Concept
Serpine
Publications associées (94)
Neurocognition and NMDAR co-agonists pathways in individuals with treatment resistant first-episode psychosis: a 3-year follow-up longitudinal study
This study aims to determine whether 1) individuals with treatment-resistant schizophrenia display early cognitive impairment compared to treatment-responders and healthy controls and 2) N-methyl-D-aspartate-receptor hypofunction is an underlying mechanism ...
Springernature2024Kidney-Specific Membrane-Bound Serine Proteases CAP1/Prss8 and CAP3/St14 Affect ENaC Subunit Abundances but Not Its Activity
The serine proteases CAP1/Prss8 and CAP3/St14 are identified as ENaC channel-activating proteases in vitro, highly suggesting that they are required for proteolytic activation of ENaC in vivo. The present study tested whether CAP3/St14 is relevant for rena ...
Basel2023Development of cyclic peptides that can be administered orally to inhibit disease targets
Christian Heinis, Manuel Leonardo Merz
Cyclic peptides can bind challenging disease targets, but their oral application is hindered by digestion and absorption issues. We developed a versatile method for the synthesis and functional screening of vast numbers of synthetic cyclic peptides and ide ...
Berlin2023Assessment of metal-based dihydrofolate reductase inhibitors on a novel mesofluidic platform
Paul Joseph Dyson, Sarah Alexandra Pais Pereira
A new miniaturized micro sequential injection coupled with the lab-on-valve (mu SIA-LOV) technique was full-blown to perform inhibitory studies on dihydrofolate reductase (DHFR). The system was used to evaluate the DHFR inhibition activity of metal-based a ...
ELSEVIER SCIENCE SA2022Bacterial matrix metalloproteases and serine proteases contribute to the extra-host inactivation of enteroviruses in lake water
Enteroviruses are ubiquitous contaminants of surface waters, yet their fate in presence of microbial congeners is poorly understood. In this work, we investigated the inactivation of Echovirus-11 (E11) and Coxsackievirus-A9 (CVA9) by bacteria isolated from ...
2022Boosted Pro-Inflammatory Activity in Human PBMCs by Lipopolysaccharide and SARS-CoV-2 Spike Protein Is Regulated by alpha-1 Antitrypsin
Florian Maria Wurm, Divor Kiseljak
For the treatment of severe COVID-19, supplementation with human plasma-purified alpha-1 antitrypsin (AAT) to patients is currently considered. AAT inhibits host proteases that facilitate viral entry and possesses broad anti-inflammatory and immunomodulato ...
MDPI2021Inhibition of Thiol‐Mediated Uptake with Irreversible Covalent Inhibitors
Jérôme Waser, Stefan Matile, Eliott Hugo Joran Le Du, Elija Grinhagena, Abhaya Kumar Mishra
Thiol-mediated uptake is emerging as method of choice to penetrate cells. This study focuses on irreversible covalent inhibitors of thiol-mediated uptake. High-content high-throughput screening of the so far largest collection of hypervalent iodine reagent ...
2021Novel inhibitors of kallikrein proteases and uses thereof
Christian Heinis, Alessandro Zorzi, Patrick Andreas Gonschorek
The present invention relates to a cyclic inhibitor of a kallikrein protease comprising or consisting of (I) the peptide (X1 (X2)(X3)R(X4)(X5)(X6)(X7)(X8)(X9)(X10)(X11) (Formula (X)), wherein (X1) is present or absent and, is preferably present, and if pre ...
2021Umpolung Of Electron-Rich Heteroarenes With Hypervalent Iodine Reagents
Five-membered heterocycles are well known for their innate nucleophilicity. In contrast, reaction of these heterocycles as electrophiles is less established and has become only recently an intensively investigated research area in synthetic chemistry. The ...
PERGAMON-ELSEVIER SCIENCE LTD2021Human proteinase 3 resistance to inhibition extends to alpha-2 macroglobulin
Polymorphonuclear neutrophils contain at least four serine endopeptidases, namely neutrophil elastase (NE), proteinase 3 (PR3), cathepsin G (CatG), and NSP4, which contribute to the regulation of infection and of inflammatory processes. In physiological co ...
2020