Platform Success Examples

Novel Allosteric Modulators of a7 nACh Receptor

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

Beactica's platform enabled the identification of multiple physiologically active novel small molecule modulators acting on previously unexplored allosteric binding sites of the receptor.

More information is available here.
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Novel Allosteric Hits for USP7

Almac Discovery wanted to identify novel and selective inhibitors for a number of ubiquitin-specific proteases – including USP7 – with the ultimate aim to develop novel cancer therapeutics for patients in need.

Beactica's platform enabled the generation of ”perhaps the most potent small-molecule inhibitor of USP7 to date” which also had extremely high selectivity against other USPs and target classes.

More information is available here.
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Novel Scaffold for Allosteric Inhibition of HIV-RT

Beactica wanted to identify novel inhibitors of wild type and drug-resistant variants of HIV-1 RT, with the ultimate aim to develop novel HIV therapeutics for patients in need.

Beactica's platform enabled the identification allosteric scaffolds with defined modes of action and desired resistance profiles against key mutant forms of HIV-1 RT.

More information is available here.


Insulin Interacting with its Full-Length Receptor

Sanofi wanted to measure the interaction kinetics between insulin and its two binding sites on the full-length insulin receptor, with the ultimate aim to optimize the clinical efficacy of novel insulin analogues.

Results from the collaboration contributed towards the regulatory approval of Insulin lispro Sanofi®, a rapid-acting insulin biosimilar introduced on the market by Sanofi.

More information is available here.
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Mechanistic investigation of Afatinib

Boehringer Ingelheim wanted an in-depth understanding of the interaction mechanism of Afatinib (inhibitor of EGFR, HER2, and ErbB4).

The results were a mechanistic rationale for the distinct pharmacological features of Afatinib and thereby an explanation of the clinical activity seen in some patients resistant to antibody or kinase inhibitor therapy.

More information is available here.

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