Chemical Biology & Drug Discovery

Our research
Histone modication by PRMTs

The Chemical Biology & Drug Discovery group (formerly Medicinal Chemistry and Chemical Biology) is embedded within the Utrecht Institute for Pharmaceutical Sciences (UIPS) and focuses on design, chemo- or biosynthesis of compounds with biological or (potential) medicinal applications and interaction with their receptors. Insights thus obtained could lead to new bio-active compounds, new approaches for the treatment of still incurable diseases and new approaches to unsatisfactory treatments. We are interested in answering questions related to understanding as well as influencing peptide-protein, carbohydrate-protein and protein-protein interactions that underlie e.g. infection, immunological and neurological disorders. Especially modified peptides and peptidomimetics as well as carbohydrates are synthesized and studied.

Our staff

Geert-Jan Boons

The research of prof. dr. Geert-Jan Boons focuses on the synthesis and biological functions of carbohydrates and glycoconjugates. This includes the development of efficient and novel glycosylation methods such as combinatorial and solid phase chemistry, the use of new approaches to control anomeric selectivity, the design of new protecting groups and the chemo-enzymatic synthesis of oligosaccharides. Some projects use synthetically modified saccharides to study the factors that are important for carbohydrate-protein complexation and it is hoped that these programs will lead to the rational design of saccharide mimetics that have improved affinities for particular proteins. Apart form synthesis, these projects require sophisticated structural and binding studies. Other programs deal with the preparation of oligosaccharides of biological importance and are often conducted in collaboration with pharmaceutical companies. The long-term objective of these projects is the development of novel carbohydrate-based drugs and vaccines.

Roland Pieters

The group of prof. dr. Roland Pieters aims to make molecules and constructs that can block or detect disease- causing processes with high affinity and specificity. In many cases these involve protein-carbohydrate interactions. A major theme in the work is the study of multivalent interactions. In many situations in nature where ligand binding is weak, simultaneous binding of larger linked (sub)ligands can greatly increase the binding strength to biologically relevant levels. Many aspects of multivalency are still unclear and should be uncovered and also as a design strategy for drug leads or biological tools multivalency has great potential. Dendrimers are used to make multivalent systems, but also nanoparticles and array surfaces are being explored.

Nathaniel Martin

The sub-group of dr. Nathaniel Martin has a number of ongoing research projects. His interests are broad and include investigating new (bio)chemical approaches to combatting infectious disease as well as developing new molecular tools with which to study cancer and epigenetic processes. Common to most of the projects is the application of synthetic organic chemistry in the development of biologically active compounds that are relevant to human disease. A specific focus area of our group’s research is in studying the N-methylation of arginine residues in various target proteins. This unique posttranslational modification is performed by a specific enzyme family known as the Protein Arginine N-Methyltransferases (PRMTs). A growing body of evidence now implicates dysregulated PRMT activity in a number of diseases including various forms of cancer. Dr. Martin develops PRMT inhibitors, which may hold potential as a means of developing new therapeutics. A second major theme in the Martin group is the development of new anti-infective agents. To this end we pursue strategies employing both small- and medium-sized molecules as a means of understanding (and potentially treating) infectious disease, both bacterial and viral.