Biophysical Screening and Characterization

National facility

The facility provides in depth information on interactions. The data can range from simple qualitative analyses demonstrating that two molecules interact, to quantitative analyses that provide mechanistic, kinetic, thermodynamic, chemodynamic information as well as molecular details of complexes. The facility primarily aids projects in the Drug Discovery and Development Platform, but can also provide services to academic and external researchers.

SERVICES

  • Kinetic characterization of hit or lead compounds with the surface plasmon resonance (SPR) technology (Biacore).
  • KD values of biomolecular interactions in solution using the method microscale thermophoresis (MST).
  • Affinity ranking of compounds with SPR or MST.
  • Protein crystallization, structure determination by X-ray crystallography and structure analysis.
  • X-ray crystallography for visualizing the interactions between a protein and a ligand for in silico optimization of hit or lead compounds.
  • Fragment based drug discovery - screening with SPR and crystallizing target protein with hit molecules for structure based fragment growth.

 

To summarize, we can provide information for drug discovery and development projects relating to:

  • Validation of target functionality and reference ligands
  • How to prove target engagement
  • Definition of suitable kinetic profile of leads
  • Resolving mode-of-action and complex interaction mechanisms

EQUIPMENT

  • Biacore T200.
  • Instruments for high-throughput crystallization such as a Mosquito® Crystal liquid handler, a Scorpion liquid handler and a Rigaku plate hotel.
  • Monolith NT. Automated (MST instrument from Nanotemper). Lable free and fluorescent red-blue detectors.