Concept

Inhibiteur de protéase

Publications associées (35)

Development of cysteine cathepsin inhibitors combined with cell type-specific delivery for the treatment of B-cell lymphoma and solid tumors

Cysteine cathepsins proteases are enzymes that play essential physiological roles, but their activity is also associated to different aspects of cancer progression and to the development of other diseases. Therefore, cysteine cathepsins are relevant and pr ...

EPFL2024

Human proteinase 3 resistance to inhibition extends to alpha-2 macroglobulin

Marc Moniatte

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

Phenylalanine Monitoring via Aptamer-Field-Effect Transistor Sensors

Nako Nakatsuka

Determination of the amino acid phenylalanine is important for lifelong disease management in patients with phenylketonuria, a genetic disorder in which phenylalanine accumulates and persists at levels that alter brain development and cause permanent neuro ...

2019

Human Kunitz-type protease inhibitor engineered for enhanced matrix retention extends longevity of fibrin biomaterials

Peter Frey, Jeffrey Alan Hubbell, Hans Mattias Larsson, Priscilla Suhasna Maithili Briquez, Kristen Lorentz

Aprotinin is a broad-spectrum serine protease inhibitor used in the clinic as an anti-fibrinolytic agent in fibrin-based tissue sealants. However, upon re-exposure, some patients suffer from hypersensitivity immune reactions likely related to the bovine or ...

2017

Therapeutic Proteins Engineered for Super-Affinity to the Extracellular Matrix in Regenerative Medicine

Priscilla Suhasna Maithili Briquez

Regenerative medicine aims to repair body tissues when natural mechanisms fail. Growth factors (GFs) are essential proteins that promote tissue regeneration upon injury, and as such, are very promising therapeutic drugs in regenerative medicine. Due to the ...

EPFL2016

DprE1-from the Discovery to the Promising Tuberculosis Drug Target

Joao Pedro De Almeida Neres

Several groups working in the field of the development of new antituberculosis drugs have recently reported active compounds targeting mycobacterial enzyme DprE1. Along with its counterpart, DprE2, it catalyses a unique epimerization reaction resulting in ...

Bentham Science Publ Ltd2014

Dithiol amino acids can structurally shape and enhance the ligand-binding properties of polypeptides

Christian Heinis, Rudolf Hovius, Florence Pojer, Shiyu Chen, Ranganath Gopalakrishnan

The disulfide bonds that form between two cysteine residues are important in defining and rigidifying the structures of proteins and peptides. In polypeptides containing multiple cysteine residues, disulfide isomerization can lead to multiple products with ...

Nature Publishing Group2014

A biocompatible "split luciferin" reaction and its application for non-invasive bioluminescent imaging of protease activity in living animals

Aurélien Godinat, Alma Rosa Morales Morales, Ghyslain Martial Alain Budin

The great complexity of many human pathologies, such as cancer, diabetes, and neurodegenerative diseases, requires new tools for studies of biological processes on the whole organism level. The discovery of novel biocompatible reactions has tremendously ad ...

2014

4-Aminoquinolone Piperidine Amides: Noncovalent Inhibitors of DprE1 with Long Residence Time and Potent Antimycobacterial Activity

John McKinney, Neeraj Dhar, Joao Pedro De Almeida Neres, François Signorino-Gelo

4-Aminoquinolone piperidine amides (AQs) were identified as a novel scaffold starting from a whole cell screen, with potent cidality on Mycobacterium tuberculosis (Mtb). Evaluation of the minimum inhibitory concentrations, followed by whole genome sequenci ...

Amer Chemical Soc2014

Unraveling the inhibitory effects of acetate on ethanol production in CEN.PK

Vassily Hatzimanikatis, Ljubisa Miskovic, Keng Cher Soh, Anirikh Chakrabarti

In this study, we used the ORACLE (Optimization and Risk Analysis of Complex Living Entities)[1] framework to study the impact of extracellular acetic acid on the S. cerevisiae metabolism with the aim to improve ethanol production in the presence of this i ...

2014

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