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n0289

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Nafamostat Mesylate Blocks Activation of SARS-CoV-2: New Treatment Option for COVID-19.
Markus Hoffmann et al.
Antimicrobial agents and chemotherapy, 64(6) (2020-04-22)
E Farcaş et al.
Analytica chimica acta, 1034, 214-222 (2018-09-09)
Only few reports describe the use of capillary electrophoresis in the context of Fragment Based Drug Discovery (FBDD). In this paper, we will present a generic, fully automated, microscale electrophoretic mobility shift displacement assay that can be used in FBDD
Mizuki Yamamoto et al.
Viruses, 12(6) (2020-06-14)
Although infection by SARS-CoV-2, the causative agent of coronavirus pneumonia disease (COVID-19), is spreading rapidly worldwide, no drug has been shown to be sufficiently effective for treating COVID-19. We previously found that nafamostat mesylate, an existing drug used for disseminated
Silvia Guglietta et al.
Nature communications, 7, 11037-11037 (2016-03-22)
Excessive activation of blood coagulation and neutrophil accumulation have been described in several human cancers. However, whether hypercoagulation and neutrophilia are linked and involved in cancer development is currently unknown. Here we show that spontaneous intestinal tumorigenesis correlates with the
Holger Laux et al.
Biotechnology and bioengineering, 115(10), 2530-2540 (2018-05-20)
An increasing number of nonantibody format proteins are entering clinical development. However, one of the major hurdles for the production of nonantibody glycoproteins is host cell-related proteolytic degradation, which can drastically impact developability and timelines of pipeline projects. Chinese hamster
Ali M Alawieh et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 40(20), 4042-4058 (2020-04-16)
Despite the success of reperfusion therapy in significantly reducing the extent of infarct expansion after stroke, the effect of revascularization on poststroke neuroinflammation and the role of anti-inflammatory strategies in postreperfusion era are yet to be explored. Here, we investigate
Mizuki Yamamoto et al.
Antimicrobial agents and chemotherapy, 60(11), 6532-6539 (2016-08-24)
Middle East respiratory syndrome (MERS) is an emerging infectious disease associated with a relatively high mortality rate of approximately 40%. MERS is caused by MERS coronavirus (MERS-CoV) infection, and no specific drugs or vaccines are currently available to prevent MERS-CoV
David K Lam et al.
Pain, 156(5), 923-930 (2015-03-04)
More than half of all cancer patients have significant pain during the course of their disease. The strategic localization of TMPRSS2, a membrane-bound serine protease, on the cancer cell surface may allow it to mediate signal transduction between the cancer
Claire Rolland-Fourcade et al.
Gut, 66(10), 1767-1778 (2017-01-18)
Proteases are key mediators of pain and altered enteric neuronal signalling, although the types and sources of these important intestinal mediators are unknown. We hypothesised that intestinal epithelium is a major source of trypsin-like activity in patients with IBS and
Xi Chen et al.
Frontiers in oncology, 9, 852-852 (2019-09-26)
Nafamostat mesylate (NM), a synthetic serine protease inhibitor first placed on the market by Japan Tobacco in 1986, has been approved to treat inflammatory-related diseases, such as pancreatitis. Recently, an increasing number of studies have highlighted the promising effects of
E Farcaş et al.
Talanta, 188, 516-521 (2018-07-22)
Capillary electrophoresis (CE) instrument was used for the generation of a robust and reliable nanoreactor for enzymatic assays in the context of antithrombotic drug screening. The activity of the screened molecules was monitored in a quick and fully automated fashion
Jean-Baptiste Coty et al.
Electrophoresis, 37(17-18), 2401-2409 (2016-07-09)
Crossed immunoelectrophoresis (C-IE) is used to detect and quantify specific proteins. An application allowed the evaluation of complement system activation by nanomaterials. The work aimed to improve the C-IE toward a higher throughput and less tedious method. A new concept
Alexandra C Vrazo et al.
Blood, 126(8), e1-e10 (2015-07-01)
Growing interest in natural killer (NK) cell-based therapy for treating human cancer has made it imperative to develop new tools to measure early events in cell death. We recently demonstrated that protease-cleavable luciferase biosensors detect granzyme B and pro-apoptotic caspase
Gunnar Pejler et al.
Cell death & disease, 8(5), e2785-e2785 (2017-05-12)
It has been recognized for a long time that the secretory granules of mast cells are acidic, but the functional importance of maintaining an acidic pH in the mast cell granules is not fully understood. Here we addressed this issue
Kinya Terao et al.
Pancreas, 47(9), 1156-1164 (2018-09-08)
Severe acute pancreatitis is a highly lethal disease caused by systemic inflammatory response syndrome, leading to multiple organ failure. We recently showed that histidine-rich glycoprotein (HRG) supplemental therapy ameliorated septic acute respiratory distress syndrome due to unnecessary neutrophil activation and
Lei Zhang et al.
