerie M. Y. Cacheux, Irena Zeiburlina, Michelle De Bruyn, Louise Battut, Carlos Moreno-Cinos, Davide Ceradini, Eric Espinosa, Gilles Dietrich, Maya Berg, Ingrid De Meester, Pieter van der Veken, Guy Boeckxstaens, Anne-Marie Lambeir, Alexandre Denadai-Souza, Koen Augustyns
Summary: Activity-based probes (ABP) are valuable tools for target identification and drug discovery. In this study, novel activity-based probes targeting serine proteases were synthesized and characterized. A library of probes with diverse chemical structures was developed, and their inhibitory potency and kinetic profile on a panel of serine proteases were determined. Surprisingly, reversible inhibitory mechanisms were observed for some of the high-affinity probes, challenging the conventional view of irreversible probes. This unexpected finding expands the potential applications of activity-based probes in proteomic studies and drug discovery.
FRONTIERS IN CHEMISTRY
(2023)
Article
Multidisciplinary Sciences
Olivia N. Pattelli, Dinh Dinh Ly Diec, Wanting Guo, Silvia Russi, Daniel Fernandez
Summary: This study reports the molecular basis, structure, and function of Aspergillus fumigatus oryzin. By using molecular replacement and molecular probing, the crystal structure and catalytic mechanism of oryzin were determined, revealing its substrate binding preferences. Furthermore, the binding of the enzyme to a calcium ion was found to provide structural stability.
SCIENTIFIC REPORTS
(2023)
Article
Genetics & Heredity
Hanan E. Shamseldin, Nada Derar, Hamad Alzaidan, Naif AlHathal, Abdullah Alfalah, Firdous Abdulwahab, Tariq Alzaid, Salim Alkeraye, Saud A. Alobaida, Fowzan S. Alkuraya
Summary: This article reports two consanguineous families with congenital ichthyosis, and identifies novel homozygous likely deleterious variants in PRSS8 through positional mapping and exome sequencing. The variant affecting canonical splice site was associated with reduced abundance of the normal transcript, while the missense variant altered a highly conserved residue. The phenotype observed in Prss8 knockout mice resembles the symptoms in human patients, suggesting a novel PRSS8-related ichthyosis disorder.
Article
Biochemistry & Molecular Biology
Shang-Jun Yin, Ho-Yeon Lee, Wei Wang, Jinhyuk Lee, Yong-Doo Park
Summary: In this study, we investigated the activity-structural relationship, folding behavior, and regulation of catalytic function in Euphausia superba serine protease (ESP). Our findings revealed the functional roles of serine residues as key residues of catalytic function and structural conformation in ESP, providing important insights into its activity and regulation.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Hematology
Nadia Freato, Floris P. J. van Alphen, Mariette Boon-Spijker, Maartje van den Biggelaar, Alexander B. Meijer, Koen Mertens, Eduard H. T. M. Ebberink
Summary: The study revealed that FIXa predominantly resembles the zymogen state in the absence of cofactor and substrate, and stabilization in its enzyme-like form is influenced not only by FVIII-binding, but also by interactions between the 220-loop, N-terminus, and the substrate binding site.
JOURNAL OF THROMBOSIS AND HAEMOSTASIS
(2021)
Review
Pharmacology & Pharmacy
Abdur Rauf, Anees Ahmed Khalil, Ahmed Olatunde, Muneeb Khan, Sirajudheen Anwar, Ahmed Alafnan, Kannan R. R. Rengasamy
Summary: Marine habitats are rich in diverse life forms that offer potential sources of novel bioactive compounds, including protease inhibitors with significant applications in pharmaceutical, nutraceutical, and cosmeceutical industries. Despite extensive research on protease inhibitors, many compounds have not advanced to clinical trials, highlighting the ongoing need for exploring new sources for their development.
PHARMACOLOGICAL RESEARCH
(2021)