The chemical synthesis of inhibitors and probes targeting endo-glycosidases.

Due to their central physiological roles in living organisms, retaining beta-glycosidases have been the subject of tremendous research efforts to examine their structure/function relation using numerous biophysical and biochemical approaches.

To this day, all cyclophellitol-based inhibitors and ABPs have been close analogues of their natural substrate counterparts. As a result, these probes showed high selectivity towards their target glycosidases.

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.

Promotores: Prof.dr. H.S. Overkleeft, Prof.dr. G.A. van der Marel

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

The studies described in this thesis deal with glycosidases, in particular alpha-galactosidases.

Promotores: Prof.dr. H.S. Overkleeft, Prof.dr. G.A. van der Marel

Synthetic methodlogy is described, aiding in the synthetic preparation of putative inhibitors of retaining and inverting glycosidases and glycosyl transferases. All constructs are cyclophellitol-based cyclitols.

Glycosidases (GHs) are enzymes responsible for the degradation of carbohydrates and play many roles in human health and pathophysiology. Often, abnormal levels of glycosidase activity are markedly linked to human pathologies.

Professor Hermen Overkleeft ontvangt de prestigieuze Roy L. Whistler International Award 2024 van de International Carbohydrate Orgasation. De prijs is een erkenning voor Overkleefts bijdrage aan de koolhydraat- en biochemie.

This thesis focuses on the design and synthesis of activity-based probes and inhibitors targeting enzymes involved in the degradation of specific plant glycans.

Student Molecular Science and Technologie Madouc Bergers maakte voor haar bachelorscriptie zelf een molecuul dat de afbraak van suikers kan remmen. Hoewel het de meeste studenten niet eens lukt om één bouwsteen te maken, maakte Madouc er drie. Mede hierdoor is ze genomineerd voor de Science Young Talent…