Brandeis University

Dorothee Kern

Adelajda Zorba

The present invention features an antibody mimetic, or an antigen binding fragment thereof, that specifically binds to an allosteric site of Aurora A kinase, therapeutic compositions comprising this antibody mimetic, and the use of the monobody to modulate Aurora A kinase for the treatment of cancer.

Compositions and methods for modulating kinase activity

In one aspect, the present invention provides a method of selecting or identifying an agent that inhibits a target protein having an active site. In another aspect, the invention provides a method of selecting an agent that inhibits a target protein having an active site for further optimization. In some embodiments, the methods comprise measuring or predicting stability of an induced fit conformation of an agent contacted to an active site of the protein, wherein the agent is selected if the stability of the induced fit conformation of the agent contacted to the active site of the protein is increased relative to a reference stability.

Biophysical platform for drug development based on energy landscape

The present invention features therapeutic compositions comprising an agent that specifically binds to a PIF pocket of Aurora A kinase and an agent that specifically binds to an ATP-binding site of Aurora A kinase, and the use of the therapeutic compositions to modulate Aurora A kinase for the treatment of cancer.

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Waltham, MA, United States of America

Dorothee Kern