PhD defence H. Wapenaar
|When:||Fr 19-01-2018 09:00 - 10:30|
Kinetics and inhibition of enzymes in early stage drug discovery
Kinetics and inhibition of enzymes in early stage drug discovery.For the development of novel drugs against diseases such as cancer or inflammatory diseases, it is important to study processes in the body. To study these processes, inhibitors of enzymes can be used. By inhibiting an enzyme, we can learn about its function in healthy or diseased conditions. In her thesis, Hannah Wapenaar has described the discovery of inhibitors for two enzymes: Lysine Acetyltransferase 8 (KAT8) and Macrophage migration inhibitory factor (MIF). Four different types of inhibitors have been described for KAT8 and the mechanism of inhibition (how the inhibitors inhibit KAT8) for each of these inhibitors has been described. This resulted in remarkable differences in the mechanism between the different inhibitors. The mechanism can influence the way these inhibitors can (or can’t) be used in the development of novel drugs. This shows that it important to investigate the mechanism of enzyme inhibitors in an early stage of their development. Additionally, novel inhibitors for MIF have been described. These inhibitors may aid in the development of novel inhibitors against inflammatory diseases.
Promotores: Prof.dr F.J. Dekker and Prof.dr. H.J. Haisma