Scientific reports, 7(1), 4950-4950 (2017-07-12)
Psychological stress has been associated with intestinal epithelial hyperpermeability, the basic process in various functional and organic bowel diseases. In the present study, we aimed to clarify the differences and underlining mechanisms in stress-induced barrier disruption in functionally and structurally
Fabio Rabelo Melo et al.
Cell death & disease, 10(9), 659-659 (2019-09-12)
It is well established that mast cell accumulation accompanies most malignancies. However, the knowledge of how mast cells functionally impact on tumors is still rudimentary. Here we addressed this issue and show that mast cells have anti-proliferative activity on melanoma
C Andersson et al.
Clinical and experimental immunology, 177(1), 219-233 (2014-03-29)
Preclinical evidence supports targeting the C5a receptor (C5aR) in rheumatoid arthritis (RA). To support ongoing clinical development of an anti-C5aR monoclonal antibody, we have investigated for the first time the mechanism of action and the pharmacodynamics of a blocking anti-murine
Lene Halkjær et al.
Frontiers in immunology, 11, 774-774 (2020-05-21)
We aimed at establishing a sensitive and robust assay for estimation of systemic complement activation at complement component C3 level in mouse and human plasma samples. In order to capture the activation products iC3b and C3dg in a specific and
Catherine Martel et al.
PloS one, 6(4), e18812-e18812 (2011-04-29)
The activation of complement during platelet activation is incompletely understood. We sought to explore the formation of C5b-9 and anaphylatoxins binding to collagen-activated platelets. C5b-9, anaphylatoxins C3a, C4a and C5a, and anaphylatoxin receptors C3aR1 and C5aR were measured by flow
Yu-Ping Lin et al.
Molecular cell, 70(2), 228-241 (2018-04-21)
The house dust mite is the principal source of perennial aeroallergens in man. How these allergens activate innate and adaptive immunity is unclear, and therefore, there are no therapies targeting mite allergens. Here, we show that house dust mite extract
Sultan Alanazi et al.
Frontiers in immunology, 12, 804408-804408 (2021-12-21)
Mast cells are immune cells that store large amounts of mast cell-restricted proteases in their secretory granules, including tryptase, chymase and carboxypeptidase A3. In mouse mast cells, it has been shown that tryptase, in addition to its canonical location in
E Farcaş et al.
Analytica chimica acta, 984, 211-222 (2017-08-28)
With the emergence of more challenging targets, a relatively new approach, fragment-based drug discovery (FBDD), proved its efficacy and gained increasing importance in the pharmaceutical industry. FBDD identifies low molecular-weight (MW) ligands (fragments) that bind to biologically important macromolecules, then
Jean-Baptiste Coty et al.
International journal of pharmaceutics, 532(2), 769-778 (2017-04-30)
The understanding of complement activation by nanomaterials is a key to a rational design of safe and efficient nanomedicines. This work proposed a systematic study investigating how molecular design of nanoparticle coronas made of dextran impacts on mechanisms that trigger
Complement Components Showed a Time-Dependent Local Expression Pattern in Constant and Acute White Light-Induced Photoreceptor Damage.
Nicole Schäfer et al.
Frontiers in molecular neuroscience, 10, 197-197 (2017-07-06)
Kenneth J Katschke et al.
Scientific reports, 8(1), 7348-7348 (2018-05-11)
Geographic atrophy (GA), the advanced form of dry age-related macular degeneration (AMD), is characterized by progressive loss of retinal pigment epithelium cells and photoreceptors in the setting of characteristic extracellular deposits and remains a serious unmet medical need. While genetic
M Elvington et al.
Clinical and experimental immunology, 177(2), 500-508 (2014-04-16)
While there is evidence of a pathogenic role for complement in inflammatory bowel disease, there is also evidence for a protective role that relates to host defence and protection from endotoxaemia. There is thus concern regarding the use of systemic
Brooke A Pereira et al.
Biomaterials, 197, 72-85 (2019-01-15)
The tumour microenvironment plays a vital role in the development of solid malignancies. Here we describe an in vitro human prostate cancer microtissue model that facilitates the incorporation and interrogation of key elements of the local prostatic tumour microenvironment. Primary
Motomu Hashimoto et al.
The Journal of experimental medicine, 207(6), 1135-1143 (2010-05-12)
Activation of serum complement triggers Th17 cell-dependent spontaneous autoimmune disease in an animal model. In genetically autoimmune-prone SKG mice, administration of mannan or beta-glucan, both of which activate serum complement, evoked Th17 cell-mediated chronic autoimmune arthritis. C5a, a chief component
S Mantovani et al.
Journal of neuroimmunology, 276(1-2), 213-218 (2014-09-30)
Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disease, characterized by the progressive loss of motor neurons within the central nervous system. Neural degeneration and inflammatory processes, including activation of the complement system are hallmarks of this pathology. Our past
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