Erratum: Mining the Wnt pathway for cancer therapeutics (Nature Reviews Drug Discovery (2006) vol. 5 (997-1014) 10.1038/nrd2154);Mining the Wnt pathway for cancer therapeutics

Nature Reviews Drug Discovery

Volumn 5, Issue 12, 2006, Pages 997-1014

  Barker, Nick ^a   Clevers, Hans ^a  

^a HUBRECHT INSTITUTE   (Netherlands)

Author keywords

[No Author keywords available]

Indexed keywords

5 (1 AZIRIDINYL) 2,4 DINITROBENZAMIDE; ACETYLSALICYLIC ACID; ANTINEOPLASTIC AGENT; AVI 4126; BETA CATENIN; CELECOXIB; CPG 049090; CYCLOOXYGENASE 2 INHIBITOR; EVEROLIMUS; FLUOROURACIL; ICG 001; INDOMETACIN; NITRIC OXIDE DONOR; NONSTEROID ANTIINFLAMMATORY AGENT; NSC 668036; PKF 115 584; PKF 118 310; PKF 222 815; PNU 74654; PREVATAC; PROTEIN ANTIBODY; RETINOID DERIVATIVE; RETINOL; ROFECOXIB; SEOCALCITOL; SULINDAC; SULINDAC SULFONE; T CELL FACTOR PROTEIN; UNINDEXED DRUG; VITAMIN D; WNT PROTEIN; ZTM 000990;

ANTINEOPLASTIC ACTIVITY; CANCER CELL CULTURE; CANCER PATIENT; CANCER THERAPY; CARCINOGENESIS; CARDIOVASCULAR DISEASE; COLON CANCER; DIGESTIVE SYSTEM CANCER; DRUG MEGADOSE; DRUG STRUCTURE; FEVER; GROWTH INHIBITION; HEPATOBLASTOMA; HUMAN; INFLAMMATION; INTESTINAL BLEEDING; KIDNEY INJURY; LIVER CANCER; LIVER CELL CARCINOMA; MELANOMA; NEPHROBLASTOMA; NONHUMAN; OVARY CANCER; PAIN; PILOMATRIXOMA; POLYP; PRIORITY JOURNAL; PROSTATE CANCER; PROTEIN TARGETING; REVIEW; SIGNAL TRANSDUCTION; UNSPECIFIED SIDE EFFECT; VIRAL GENE DELIVERY SYSTEM;

EID: 33751530490     PISSN: 14741776     EISSN: 14741784     Source Type: Journal    
DOI: 10.1038/nrd2279     Document Type: Erratum

References (200)

