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 […]
2023Synthesis and structure-activity relationship studies of original cyclic diadenosine derivatives as nanomolar inhibitors of NAD kinase from pathogenic bacteria., Eur J Med Chem 2023 Jan; 246(): 114941.
2022Structure-based design, synthesis and biological evaluation of a NAD+ analogue targeting Pseudomonas aeruginosa NAD kinase., FEBS J 2022 Aug; (): .
2020From Substrate to Fragments to Inhibitor Active In Vivo against Staphylococcus aureus., ACS Infect Dis 2020 Mar; 6(3): 422-435.
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.
2014Synthesis of novel 9-aryl and heteroarylpurine derivatives via copper mediated coupling reaction, Tetrahedron Letters 02/2014; 55(9):1625–1627. .
2012Screening and in situ synthesis using crystals of a NAD kinase lead to a potent antistaphylococcal compound., Structure 2012 Jun; 20(6): 1107-17.
2008A new synthetic access to furo[3,2-f]chromene analogues of an antimycobacterial, Bioorg. Med. Chem. 2008 Sep;16(17):8264-72.
2008Substituted benzyl-pyrimidines targeting thymidine monophosphate kinase of Mycobacterium tuberculosis: synthesis and in vitro anti-mycobacterial activity, Bioorg. Med. Chem. 2008 Jun;16(11):6075-85.