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Concept

Concentration inhibitrice médiane

Publications associées (26)

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

Elucidating the Role of Quaternary Structure in Modulating Macrophage Migration Inhibitory Factor (MIF) Functions

Macrophage Migration Inhibitory Factor (MIF) is a multifunctional protein and a major mediator of innate immunity. The paramount importance of MIF in the pathogenesis of many inflammatory, infectious, auto-immune and oncogenic diseases led to its emergence ...

EPFL2010

Characterization of the 5HT3 receptor in live cells and in vitro : heterologous expression, isolation and reconstitution in lipid membranes

The serotonin type 3 receptor (5HT3R) is a homopentameric, cation selective channel that mediates fast excitatory transmission in the nervous system. It is a member of the Cys-loop family of receptors that include the nicotinic acetylcholine receptor (nACh ...

EPFL2009

In vitro anticancer activity and biologically relevant metabolization of organometallic ruthenium complexes with carbohydrate-based ligands

Paul Joseph Dyson, Christian Hartinger, Alexey Nazarov, Olivier Pierre Zava, Michael Groessl, Frédéric Schmitt

The synthesis and in vitro anticancer activity of dihalo(η6-p-cymene)(3,5,6-bicyclophosphite-α-D-glucofuranoside)ruthenium(II) complexes are described. The compds. were characterized by NMR spectroscopy and ESI mass spectrometry, and the mol. structures of ...

2008

Determining a receptor-ligand interaction useful in e.g. drug screening involves repetitive application of reversibly binding fluorescent ligands with fast association-dissociation kinetics

Horst Arthur Vogel, Rudolf Hovius, Jean-Manuel Segura, Marinela Gjoni Boillat, Christoph Schreiter

NOVELTY - Determining a receptor-ligand interaction involves repeatedly contacting a cell comprising a receptor, with a ligand, of the receptor in which the ligand has a fluorescence labeling group and binds reversibly to the receptor under conditions in w ...

2006

Reversible sequential-binding probe receptor-ligand interactions in single cells

Horst Arthur Vogel, Rudolf Hovius, Jean-Manuel Segura, Marinela Gjoni Boillat, Christoph Schreiter

With the reversible sequential (ReSeq) binding assay, we present a novel approach for the ultrasensitive profiling of receptor function in single living cells. This assay is based on the repetitive application of fluorescent ligands that have fast assocn.- ...

2005