Concept

Suicide inhibition

Publications associées (64)

Pyrrolidine derivatives as new inhibitors of alpha-mannosidases and growth inhibitors of human cancer cells

Pierre Vogel, Sandrine Gerber, Hélène Fiaux

New pyrrolidine-3,4-diol derivatives were prepared from D-(-)- and L(+)-phenylglycinol and tested for their ability to inhibit 25 commercial glycosidases. The influence of the substitution of the lateral side chain and of the pyrrolidine ring on the enzyme ...

2006

New 1-amino-1-deoxy- and 2-amino-2-deoxy-polyhydroxyazepanes: synthesis and inhibition of glycosidases

Pierre Vogel, Eliazar Rodriguez Garcia

Eight new seven-membered ring iminoalditols, displaying an amino group and a hydroxymethyl group on the ring, have been synthesized from D-arabinose via epoxidation of a protected azacycloheptene and subsequent nucleophilic opening. Three of them show a po ...

2005

Inhibition of S6 Kinase activity for the treatment of insulin resistance

Johan Auwerx

This invention provides screening methods for agents effective in treating insulin resistance through specific inhibition of S6 kinase 1 activity. Also provided are methods of treating insulin resistance by administering an effective amount of an inhibitor ...

2005

Labeling of fusion proteins of O6-alkylguanine-DNA alkyltransferase with small molecules in vivo and in vitro

Horst Vogel, Kai Johnsson, Horst Pick, Antje Keppler

The in vivo and in vitro labeling of fusion proteins with synthetic mols. capable of probing and controlling protein function has the potential to become an important method in functional genomics and proteomics. We have recently introduced an approach for ...

2004

Directed Evolution of O6-Alkylguanine-DNA Alkyltransferase for Efficient Labeling of Fusion Proteins with Small Molecules In Vivo

Horst Vogel, Kai Johnsson, Horst Pick, Alexandre Juillerat, Thomas Gronemeyer, Antje Keppler

We report here the generation of mutants of the human O6-alkylguanine-DNA alkyltransferase (hAGT) for the efficient in vivo labeling of fusion proteins with synthetic reporter mols. Libraries of hAGT were displayed on phage, and mutants capable of efficien ...

2003

Protonation states of methionine aminopeptidase and their relevance for inhibitor binding and catalytic activity

The authors have performed a computational study of different protomeric states of the methionine aminopeptidase active site using a combined quantum-mech./mol. mech. simulation approach. The aim of this study was to clarify the native protonation state of ...

2003

Covalent labeling of fusion proteins with chemical probes in living cells

Horst Vogel, Kai Johnsson, Horst Pick, Alexandre Juillerat, Thomas Gronemeyer, Antje Keppler

A general method for the specific and covalent labeling of fusion proteins in vivo is described. The approach is based on the unusual mechanism of the human DNA repair protein O6-alkylguanine-DNA alkyl-transferase, which irreversibly transfers an alkyl gro ...

2003

An immune-responsive Serpin regulates the melanization cascade in Drosophila

Bruno Lemaitre

In arthropods, the melanization reaction is associated with multiple host defense mechanisms leading to the sequestration and killing of invading microorganisms. Arthropod melanization is controlled by a cascade of serine proteases that ultimately activate ...

Elsevier2002

Investigation on the structure of the active site of monoamine oxidase-B by affinity labeling with the selective inhibitor lazabemide and by site-directed mutagenesis

Ursula Röthlisberger

The structural features of the active site of human monoamine oxidase B (MAO-B) were investigated by affinity labeling and site-directed mutagenesis. The pseudosubstrate inhibitor N-[2-aminoethyl]-5-chloro-2-pyridine carboxamide HCl (lazabemide) can be irr ...

1996

Assignment of the Absolute-Configuration of Natural Lentiginosine by Synthesis and Enzymatic Assays of Optically Pure (+)-Enantiomers and (-)-Enantiomers

Pierre Vogel

The structure and absolute configuration of natural lentiginosine isolated from plant sources was determined to be (1S,2S,8aS)-1,2-dihydroxyindolizidine ((+)-4) on the basis of the synthesis of both enantiomers (+)-4 and (-)-4 and their inhibition of amylo ...

1995

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