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PMID: 20941789 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't

Loss of WNT-TCF addiction and enhancement of HH-GLI1 signalling define the metastatic transition of human colon carcinomas.

EMBO molecular medicine ·Vol. 2 ·No. 11 ·2010-11-00 ·Pages 440-57

Varnat F, Siegl-Cachedenier I, Malerba M, Gervaz P, Ruiz i Altaba A

Abstract

Previous studies demonstrate the initiation of colon cancers through deregulation of WNT-TCF signalling. An accepted but untested extension of this finding is that incurable metastatic colon carcinomas (CCs) universally remain WNT-TCF-dependent, prompting the search for WNT-TCF inhibitors. CCs and their stem cells also require Hedgehog (HH)-GLI1 activity, but how these pathways interact is unclear. Here we define coincident high-to-low WNT-TCF and low-to-high HH-GLI transitions in patient CCs, most strikingly in their CD133(+) stem cells, that mark the development of metastases. We find that enhanced HH-GLI mimics this transition, driving also an embryonic stem (ES)-like stemness signature and that GLI1 can be regulated by multiple CC oncogenes. The data support a model in which the metastatic transition involves the acquisition or enhancement of a more primitive ES-like phenotype, and the downregulation of the early WNT-TCF programme, driven by oncogene-regulated high GLI1 activity. Consistently, TCF blockade does not generally inhibit tumour growth; instead, it, like enhanced HH-GLI, promotes metastatic growth in vivo. Treatments for metastatic disease should therefore block HH-GLI1 but not WNT-TCF activities.

