Chimie et biocatalyse

Pathogenic protozoans of the trypanosomatid group still remain a major world health problem. Cycling between insect vectors and mammalian hosts, Trypanosoma cruzi is the causative agent of Chagas disease, while over 20 Leishmania species […]

AEGIS is a Marie Skłodowska -Curie Innovative Training Network (ITN) for early stage researchers (ESR) funded by the European Commission under the H2020 Programme the EU framework programme for research and innovation. The principal […]

IMPDH from Pseudomonas aeruginosa (see Inosine-5′-monophosphate dehydrogenase project) was found to be allosterically regulated by MgATP (Labesse et al., 2013). The discovery of this mode of regulation of the catalytic activity, never described before […]

TMPK from Mycobacterium tuberculosis belongs to the NMPK family, which was chosen as potential targets for the development of new antimicrobials (see “Nucleoside monophosphate kinases” project). Based on the 3D-structure of TMPK from M. […]

The use of light from the abyss in biology   In the last decades, bioluminescent systems based on the expression of a luciferase and the addition of a luciferin to monitor the emission of […]

A selective antimycobacterial effect This project started from the modest but rather selective antimycobacterial effect of “dibenzofuran” derivatives such as compounds 1 and 2. Their minimum inhibitory concentration necessary to prevent 99 % (MIC […]

Nucleoside analogues as potential antitumor agents.   This project aims to characterize and validate the nucleotide N-hydrolase DNPH1 as a new target in oncology. Inhibition of Rcl alone or in combination with other chemotherapeutic drugs […]

A thousand fold improvement of an antiviral activity   The starting point of this project was the modest activity displayed by compounds 1 and 2, on the phenotypic Measles-based antiviral assay designed by Pierre-Olivier […]

Organic synthesis, still the limiting factor of Medicinal Chemistry?   This ongoing project is based on our reviews (1-3) on the inhibitors of the ATPase functions of human heat shock protein 90 (HSP90) or […]

NAD mimics as potential antibacterial agents The NAD(P) biosynthesis pathways have attracted recent interest as a source of enzyme targets for the development of antimicrobial agents. Our own research focused on the structure-based development […]

Removing “chemical blind spots”, the case of the hydroxpyrazoles The synthesis of 5-hydroxypyrazoles has been trivial for about 140 years. Indeed, the synthetic path found by Knorr in 1883 was extensively used over the […]

 Inosine-5′-monophosphate dehydrogenase (IMPDH) is ubiquitously essential for the biosynthesis of guanosine nucleotides and catalyzes the NAD-dependent oxidation of IMP to XMP. IMPDH is a major target in the design of both antitumor and immunosuppresive […]

NMPKs are ubiquitous enzymes, which catalyze the reversible transfer of phosphoryl group from ATP to an NMP, and are essential for cell division, growth and metabolism. In bacteria there are five NMPKs, each one […]