Sunesis Pharmaceuticals, Inc.

Andrew Braisted

Jim Wells

Dan Erlanson

John C Prescott

Robert S McDowell

Daniel A Erlanson

The invention concerns the identification of protein kinase inhibitors that preferentially bind to the inactive conformation of a target protein kinase. The inhibitors are identified by locking the target protein kinase in an inactive conformation, and using a covalent tethering approach to identify inhibitors preferentially targeting the inactive conformation.

Identification of kinase inhibitors

The present invention provides novel methods for ligand discovery. The inventive methods rely on a process termed 'tethering' where potential ligands are covalently bonded or 'tethered' to a target and subsequently identified.

Methods for ligand discovery

The invention concerns a method for rapid identification and characterization of binding partners for a target molecule, and for providing binding partners with improved binding affinity. More specifically, the invention concerns an improved tethering method for the rapid identification of at least two binding partners that bind near one another to a target molecule.

Extended tethering approach for rapid identification of ligands

The present invention is directed to novel methods for rapidly and unambiguously identifying small organic molecule ligands for binding to biological target molecules. Small organic molecule ligands identified according to the methods of the present invention may find use, for example, as novel therapeutic drug lead compounds, enzyme inhibitors, labeling compounds, diagnostic reagents, affinity reagents for protein purification, and the like. Also presented are novel methods for identifying high affinity binding ligands for a biological target molecule of interest, wherein those methods comprise linking two or more small organic molecule ligands previously identified as being capable of binding to the biological target molecule of interest. Biological target molecules include, for example, polypeptides, nucleic acids, carbohydrates, nucleoproteins, glycoproteins, glycolipids and lipoproteins.

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San Francisco, CA, United States of America

Andrew Braisted