Concept

Suicide inhibition

Related publications (64)

Inhibition of Sepiapterin Reductase through Formation of a Ternary Complex with Sulfasalazine or other Sulfa Drugs and NADP+

The mechanism of action of sulfasalazine, an anti-inflammatory drug used against inflammatory bowel diseases and rheumatoid arthritis is, despite its medical importance, still not well understood. Recently, it was shown that sulfasalazine and its metabolit ...

EPFL2014

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

Towards a new combination therapy for tuberculosis with next generation benzothiazinones

Paul Joseph Dyson, Stewart Cole, Florence Pojer, Ruben Hartkoorn, Anthony Vocat, Ming Zhang, Joao Pedro De Almeida Neres, Thierry Buclin, Benoit Lechartier

The benzothiazinone lead compound, BTZ043, kills Mycobacterium tuberculosis by inhibiting the essential flavo-enzyme DprE1, decaprenylphosphoryl-beta-D-ribose 2-epimerase. Here, we synthesized a new series of piperazine-containing benzothiazinones (PBTZ) a ...

2014

Targeting cytokine networks in KRAS-driven tumorigenesis

KRAS is one of the most commonly mutated oncogenes in human tumors, and is typically associated with aggressive disease. Despite intensive study and years of effort, KRAS has remained refractory to targeted inhibition. Given the challenge of inhibiting KRA ...

Expert Reviews2014

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

Benzothiazinones Are Suicide Inhibitors of Mycobacterial Decaprenylphosphoryl-β-

Stewart Cole, Kai Johnsson, Florence Pojer, Claudia Trefzer

Benzothiazinones (BTZs) are antituberculosis drug candidates with nanomolar bactericidal activity against tubercle bacilli. Here we demonstrate that BTZs are suicide substrates of the FAD-dependent decaprenylphosphoryl-beta-D-ribofuranose 2'-oxidase DprE1, ...

2012

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

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