HTS to Identify Inhibitors of c-Abl kinase for the Potential Treatment of Epilepsy and Neurodegenerative diseases

National Center For Advancing Translational Sciences

Investigators

Linked publications, trials & patents

Abstract

During this period, the project team completed the structure activity relationship studies producing a highly potent selective cAbl allosteric inhibitor (Neurotinib) with good pharmacokinetics and preferential distribution toward CNS. Evaluation of this inhibitor in several mouse models of Alzheimer's disease results in good efficacy, with recovery of cognitive impairments and reduction of plaque and inflammatory markers. In addition, the team has evaluated Neurotinib in Niemann Pick A mouse model with good efficacy results. The team also demonstrated the therapeutic value of this molecule for the treatment of epilepsy and has encouraging results in several models of Parkinson disease, which we will publish soon.