Chimerizing protein kinases for drug discovery

摘要

The present invention relates to chimeric protein kinase molecules and methods for designing inhibitors of protein kinases using the chimeric protein kinases of the present invention. The chimeric protein kinase of the present invention comprise inhibitor binding site residues of a non-crystallizable protein and non-inhibitor binding site residues of a crystallizable protein. The chimeric protein is preferably crystallizable and is useful for designing inhibitors for the non-crystallizable protein. In addition, the present invention is directed to a protein kinase inhibitor binding site which is outside the ATP binding site of the protein kinase and methods of use therefore.