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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 activity-independent functions of kinases and other enzymes.

SUBMITTER: Meyerowitz JG

PROVIDER: S-EPMC4904880 | biostudies-literature | 2015 Apr-Jun

REPOSITORIES: biostudies-literature

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A new "angle" on kinase inhibitor design: Prioritizing amphosteric activity above kinase inhibition.

Meyerowitz Justin G JG Weiss William A WA Gustafson W Clay WC

Molecular & cellular oncology 20150225 2

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 activity-independent functions of kinases and other enzymes. ...[more]

PMID: 27308435

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