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Review
. 2012 Jun 13;31(12):2737-46.
doi: 10.1038/emboj.2012.126. Epub 2012 May 22.

Drugging Wnt signalling in cancer

Paul Polakis  1
Affiliations
Review

Drugging Wnt signalling in cancer

Paul Polakis. EMBO J. .

Erratum in

  • EMBO J. 2012 Aug;31(15):3375

Abstract

Aberrant regulation of the Wnt signalling pathway has emerged as a prevalent theme in cancer biology. This chapter summarizes the research that provides a proof of concept for inhibiting Wnt signalling in cancer, the potential means by which this could be achieved, and some recent advances towards this goal. A brief discussion of molecular diagnostics and possible safety concerns is also provided.

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Conflict of interest statement

The author declares that he has no conflict of interest.

Figures

Figure 1
Figure 1
Therapeutic intervention in Wnt signalling. Components of Wnt signalling at the plasma membrane (PM), in the cytoplasm and nucleus are represented with the locus of intervention for some of the inhibitors (red text) described in this chapter.
Figure 2
Figure 2
Overlapping regions of interaction for β-catenin-binding proteins. The 12 armadillo repeats in β-catenin are depicted in orange and the generalized areas of interaction for various proteins that bind to them are shown. APC R3 is the third 20-amino-acid repeat unit in the APC protein and pR3 is the phosphorylated form. RA is the first 15-amino-acid repeat unit in APC.
Figure 3
Figure 3
Relative levels of Axin II mRNA in cancer cell lines. Levels of AxinII mRNA in 287 cancer cells of various origins were measured by microarray analysis on the Affymetrix U133P platform (unpublished data). Each vertical bar (signal intensity/average difference) represents a measurement from an individual cell line from the indicated class, although specific identification is provided for only a portion of the cell lines. Axin II levels are particularly high in cell lines derived from colorectal cancers (CRC) relative to those from NSCLC, pancreatic cancer (PanCa), breast cancer (BrCa), small-cell lung cancer (SCLC), ovarian cancer (OvCa), melanoma (Mel), prostate cancer (PrCa) and glioblastoma (GB). The cell line and mutation is noted for some cell lines not in the colorectal category that exhibit high-level Axin II mRNA expression. Three colorectal cell lines, KM12, colo741 and RKO, known to be wt for Wnt signalling components, express low levels of Axin II mRNA.
See this image and copyright information in PMC

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