MeSH Terms
AC133 Antigen Antigens, CD/analysis Carcinoma/pathology,physiopathology Colonic Neoplasms/pathology,physiopathology Gene Expression Profiling Glycoproteins/analysis Hedgehog Proteins/metabolism Humans Neoplasm Metastasis/pathology,physiopathology Peptides/analysis Stem Cells TCF Transcription Factors/metabolism Transcription Factors/metabolism Wnt Proteins/metabolism Zinc Finger Protein GLI1
Chemicals
AC133 Antigen Antigens, CD GLI1 protein, human Glycoproteins Hedgehog Proteins PROM1 protein, human Peptides TCF Transcription Factors Transcription Factors Wnt Proteins Zinc Finger Protein GLI1
Authors & Affiliations
5 authors, click to expand affiliations / ORCID
Varnat Frédéric
Faculty of Medicine, Department of Genetic Medicine and Development, University of Geneva, Geneva, Switzerland.
Siegl-Cachedenier Irene
Malerba Monica
Gervaz Pascal
Ruiz i Altaba Ariel
References (54)
54 references, click to expand
  1. Wnt/beta-catenin signaling: components, mechanisms, and diseases.
    Dev Cell. 2009 Jul;17(1):9-26 PMID: 19619488
  2. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling.
    Nature. 2009 Oct 1;461(7264):614-20 PMID: 19759537
  3. Myc deletion rescues Apc deficiency in the small intestine.
    Nature. 2007 Apr 5;446(7136):676-9 PMID: 17377531
  4. Prominin 1 marks intestinal stem cells that are susceptible to neoplastic transformation.
    Nature. 2009 Jan 29;457(7229):603-7 PMID: 19092805
  5. Reduction of beta-catenin/T-cell transcription factor signaling by aspirin and indomethacin is caused by an increased stabilization of phosphorylated beta-catenin.
    Mol Cancer Ther. 2003 Jun;2(6):509-16 PMID: 12813129
  6. The EWS/FLI1 oncogenic transcription factor deregulates GLI1.
    Oncogene. 2008 May 22;27(23):3282-91 PMID: 18084326
  7. A subpopulation of CD26+ cancer stem cells with metastatic capacity in human colorectal cancer.
    Cell Stem Cell. 2010 Jun 4;6(6):603-15 PMID: 20569697
  8. Genetic alterations during colorectal-tumor development.
    N Engl J Med. 1988 Sep 1;319(9):525-32 PMID: 2841597
  9. Identification of stem cells in small intestine and colon by marker gene Lgr5.
    Nature. 2007 Oct 25;449(7165):1003-7 PMID: 17934449
  10. The Intestinal Wnt/TCF Signature.
    Gastroenterology. 2007 Feb;132(2):628-32 PMID: 17320548
  11. Induced pluripotent stem cell lines derived from human somatic cells.
    Science. 2007 Dec 21;318(5858):1917-20 PMID: 18029452
  12. APC and oncogenic KRAS are synergistic in enhancing Wnt signaling in intestinal tumor formation and progression.
    Gastroenterology. 2006 Oct;131(4):1096-109 PMID: 17030180
  13. Down-regulation of beta-catenin by activated p53.
    Mol Cell Biol. 2001 Oct;21(20):6768-81 PMID: 11564862
  14. Small-molecule antagonists of the oncogenic Tcf/beta-catenin protein complex.
    Cancer Cell. 2004 Jan;5(1):91-102 PMID: 14749129
  15. Expression of the PTCH1 tumor suppressor gene is regulated by alternative promoters and a single functional Gli-binding site.
    Gene. 2004 Apr 14;330:101-14 PMID: 15087129
  16. Gli and hedgehog in cancer: tumours, embryos and stem cells.
    Nat Rev Cancer. 2002 May;2(5):361-72 PMID: 12044012
  17. Induction of pluripotent stem cells from mouse embryonic and adult fibroblast cultures by defined factors.
    Cell. 2006 Aug 25;126(4):663-76 PMID: 16904174
  18. Wnt signalling: variety at the core.
    J Cell Sci. 2007 Feb 1;120(Pt 3):385-93 PMID: 17251379
  19. NANOG regulates glioma stem cells and is essential in vivo acting in a cross-functional network with GLI1 and p53.
    EMBO J. 2010 Aug 4;29(15):2659-74 PMID: 20581802
  20. Gli proteins encode context-dependent positive and negative functions: implications for development and disease.
    Development. 1999 Jun;126(14):3205-16 PMID: 10375510
  21. HEDGEHOG-GLI1 signaling regulates human glioma growth, cancer stem cell self-renewal, and tumorigenicity.
    Curr Biol. 2007 Jan 23;17(2):165-72 PMID: 17196391
  22. DKK1, a negative regulator of Wnt signaling, is a target of the beta-catenin/TCF pathway.
    Oncogene. 2004 Nov 4;23(52):8520-6 PMID: 15378020
  23. Reduced level of smoothened suppresses intestinal tumorigenesis by down-regulation of Wnt signaling.
    Gastroenterology. 2009 Aug;137(2):629-38 PMID: 19427313
  24. Core transcriptional regulatory circuitry in human embryonic stem cells.
    Cell. 2005 Sep 23;122(6):947-56 PMID: 16153702
  25. Serial analysis of chromatin occupancy identifies beta-catenin target genes in colorectal carcinoma cells.
    Proc Natl Acad Sci U S A. 2007 Feb 27;104(9):3324-9 PMID: 17360646
  26. Cancer statistics, 2009.
    CA Cancer J Clin. 2009 Jul-Aug;59(4):225-49 PMID: 19474385
