This thesis describes the design and development of subunit‐selective inhibitors of particular catalytically active subunits of human constitutive proteasomes and immunoproteasomes.

Promotor: H.S. Overkleeft, Co-Promotor: B.I. Florea

In the last decades, activity-based protein profiling (ABPP) has emerged as a powerful chemical tool that may aid the ever-challenging drug discovery process.

In this thesis an activity-based probe was discovered that could visualize the activity of PLAATs. With an optimized gel-based ABPP assay in hand, screening of a compound library led to the discovery of alpha-ketoamides as a hit for PLAAT3.

Promotores: H.S. Overkleeft, G.A. van der Marel, Co-promotor: B.I. Florea

Large parts of the research described in this Thesis aims at the development of oligopeptide-masked toxins and their in situ immunoproteasome-mediated activation.

Glycosidases are important enzymes in the turnover of polysaccharides and glycoconjugates, and are involved in a range of human pathologies including genetic disorders such as Gaucher and Pompe disease, but also in various cancers.

Vitamin A or retinol is essential in embryonic development, the visual cycle and the immune system.

Promotor: H.S. Overkleeft, Co-promotor: M. van der Stelt

Glycosidases are essential in fundamental biological processes and are responsible for the degradation of most (oligo)saccharides, glycolipids and glycoproteins.

Less than 1 in 10 drug candidates that enter phase 1 clinical trials actually gets approved for human use.

Endocannabinoïden - lichaamseigen marihuana – zijn veelbelovende startpunten voor geneesmiddelenonderzoek. Hoogleraar Moleculaire Fysiologie Mario van der Stelt onderzoekt of remming van hun productie ingezet kan worden tegen ontstekingen in de hersenen en de bestrijding van obesitas. Oratie op 19 o…

Congres/symposium