Research

Towards innovative new drugs

Expertise

Hit Discovery
Discovery of novel hits through virtual and experimental screenings
 
Computer-aided drug design
During all the process of drug discovery, in silico techniques are applied to improve the efficiency of the "hit-to-lead" optimization process.
 
Chemical synthesis of novel molecules
Various and up-to-date methodologies are used to synthesize (classical organic synthesis, microwave synthesis and continuous-flow chemistry) and purify (flash chromatography and preparative HPLC) novel compounds.
 
Pharmaceutical analysis and characterization of new compounds
New chemical entities are structurally caracterized and the purity is assessed (NMR, LC-MS, X-ray crystallography and elemental analysis). Various physicochemical properties are also evaluated (log P, pKa, solubility, stability, bioavailability and toxicity).
 
Preclinical evaluation using bioassays
The activity toward the target is measured using bioassays: in vitro such as enzymatic assays, ex vivo such as coagulation assays on plasma or in vivo in various animal models.

Research topics

Cancer

  • Structural study of the membrane protein TMEM45A involved in chemoresistance of cancer cells. Read more
  • Identification of chemosensitizing compounds, which are able to inhibit the resistance to chemotherapy induced by the TMEM45A protein. Read more
  • Design and enzymatic evaluation of new inhibitors of the serine metabolic pathway as potential anticancer agents. This research focuses on phosphoglycerate dehydrogenase (PHGDH), an interesting therapeutic target. Read more
  • Development of inhibitors of lactate dehydrogenase B (LDHB) tetramerization to block oxidative lactate metabolism and signaling in cancer. Read more

Infectiology

  • Structural studies of Mycobacterium tuberculosis phosphoserine phosphatase in order to design original inhibitors. Read more

Thrombosis

  • Development of new inhibitors targeting factor XII as potential antithrombotic agents. Read more

X-Ray Diffraction & Solid State Chemistry

  • Use of cocrystals as potential alternatives to combine drugs. Her work includes cocrystallization, physico-chemical characterization and structural determination of cocrystallized active pharmaceutical ingredients. Read more
  • Using cocrystallization to develop improved organic photochromic and thermochromic solid-state materials. Read more

Facilities

UNamur PC² platform (Physico-chemical characterization)