Protein synthesis machinery of Trypanosomatid as a therapeutic target
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 […]
FP7 Targeting the Leishmania kinome for the development of novel anti-parasitic strategies (LeishDrug)
Visceral leishmaniasis is caused by the protozoan parasites Leishmania donovani and Leishmania infantum and is a potentially fatal disease in endemic areas around the world. During the infectious cycle, Leishmania alternate between the insect […]
Inhibitors of Pseudomonas aeruginosa IMPDH
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 […]
Inhibitors of TMPK from Mycobacterium tuberculosis
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. […]
Inhibitors of the 2’-deoxyribonucleotide N-hydrolase DNPH1, an enzyme involved in cellular growth and angiogenesis
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 […]
Inhibitors of bacterial NAD kinases
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 […]
2019Crystal structure of the Trypanosoma cruzi EIF4E5 translation factor homologue in complex with mRNA cap-4, Nucleic Acids Res. 2019 Jun;47(11):5973-5987.
20192′-Deoxyribonucleoside 5′-triphosphates bearing 4-phenyl and 4-pyrimidinyl imidazoles as DNA polymerase substrates, Org. Biomol. Chem. 2019 01;17(2):290-301.
2018Enzymatic synthesis of random sequences of RNA and RNA analogues by DNA polymerase theta mutants for the generation of aptamer libraries, Nucleic Acids Res. 2018 07;46(12):6271-6284.
2017An expedient synthesis of flexible nucleosides via a regiocontrolled enzymatic glycosylation of functionalized imidazoles, Org. Biomol. Chem., 2017, 15, 8193.
20168-Thioalkyl-adenosine derivatives inhibit Listeria monocytogenes NAD kinase through a novel binding mode, Eur. J. Med. Chem. 2016, 124, 1041–1056.
2016Expedient and generic synthesis of imidazole nucleosides by enzymatic transglycosylation, Org. Biomol. Chem., 2016, 14, 3638.
2015Unprecedented formation of 8(R),5′-O-cycloribonucleosides through a triflation reaction of purine ribonucleosides, Tetrahedron, 71, 2525-2529..
2014A convenient synthesis of 4(5)-(hetero)aryl-1H-imidazoles via microwave-assisted Suzuki-Miyaura cross-coupling reaction, Tetrahedron Lett. 2014; 55(46);6347–6350.
20146-(Hetero)Arylpurine nucleotides as inhibitors of the oncogenic target DNPH1: synthesis, structural studies and cytotoxic activities, Eur J Med Chem 2014 Oct;85:418-37.
2014Synthesis of novel 9-aryl and heteroarylpurine derivatives via copper mediated coupling reaction, Tetrahedron Letters 02/2014; 55(9):1625–1627. .
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