Allosteric activators and inhibitors of proteinkinases of the AGC- and the Aurora-family
Another new approach to influence protein kinases which is also part of this invention is the allosteric regulation of such enzymes.
A hydrophobe binding site on the surface of some protein kinases of the AGC-family was identified by analyzing their crystal structure. The invention includes some new classes of small molecule compounds which bind to and by allosteric effect influence the acitivity of protein kinases. The inventors were able to inhibit the kinase activity as well as to cause an activation of the kinase. Both were examined with several different protein kinase assays.
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