Format

Send to

Choose Destination
See comment in PubMed Commons below
Nat Med. 2004 Mar;10(3):262-7. Epub 2004 Feb 22.

VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo.

Author information

1
Vertex Pharmaceuticals (Europe) Limited, 88 Milton Park, Abingdon, Oxfordshire, OX14 4RY, UK.

Erratum in

  • Nat Med. 2007 Apr;13(4):511.

Abstract

The Aurora kinases are essential for the regulation of chromosome segregation and cytokinesis during mitosis. Aberrant expression and activity of these kinases occur in a wide range of human tumors, and lead to aneuploidy and tumorigenesis. Here we report the discovery of a highly potent and selective small-molecule inhibitor of Aurora kinases, VX-680, that blocks cell-cycle progression and induces apoptosis in a diverse range of human tumor types. This compound causes profound inhibition of tumor growth in a variety of in vivo xenograft models, leading to regression of leukemia, colon and pancreatic tumors at well-tolerated doses. Our data indicate that Aurora kinase inhibition provides a new approach for the treatment of multiple human malignancies.

PMID:
14981513
DOI:
10.1038/nm1003
[Indexed for MEDLINE]
Free full text
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Nature Publishing Group
    Loading ...
    Support Center