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Cancer Cell. 2010 Sep 14;18(3):258-67. doi: 10.1016/j.ccr.2010.08.008.

Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein.

Author information

  • 1Department of Immunology and Microbial Science, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.

Erratum in

  • Cancer Cell. 2010 Oct 19;18(4):396.

Abstract

BMK1 is activated by mitogens and oncogenic signals and, thus, is strongly implicated in tumorigenesis. We found that BMK1 interacted with promyelocytic leukemia protein (PML), and inhibited its tumor-suppressor function through phosphorylation. Furthermore, activated BMK1 notably inhibited PML-dependent activation of p21. To further investigate the BMK-mediated inhibition of the tumor suppressor activity of PML in tumor cells, we developed a small-molecule inhibitor of the kinase activity of BMK1, XMD8-92. Inhibition of BMK1 by XMD8-92 blocked tumor cell proliferation in vitro and significantly inhibited tumor growth in vivo by 95%, demonstrating the efficacy and tolerability of BMK1-targeted cancer treatment in animals.

Copyright © 2010 Elsevier Inc. All rights reserved.

PMID:
20832753
[PubMed - indexed for MEDLINE]
PMCID:
PMC2939729
Free PMC Article

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