Presentation: P02015

SPR imaging combined with chemical microarrays can detect low affinity interactions of proteins with surface-immobilized fragment or lead-like compounds in a miniaturized and high throughput fashion. It allows the direct analysis of binding events without the need of reporter systems or tags and is therefore suited for function blind screening. Additionally, on-array competition studies with known ligands can be used to map the target´s binding site.

The analysis of weak interactions using SPR Imaging is particularly important for fragment screening, which offers a conceptually new drug discovery approach. Instead of trying to identify relevant features in a rather complex hit compound it aims at a stepwise discovery starting from small molecular fragments.

The presentation will discuss Graffinity´s SPR Imaging Technology for screening protein-ligand interactions on chemical microarrays. A case study describing the identification of selective phosphodiesterase (PDE) inhibitors will be presented.

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