A new “angle” on kinase inhibitor design: Prioritizing amphosteric activity above kinase inhibition

Abstract

The MYCN oncoprotein has remained an elusive target for decades. We recently reported a new class of kinase inhibitors designed to disrupt the conformation of Aurora kinase A enough to block its kinase-independent interaction with MYCN, resulting in potent degradation of MYCN. These studies provide proof-of-principle for a new method of targeting enzyme… (More)
DOI: 10.4161/23723556.2014.975641

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