Protease Directed Drug Discovery - A Platform Approach

Presentation: 3C01

Session: Target Biology & Screening: Kinases & Proteases

Bernd Gerhartz, Ulrich Hassiepen, Nils Ostermann, Benoit Pierrat and Joerg Trappe,
Novartis Institutes for Biomedical Research

Presenting Author: Joreg Trappe, Novartis - Switzerland

    Traditionally, progress in the development of protease inhibitors has been hampered to a large degree by their limited selectivity. Therefore, the ability to efficiently profile compounds against a large panel of protease assays is important to successfully discover new generation protease drugs. In order to efficiently profile compounds within and across the various assay panels, we have developed a semi-automated parallel screening technology which is linked to a high capacity data analysis tool.

    The compound profiling system as established in the Protease Platform is used to routinely determine the potency and specificity of inhibitors from multiple protease drug discovery projects, and is part of the integrated approach towards protease-directed drug discovery.


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