A new "angle" on kinase inhibitor design: Prioritizing amphosteric activity above kinase inhibition.
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.
Department of Cellular and Molecular Pharmacology; School of Medicine; Helen Diller Family Comprehensive Cancer Center.
Justin G
JG
Meyerowitz
Helen Diller Family Comprehensive Cancer Center; Departments of Neurology and Neurosurgery; University of California San Francisco; San Francisco, CA USA.
William A
WA
Weiss
Helen Diller Family Comprehensive Cancer Center; Department of Pediatrics; UCSF Benioff Children's Hospital.
W Clay
WC
Gustafson
AURKA; Aurora kinase A; MYC; MYCN; cancer; kinase inhibition