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Concept

Suicide inhibition

Publications associées (28)

A new target for gold(I) compounds: glutathione-S.transferase inhibition by auranofin

Paul Joseph Dyson, Christian Hartinger, Angela Casini

Nowadays, gold compounds occupy a relevant position constituting a promising class of experimental anticancer metallodrugs. Several research efforts have been devoted to the investigations of the pharmacological properties of gold(I) complexes bearing phos ...

Elsevier Science Inc2013

Enzyme inhibition by metal complexes: concepts, strategies and applications

Paul Joseph Dyson, Kelly Joan Kilpin

Metal complexes are increasingly being used to inhibit enzymes. The reasons for this increased interest arise from the special features that metal complexes offer, e.g. the facile construction of 3D architectures that tightly fill enzyme active sites incre ...

2013

Directed evolution of the suicide protein O⁶-alkylguanine-DNA alkyltransferase for increased reactivity results in an alkylated protein with exceptional stability

Ursula Röthlisberger, Kai Johnsson, Florence Pojer, Elizabeth Claire Brunk, Birgit Mollwitz, Simone Schmitt

Here we present a biophysical, structural, and computational analysis of the directed evolution of the human DNA repair protein O-6-alkylguanine-DNA alkyltransferase (hAGT) into SNAP-tag, a self-labeling protein tag. Evolution of hAGT led not only to incre ...

2012

Infection-induced host translational blockage inhibits immune responses and epithelial renewal in the Drosophila gut

Bruno Lemaitre, Sveta Chakrabarti

Typically, immune responses control the pathogen, while repair and stress pathways limit damage caused by pathogenesis. The relative contribution of damage to the outcome of pathogenesis and the mechanistic links between the immune and repair pathways are ...

Cell Press2012

DprE1 as a Drug Target from Mycobacterium Tuberculosis

Claudia Trefzer

Benzothiazinones (BTZs) form a new class of potent antimycobacterial agents with a minimal inhibitory concentration of 1 ng/mL against Mycobacterium tuberculosis. Although the target of BTZs has been identified as decaprenylphosphoryl--D-ribose 2- oxidase ...

EPFL2012

Study of Topoisomerase-DNA Interaction Using Atomic Force Microscopy

Livan Bladimir Alonso Sarduy

The aim of this thesis was to explore the topoisomerase-DNA interactions using atomic force microscopy (AFM) in a liquid environment. Firstly, we present a programmable microcontroller-driven injection system for the exchange of an imaging medium while usi ...

EPFL2012

Structural Basis for Benzothiazinone-Mediated Killing of Mycobacterium tuberculosis

Paul Joseph Dyson, Stewart Cole, John McKinney, Florence Pojer, Neeraj Dhar, Joao Pedro De Almeida Neres

The benzothiazinone BTZ043 is a tuberculosis drug candidate with nanomolar whole-cell activity. BTZ043 targets the DprE1 catalytic component of the essential enzyme decaprenylphosphoryl-beta-D-ribofuranose-2'-epimerase, thus blocking biosynthesis of arabin ...

American Association for the Advancement of Science2012

Thioredoxin reductase, an emerging target for anticancer metallodrugs

Angela Casini

Enzyme inhibition by cytotoxic gold(III) compounds studied with combined mass spectrometry and biochemical assays ...

2011