The Division of Medicinal Chemistry is focusing on structure-based drug design, and in particular on Fragment-Based Lead Discovery (FBLD).
Fragment-based approaches are ideal for academic and small bio-tech drug discovery efforts, as these technologies are design intensive. The division has established a fragment library containing 1500 low molecular weight compounds. Currently, this library is effectively used to develop ligands against a variety of targets: GPCRs, kinases, ligand-gated ion channels, protein-protein interactions, etc.
The medicinal chemistry group will move to a brand new building in the heart of the VU University campus. These new premises, called the O|2 lab building, will offer the life sciences research groups of the university state-of-the-art facilities. The Institute supports state-of-the art core facilities, which facilitate the performance of cutting edge (bio)chemical research with both basic and translational scientific value. The academic group has access to industry standard as well as proprietary molecular modelling software, biochemical and biophysical screening technologies and ample organic synthesis facilities.
Website link: VU University
Staff involved in this project:
Prof. Iwan de Esch (Fragnet Coordinator) - did his PhD research at the Department of Pharmacochemistry, VU University Amsterdam, The Netherlands. In 1998, he became research associate at the Drug Design Group of the University of Cambridge. Dr de Esch is a co-founder of De Novo Pharmaceuticals (2000) where he worked as a group and project leader. Dr de Esch returned to academia in 2003 and is now professor at the Medicinal Chemistry Department. The group focuses on two research lines, namely G-protein-coupled receptors (GPCRs) and fragment-based lead discovery (FBLD). Iwan is interested in applying FBDD approaches for lead discovery on a wide variety of targets (including GPCRs, kinases, PDEs and PPIs) and to use fragment-based approaches to study the ligand-protein binding event (in terms of affinity, thermodynamics and kinetics). Dr. de Esch is co-founder of IOTA Pharmaceuticals Ltd (2007) and Griffin Discoveries BV (2009). In 2011, he was awarded the Galenus Research Price for his work on FBLD.
Dr. Jacqueline van Muijlwijk– assistant professor in Medicinal Chemistry research group and educational director Dr Jacqueline van Muijlwijk did her PhD research in a joint project between the Department of Pharmacochemistry, VU University Amsterdam, The Netherlands, with Leiden University, the Netherlands. Her interest is the combination of medicinal chemistry research and innovation of science education. She got experience in teaching at all levels and in several disciplines: high school, higher education (applied sciences) , undergraduates and graduates. In 2006 she was the coordinator of a consortium of >30 high schools, 2 schools for applied sciences and 2 universities in Amsterdam in the field of natural sciences. Dr. van Muijlwijk was co-founder of (member of the MT of the department of Chemistry and Pharmaceutical sciences) and involved in the development of the bachelor programme Science Business and Innovation (SBI). In 2010 she became managing director of the Amsterdam Institute for Molecules, Medicines and Systems. From 2013 she is educational director of bachelor and master programmes in Pharmaceutical Sciences.
Iina Hellsten, Associate Professor in Social Sciences with expertise in communication networks, science and technology studies (STS) and scientometrics.
Dr. Chris de Graaf – assistant professor Computational Medicinal Chemistry with 12 years experience in computational chemistry, chemoinformatics, and computer-aided drug discovery and design.
Dr. Maikel Wijtmans – assistant professor Drug Synthesis with 14 years experience in synthetic organic chemistry, awarded the best academic chemistry teacher in The Netherlands (2013-2016).
Prof. Martine Smit - full professor of Target & Systems Biology and 22 years experience in biochemistry and molecular pharmacology Prof. Rob Leurs - full professor Medicinal Chemistry, 24 years experience in research on medicinal chemistry and industrial applications and is co-founder of Griffin Discoveries.
Prof. Peter van der Sijde - full professor Science, Business & Innovation, has a background in social sciences. He does research and teaching that is focused on entrepreneurship and technology transfer.