Projects
Design, synthesis and evaluation of protein kinase D inhibitors forcancer treatment KU Leuven
Cancer is gradually becoming the leading cause of premature death in our global society. In Europe, approximately one in three develops cancer before the age of 75. With a global death rate of almost 10 million individuals per year, there is a clear need for better treatments. This thesis aimed at developing novel and potent small molecule inhibitors of Protein Kinase D (PKD), an attractive anti-cancer drug target.
In first instance, ...
Structural biology in aid of the design of next generation PKD2 inhibitors KU Leuven
Multiple clinically inhibitors targeting protein kinase D2 (PKD2) are available, but all of these compounds are currently ATP-competitive and lack target sensitivity. As PKD1 has an opposing effect to the PKD2, this selectivity is essential. Recently, the host laboratory identified a series of compounds named AllStars (Allosteric Stabilizers) targeting PKD2 in an allosteric and PKD2 specific way. Therefore, the main goal of my project is to ...
Rational design of tRNA synthetase inhibitors as new antibacterials. KU Leuven
Since their development in the 20th century, antibiotics and the introduction of general hygiene have played a major part in improving human health by combating different kinds of infections. However, the widespread (mis)use of antibiotics has lead to increasing development of antibiotic resistant bacteria which has become a major problem worldwide. This has obviated the need for continuous development of new drugs able to ward off these ...
Design and synthesis of inhibitors of the MEP pathway Ghent University
Fosmidomycin and multiple analogues of this natural phosphonate product demonstrate promising
antiplasmodial activitiy, but fail to show promising antibacterial activity even when the inhibitory
activity for bacterial and plasmodial DXR is comparable. This projects therefore aims at discovering
new DXR inhibitors with improved bacterial uptake by applying the eNTRy Rules and prodrug
strategies.
...Design, synthesis and biological evaluation of novel ferroptosis and necroptosis inhibitors. University of Antwerp
Design and development of FabV inhibitors as a new class of antibacterials for pathogenic Gram-negative bacteria KU Leuven
Due to the rapid spread and continuous threat of antimicrobial resistance (AMR), there is an urgent need for the development of novel classes of antibiotics. Despite a renewed public interest, the current pace of drug development will be insufficient to overcome the looming AMR crisis. Therefore, the identification of novel drug targets and the design of inhibitors for these targets is of primordial importance. The fatty acid synthesis ...
Structure-based design and synthesis of nucleoside-triphosphate analogs as new classes of viral polymerase inhibitors KU Leuven
Nucleoside analog inhibitors (NIs) are well-established antiviral drugs. In order to be an active substrate-mimic, an NI must undergo three consecutive phosphorylation steps by three distinct cellular kinases to add α-, β-, and ɤ-phosphates, and the resulting triphosphate form of an NI is the substrate of the viral polymerase. However, the efficiency of phosphorylation steps is a bottleneck for high efficacy of an NI drug. In this project, we ...
“Design and synthesis of inhibitors of the SARS-CoV-2 main protease based on the 1,2,3-triazole scaffold” KU Leuven
This project is focused towards obtaining new chemical entities with potential application to the pharmacological management of COVID-19 disease, pathology caused by infection with the SARS-CoV2 virus. The rapid worldwide spread of this disease has outlined the high priority of scientific efforts towards the discovery and obtaining of new therapies based on small molecule drugs, complementing the effectiveness of vaccines approved to date. In ...