Crystallographic facility for target-based drug design

Rational discovery of new medicines, be it traditional smallmolecule drugs or biologics such as antibodies, is a major field of paramount importance. University-based research in Flanders plays a key role here, being able to explore novel directions, high-risk opportunities and clinically unmet needs. The rational approach requires the knowledge of the three-dimensional structure of the given drug target (usually a protein). In addition, specific interactions between the target and the drug being developed must be validated in atomic detail. To this end, X-ray crystallography is indisputably the most prolific technique. Here we propose to set up a new facility at KU Leuven centered on high-throughput crystallographic studies. The facility will cater to the drug discovery efforts of 9 laboratories acting as co-proposers as well as other KU Leuven researchers, external collaborators and third parties. Our proposal is to incorporate the existing crystallization robotics and the X-ray source but add two state-of-the-art crystallization imaging systems with ultraviolet capacity as well as the latest generation X-ray detector. The new equipment should boost the progression from first designs to highly active drug molecules. This facility, together with the major accumulated know-how in structural biology, medicinal chemistry and in silico drug design, is aimed to become a cornerstone of future drug discoveries, securing the world-leading position of KU Leuven.