Send to

Choose Destination
See comment in PubMed Commons below
Cancer Res. 2007 Jan 15;67(2):573-9.

An antagonist of dishevelled protein-protein interaction suppresses beta-catenin-dependent tumor cell growth.

Author information

Department of Pharmaceutical Chemistry, Thoracic Oncology Labratory, University of California San Francisco, and Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, TN 38105, USA.

Erratum in

  • Cancer Res. 2007 Mar 1;67(5):2389.


Recent progress in the development of inhibitors of protein-protein interactions has opened the door for developing drugs that act by novel and selective mechanisms. Building on that work, we designed a small-molecule inhibitor of the Wnt signaling pathway, which is aberrantly activated across a wide range of human tumors. The compound, named FJ9, disrupts the interaction between the Frizzed-7 Wnt receptor and the PDZ domain of Dishevelled, down-regulating canonical Wnt signaling and suppressing tumor cell growth. The antitumorigenic effects of FJ9 were pronounced, including induction of apoptosis in human cancer cell lines and tumor growth inhibition in a mouse xenograft model. FJ9 is thus among the first non-peptide inhibitors to show therapeutic efficacy through disruption of PDZ protein-protein interactions.

[Indexed for MEDLINE]
Free full text
PubMed Commons home

PubMed Commons

How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for HighWire
    Loading ...
    Support Center