Beactica scientists reveal novel strategies for discovery of drugs targeting ion channels involved in synaptic signalling

Beactica, the Swedish fragment-based drug discovery company, today announced the publication of three key papers in leading scientific journals*. The papers describe important work towards the discovery of novel drugs targeting Cys-loop ion channel receptors, a significant family of drug targets involved in various neurological diseases, for example epilepsy.

Two of the publications outline the development of SPR biosensor-based assays suitable for screening and kinetic characterization of compounds interacting with Cys-loop ion channel receptors. In a third paper, the highly sensitive assays are shown to be suitable for fragment-based drug discovery. The high information content of the developed assays is expected to be powerful for the discovery of efficient inhibitors towards this class of drug targets.

Neural signalling involves activation of synaptic ion channels by released neurotransmitters. Scientific challenges in exploring ion channels as drug targets can be circumvented by using acetylcholine-binding protein, a surrogate protein from a fresh water mollusc which mimics the extracellular domain of Cys-loop receptors.

The research was performed in collaboration between Beactica and scientists at the Vrije Universiteit Amsterdam, the Netherlands, and Uppsala University, Sweden. It is part of NeuroCypres, a project funded through EU’s 7th Framework Programme. For more information, please visit www.neurocypres.eu.
For additional information please contact Dr Per Källblad, Beactica CEO, +46 18 560880.

Publication references

• 
Retra et al., Development of SPR biosensor assays for primary and secondary screening of AChBP ligands,Analytical Biochemistry, 2010, 407:58–64 (DOI:10.1016/j.ab.2010.06.021).
• Geitmann et al., Interaction kinetic and structural dynamic analysis of ligand binding to acetylcholine-binding protein, Biochemistry, 2010, 49:8143–8154. DOI: 10.1021/bi1006354).
• de Kloe et al., Surface plasmon resonance biosensor-based fragment screening using acetylcholine binding protein identifies ligand efficiency hot spots (LE hot spots) by deconstruction of nicotinic acetylcholine receptor α7 ligands, Journal of Medicinal Chemistry, 2010, 53:7192–7201 (DOI: 10.1021/jm100834y).

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