Projektnummer

0050563

Zusammenfassung

It is proposed to target the TPX2 recognition site of the kinase for the development of small-molecule inhibitors that would bind Aurora-A and impair the conformational change required for its full activation. For this purpose, it is planned to synthesise a library of about 300 chemical compounds. The design of the library is based on structural information, and the compounds are intended to mimic TPX2. Particular chemical moieties will be included to prevent activation by stabilizing the inactive conformation. A high-throughput assay for TPX2 - Aurora-A interaction based on fluorescen...