Platform Success Example I – Novel Allosteric Modulators of a7 nACh Receptor

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Business Need

Janssen wanted to identify novel modulators of the a7 nicotinic acetylcholine receptor, with the ultimate aim to develop novel CNS therapeutics for patients in need.

Technical Challenge

The identification of novel small molecules that modulate the activity of their target protein through allosteric binding sites is a known significant challenge

Solution

Beactica’s team of highly skilled scientists applied the Company’s SPR biosensor-based discovery platform with an experimental approach designed to identify allosteric modulators

Results

Multiple novel small molecule modulators acting on previously unexplored allosteric binding sites were identified and confirmed to be physiologically active

Janssen - a7 nAChR - Fig1

The therapeutic programme was reprioritized by Janssen and the collaborative work was published in PNAS in May 2015

Janssen - a7 nAChR - Fig2

Reference

Spurny R, Debaveye S, Farinha A, Veys K, Vos A.M, Gossas T, Atack J, Bertrand S, Danielson UH, Tresadern G, Ulens C. (2015) Molecular blueprint of allosteric binding sites in a homologue of the agonist-binding domain of the α7 nicotinic acetylcholine receptor, PNAS, 112:E2543–52.