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Concept

Inhibiteur de protéase

Publications associées (21)

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

Aaron Simone Petruzzella

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

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

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

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, Florence Pojer, Rudolf Hovius, 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

Role and regulation of the melanization reaction in Drosophila immune response

Olivier Binggeli

In arthropods, the melanization reaction consists in the rapid synthesis of melanin at the site of infection and injury. A key enzyme in the melanization process is phenoloxidase (PO), which catalyzes the oxidation of phenols to quinones that subsequently ...

EPFL2013

Biofunctional Scaffold Design for Soft Tissue Regeneration

Fibrin has long been used clinically for hemostasis and sealing and has been extensively characterized as a biomaterial. Yet, in terms of harnessing its potential for use in tissue regeneration, there remains a wide gap between in vitro experimentation and ...

EPFL2011

It is All About Proteases: From Drug Delivery to In Vivo Imaging and Photomedicine

Hubert van den Bergh

Clinical studies provide overwhelming evidence for the importance of proteolytic imbalance and the upregulation of diverse protease classes in diseases such as cancer and arthritis. While the complex nature of proteolytic networks has hampered the developm ...

Bentham Science Publishers2011

Tg-aprotinin fusion proteins and matrices thereof

Jeffrey Alan Hubbell, Peter Frey

Fusion proteins containing a first domain and a second domain, where the first domain contains a crosslinkable substrate domain and the second domain contains a fibrinolysis inhibitor, are provided. In a preferred embodiment, the fibrinolysis inhibitor is ...

2011

Engineered aprotinin for improved stability of fibrin biomaterials

Jeffrey Alan Hubbell, Peter Frey

Fibrin has been long used clinically for hemostasis and sealing, yet extension of use in other applications has been limited due to its relatively rapid resorption in vivo, even with addition of aprotinin or other protease inhibitors. We report an engineer ...

2011

An integrative in silico methodology for the identification of modulators of macrophage migration inhibitory factor (MIF) tautomerase activity

Hilal Lashuel, Bruno Claude Daniel Fauvet

Macrophage migration inhibitory factor (MIF) is a major proinflammatory cytokine that has been increasingly implicated in the pathogenesis of several inflammatory, autoimmune, infectious and oncogenic diseases. Accumulating evidence suggests that the tauto ...

Elsevier2010

Trans-cis-cis-[RuCl2(DMSO)(2)(2-amino-5-methyl-thiazole)(2)], (PMRu52), a novel ruthenium(II) compound acting as a strong inhibitor of cathepsin B

Angela Casini

A novel ruthenium(II) compound, trans-cis-cis-[Ru(II)Cl-2(DMSO)(2)(2-amino-5-methyl-thiazole)(2)], (I), PMRu52 hereafter, that may be obtained from the previously described (cis and trans)[Ru(II)Cl-2(DMSO)(4)] complexes, was designed, synthesized and chara ...

2010

Rationalization of the inhibition activity of structurally related organometallic compounds against the drug target cathepsin B by DFT

Paul Joseph Dyson, Angela Casini, Fabio Edafe

A series of organometallic compds. of general formula [(arene)M(PTA)nXm]Y (arene = η6-C10H14, η-C5Me5); (M = Ru(II), Os(II), Rh(III) and Ir(III); X = Cl, mPTA; Y = OTf, PF6) have been screened for their cytotoxicity and ability to inhibit cathepsin B in vi ...

Royal Society of Chemistry2010

Multi-scale modeling of HIV-1 proteins

Marilisa Neri

The efficiency of protease inhibiting drugs is hampered by the rapid emergence of protease variants. Understanding this phenomenon requires the characterization of the salient steps of HIV-1 protease's catalytic cycle. We summarize Our investigations on th ...

2009

Intracellular 'boosting' of darunavir using known transport inhibitors in primary PBMC

Ruben Hartkoorn

center dot Antiretroviral protease inhibitors such as lopinavir and saquinavir have been shown to be substrates of ABCB1. Co-administration with the potent ABCB1 and CYP3A4 inhibitor, ritonavir, has shown improved pharmacokinetics and subsequent therapeuti ...

2009

Rational Design of an Organometallic Glutathione Transferase Inhibitor

Paul Joseph Dyson, Wee Han Ang

Double trouble: A hybrid org.-inorg. (organometallic) inhibitor was designed to target glutathione transferases. The metal center is used to direct protein binding, while the org. moiety acts as the active-site inhibitor (see picture). The mechanism of inh ...

Wiley-VCH Verlag GmbH2009

The serpin Spn5 is essential for wing expansion in Drosophila melanogaster

Giorgio Margaritondo, Vincent Gajdosik

Serpins, a superfamily of protease inhibitors, control proteolytic cascades in many physiological processes. Genomic studies have revealed the presence of a high number of serpin-encoding genes in Drosophila melanogaster, but their functions remain largely ...

University of the Basque Country Press2008

A serpin that regulates immune melanization in the respiratory system of Drosophila

Bruno Lemaitre

Epithelial tissues facing the external environment are essential to combating microbial infection. In addition to providing a physical barrier, epithelial tissues mount chemical defenses to prevent invasion of internal tissues by pathogens. Here, we descri ...

Cell Press - Elsevier2008

Secondary Metabolites from Cyanobacteria: Complex Structures and Powerful Bioactivities

Karl Gademann, Cyril Portmann

This review presents natural products from cyanobacteria. Several classes of secondary metabolites are highlighted. Toxic metabolites from these prokaryotic photosynthetic organisms include compounds such as microcystin, anatoxin and saxitoxin, which displ ...

2008