  27. Identification and expansion of human colon-cancer-initiating cells.
    Nature. 2007 Jan 4;445(7123):111-5 PMID: 17122771
  28. Nitric oxide-donating aspirin inhibits beta-catenin/T cell factor (TCF) signaling in SW480 colon cancer cells by disrupting the nuclear beta-catenin-TCF association.
    Proc Natl Acad Sci U S A. 2003 Oct 28;100(22):12584-9 PMID: 14566053
  29. The beta-catenin/TCF-4 complex imposes a crypt progenitor phenotype on colorectal cancer cells.
    Cell. 2002 Oct 18;111(2):241-50 PMID: 12408868
  30. Genetic elimination of Suppressor of fused reveals an essential repressor function in the mammalian Hedgehog signaling pathway.
    Dev Cell. 2006 Feb;10(2):187-97 PMID: 16459298
  31. SOX2 silencing in glioblastoma tumor-initiating cells causes stop of proliferation and loss of tumorigenicity.
    Stem Cells. 2009 Jan;27(1):40-8 PMID: 18948646
  32. Wnt canonical pathway restricts graded Shh/Gli patterning activity through the regulation of Gli3 expression.
    Development. 2008 Jan;135(2):237-47 PMID: 18057099
  33. A GLI1-p53 inhibitory loop controls neural stem cell and tumour cell numbers.
    EMBO J. 2009 Mar 18;28(6):663-76 PMID: 19214186
  34. Wnt activity defines colon cancer stem cells and is regulated by the microenvironment.
    Nat Cell Biol. 2010 May;12(5):468-76 PMID: 20418870
  35. Aberrant activation of hedgehog signaling pathway contributes to endometrial carcinogenesis through beta-catenin.
    Mod Pathol. 2009 Jun;22(6):839-47 PMID: 19329935
  36. Suppression of beta-catenin inhibits the neoplastic growth of APC-mutant colon cancer cells.
    Cancer Res. 2001 Sep 1;61(17):6563-8 PMID: 11522655
  37. Hedgehog pathway activity is required for the lethality and intestinal phenotypes of mice with hyperactive Wnt signaling.
    Mech Dev. 2010 Jan-Feb;127(1-2):73-81 PMID: 19861162
  38. Activation of AXIN2 expression by beta-catenin-T cell factor. A feedback repressor pathway regulating Wnt signaling.
    J Biol Chem. 2002 Jun 14;277(24):21657-65 PMID: 11940574
  39. An embryonic stem cell-like gene expression signature in poorly differentiated aggressive human tumors.
    Nat Genet. 2008 May;40(5):499-507 PMID: 18443585
  40. Epigenetic inactivation of SFRP genes allows constitutive WNT signaling in colorectal cancer.
    Nat Genet. 2004 Apr;36(4):417-22 PMID: 15034581
  41. Enhancement of GLI1-transcriptional activity by beta-catenin in human cancer cells.
    Oncol Rep. 2006 Jul;16(1):91-6 PMID: 16786128
  42. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer.
    Nat Chem Biol. 2009 Feb;5(2):100-7 PMID: 19125156
  43. The Wnt antagonist DICKKOPF-1 gene is a downstream target of beta-catenin/TCF and is downregulated in human colon cancer.
    Oncogene. 2005 Feb 3;24(6):1098-103 PMID: 15592505
  44. Gli1, downregulated in colorectal cancers, inhibits proliferation of colon cancer cells involving Wnt signalling activation.
    Gut. 2006 Jul;55(7):991-9 PMID: 16299030
  45. The Gli code: an information nexus regulating cell fate, stemness and cancer.
    Trends Cell Biol. 2007 Sep;17(9):438-47 PMID: 17845852
  46. A human colon cancer cell capable of initiating tumour growth in immunodeficient mice.
    Nature. 2007 Jan 4;445(7123):106-10 PMID: 17122772
  47. Context-dependent regulation of the GLI code in cancer by HEDGEHOG and non-HEDGEHOG signals.
    J Mol Cell Biol. 2010 Apr;2(2):84-95 PMID: 20083481
  48. DYRK1B-dependent autocrine-to-paracrine shift of Hedgehog signaling by mutant RAS.
    Nat Struct Mol Biol. 2010 Jun;17(6):718-25 PMID: 20512148
  49. Melanomas require HEDGEHOG-GLI signaling regulated by interactions between GLI1 and the RAS-MEK/AKT pathways.
    Proc Natl Acad Sci U S A. 2007 Apr 3;104(14):5895-900 PMID: 17392427
  50. Mining the Wnt pathway for cancer therapeutics.
    Nat Rev Drug Discov. 2006 Dec;5(12):997-1014 PMID: 17139285
  51. Human colon cancer epithelial cells harbour active HEDGEHOG-GLI signalling that is essential for tumour growth, recurrence, metastasis and stem cell survival and expansion.
    EMBO Mol Med. 2009 Sep;1(6-7):338-51 PMID: 20049737
  52. Inhibitory Gli3 activity negatively regulates Wnt/beta-catenin signaling.
    Curr Biol. 2007 Mar 20;17(6):545-50 PMID: 17331723
  53. Omomyc, a potential Myc dominant negative, enhances Myc-induced apoptosis.
    Cancer Res. 2002 Jun 15;62(12):3507-10 PMID: 12067996
  54. Chemotherapy, bevacizumab, and cetuximab in metastatic colorectal cancer.
    N Engl J Med. 2009 Feb 5;360(6):563-72 PMID: 19196673
Article Info
Journal
EMBO molecular medicine
Abbr.
EMBO Mol Med
ISSN
1757-4684
Published
2010-11-00
Pages
440-57
Language
English
Region
England
NLM ID
101487380
PMCID
PMC3394505
Subset
IM
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