DUB Inhibitor Library. DUBs have many links to human diseases and for this reason are attractive drug targets. In this project we are developing a large compound library of small molecule DUB inhibitors by parallel synthesis using Echo Acoustic Liquid Dispensing. These compounds are tested on a series of DUBs with the goal to find potent, selective and cell-permeable DUB inhibitors.
Various projects. Currently I am working on the synthesis of ML-792, a SUMO E1 inhibitor. Recently I finished the development of a fluorescent UCHL-1 probe and I worked on the synthesis of novel analogues based on Neratinib – a tyrosine kinase inhibitor. Finally I am involved in the large scale preparation of γ-thiolysine, an amino acid building block we often use in peptide chemistry.
I studied Chemistry at Hogeschool Utrecht, the Netherlands. In 2006 I did my first internship in the laboratory of Prof dr. Roland Pieters in the department of Medicinal Chemistry at Utrecht University. During this internship I optimized the enzymatic synthesis of the disaccharide galabiose, a key building block which was used in the synthesis of inhibitors of the pathogen Streptococcus suis. In 2007 I finished my graduation internship at Prosensa, Leiden, the Netherlands. In this internship I worked on exon-skipping, a new strategy for the treatment of Duchenne muscular dystrophy and for this project I synthesized multiple glyco -and peptide conjugates. In 2008 I re-joined the lab of Prof. dr. Roland Pieters for a four-year period as a technician. Work was mainly focussed on the synthesis of glycodendrimers, glycosidase inhibitors and the development of ‘click’-chemistry on microarrays. In 2012 I moved to the lab of Prof. dr. Ovaa at the Netherlands Cancer Institute, Amsterdam. Since 2017, after the transition of the laboratory to Leiden, I am working as a senior technician at the LUMC in the department of Cell & Chemical Biology.
• Synthesis of Poly-Ubiquitin Chains Using a Bifunctional Ubiquitin Monomer.
van der Heden van Noort, G. J.*; Kooij, R.*; Elliott PR.; Komander, D.; Ovaa, H.
Organic Letters. 2017. doi: 10.1021/acs.orglett.7b03085
• Release of Enzymatically Active Deubiquitinating Enzymes upon Reversible Capture by Disulfide Ubiquitin Reagents.
De Jong, A.; Witting, K.*; Kooij, R.*; Flierman, D.; Ovaa, H.
Angew. Chem. Int. Ed. 2017. doi: 10.1002/anie.201706738
• Glycosidase inhibition by novel guanidinium and urea iminosugar derivatives.
Kooij, R.; Branderhorst, H.M.; Bonte, S.; Wieclawska, S.; Martin, N.I.; Pieters, R.J.
MedChemComm. 2012. doi: 10.1039/C2MD20343J