1. Tetsu, O. & McCormick, F. β-catenin regulates expression of cyclin D1 in colon carcinoma cells. Nature 398, 422-426 (1999).
2. van de Wetering, M. et al. The β-catenin/TCF-4 complex imposes a crypt progenitor phenotype on colorectal cancer cells. Cell 111, 241-250 (2002).
3. Van der Flier, L. et al. The intestinal Wnt signature. Gastroenterology (in the press).
4. Logan, C. Y. & Nusse, R. The Wnt signaling pathway in development and disease. Annu. Rev. Cell Dev. Biol. 20, 781-810 (2004).
5. Kinzler, K. W. et al. Identification of FAP locus genes from chromosome 5q21. Science 253, 661-665 (1991).
6. Nishisho, I. et al. Mutations of chromosome 5q21 genes in FAP and colorectal cancer patients. Science 253, 665-669 (1991).
7. -/- colon carcinoma. Science 275, 1784-1787 (1997).
8. Morin, P. J. et al. Activation of β-catenin-Tcf signaling in colon cancer by mutations in β-catenin or APC. Science 275, 1787-1790 (1997).
9. Moser, A. R., Pitot, H. C. & Dove, W. F. A dominant mutation that predisposes to multiple intestinal neoplasia in the mouse. Science 247, 322-324 (1990).
10. Su, L. K. et al. Multiple intestinal neoplasia caused by a mutation in the murine homolog of the APC gene. Science 256, 668-670 (1992).
11. Miyaki, M. et al. Characteristics of somatic mutation of the adenomatous polyposis coli gene in colorectal tumors. Cancer Res. 54, 3011-3020 (1994).
12. Miyoshi, Y. et al. Somatic mutations of the APC gene in colorectal tumors: Mutation cluster region in the APC gene. Hum. Mol. Genet. 1, 229-233 (1992).
13. Powell, S. M. et al. APC mutations occur early during colorectal tumorigenesis. Nature 359, 235-237 (1992).
14. Polakis, P. Wnt signaling and cancer. Genes Dev. 14, 1837-1851 (2000).
15. Lammi, L. et al. Mutations in AXIN2 cause familial tooth agenesis and predispose to colorectal cancer. Am. J. Hum. Genet. 74, 1043-1050 (2004).
16. Liu, W. et al. Mutations in AXIN2 cause colorectal cancer with defective mismatch repair by activating β-catenin/TCF signalling. Nature Genet. 26, 146-147 (2000).
17. Caldwell, G. M. et al. The Wnt antagonist sFRP1 in colorectal tumorigenesis. Cancer Res. 64, 883-888 (2004).
18. Suzuki, H. et al. Epigenetic inactivation of SFRP genes allows constitutive WNT signaling in colorectal cancer. Nature Genet. 36, 417-422 (2004).
19. He, B. et al. Blockade of Wnt-1 signaling induces apoptosis in human colorectal cancer cells containing downstream mutations. Oncogene 24, 3054-3058 (2005).
20. Chan, T. A., Wang, Z., Dang, L. H., Vogelstein, B. & Kinzler, K. W. Targeted inactivation of CTNNB1 reveals unexpected effects of β-catenin mutation. Proc. Natl Acad. Sci. USA 99, 8265-8270 (2002).
21. Dahmen, R. P. et al. Deletions of AXIN1, a component of the WNT/wingless pathway, in sporadic medulloblastomas. Cancer Res. 61, 7039-7043 (2001).
22. Satoh, S. et al. AXIN1 mutations in hepatocellular carcinomas, and growth suppression in cancer cells by virus-mediated transfer of AXIN1. Nature Genet. 24, 245-250 (2000).
23. Fukui, T. et al. Transcriptional silencing of secreted frizzled related protein 1 (SFRP 1) by promoter hypermethylation in non-small-cell lung cancer. Oncogene 24, 6323-6327 (2005).
24. Lee, A. Y. et al. Expression of the secreted frizzled-related protein gene family is downregulated in human mesothelioma. Oncogene 23, 6672-6676 (2004).
25. Liu, T. H. et al. CpG island methylation and expression of the secreted frizzled-related protein gene family in chronic lymphocytic leukemia. Cancer Res. 66, 653-658 (2006).
26. To, K. F. et al. Alterations of frizzled (FzE3) and secreted frizzled related protein (hsFRP) expression in gastric cancer. Life Sci. 70, 483-489 (2001).
27. Ugolini, F. et al. WNT pathway and mammary carcinogenesis: Loss of expression of candidate tumor suppressor gene SFRP1 in most invasive carcinomas except of the medullary type. Oncogene 20, 5810-5817 (2001).
28. Wong, S. C. et al. Expression of frizzled-related protein and Wnt-signalling molecules in invasive human breast tumours. J. Pathol. 196, 145-153 (2002).
29. Zou, H. et al. Aberrant methylation of secreted frizzled-related protein genes in esophageal adenocarcinoma and Barrett's esophagus. Int. J. Cancer 116, 584-591 (2005).
30. Ai, L. et al. Inactivation of Wnt inhibitory factor-1 (WIF1) expression by epigenetic silencing is a common event in breast cancer. Carcinogenesis 27, 1341-1348 (2006).
31. Batra, S. et al. Wnt inhibitory factor-1, a Wnt antagonist, is silenced by promoter hypermethylation in malignant pleural mesothelioma. Biochem. Biophys. Res. Commun. 342, 1228-1232 (2006).
32. Mazieres, J. et al. Wnt inhibitory factor-1 is silenced by promoter hypermethylation in human lung cancer. Cancer Res. 64, 4717-4720 (2004).
33. Urakami, S. et al. Epigenetic inactivation of Wnt inhibitory factor-1 plays an important role in bladder cancer through aberrant canonical Wnt/ β-catenin signaling pathway. Clin. Cancer Res. 12, 383-391 (2006).
34. Wissmann, C. et al. WIF1, a component of the Wnt pathway, is down-regulated in prostate, breast, lung, and bladder cancer. J. Pathol. 201, 204-212 (2003).
35. Clement, G., Braunschweig, R., Pasquier, N., Bosman, F. T. & Benhattar, J. Alterations of the Wnt signaling pathway during the neoplastic progression of Barrett's esophagus. Oncogene 25, 3084-3092 (2006).
36. He, B. et al. Wnt signaling in stem cells and non-small-cell lung cancer. Clin. Lung Cancer 7, 54-60 (2005).
37. Katoh, M. Expression and regulation of WNT1 in human cancer: up-regulation of WNT1 by β-estradiol in MCF-7 cells. Int. J. Oncol. 22, 209-212 (2003).
38. Katoh, M., Kirikoshi, H., Terasaki, H. & Shiokawa, K. WNT2B2 mRNA, up-regulated in primary gastric cancer, is a positive regulator of the WNT-β-catenin-TCF signaling pathway. Biochem. Biophys. Res. Commun. 289, 1093-1098 (2001).
39. Mazieres, J. et al. Wnt2 as a new therapeutic target in malignant pleural mesothelioma. Int. J. Cancer 117, 326-332 (2005).
40. Milovanovic, T. et al. Expression of Wnt genes and frizzled 1 and 2 receptors in normal breast epithelium and infiltrating breast carcinoma. Int. J. Oncol. 25, 1337-1342 (2004).
41. Miyaoka, T., Seno, H. & Ishino, H. Increased expression of Wnt-1 in schizophrenic brains. Schizophr Res 38, 1-6 (1999).
42. Rhee, C. S. et al. Wnt and frizzled receptors as potential targets for immunotherapy in head and neck squamous cell carcinomas. Oncogene 21, 6598-6605 (2002).
43. Sen, M., Chamorro, M., Reifert, J., Corr, M. & Carson, D. A. Blockade of Wnt-5A/frizzled 5 signaling inhibits rheumatoid synoviocyte activation. Arthritis Rheum. 44, 772-781 (2001).
44. Sen, M. et al. Expression and function of wingless and frizzled homologs in rheumatoid arthritis. Proc. Natl Acad. Sci. USA 97, 2791-2796 (2000).
45. You, L. et al. Inhibition of Wnt-2-mediated signaling induces programmed cell death in non-small-cell lung cancer cells. Oncogene 23, 6170-6174 (2004).
46. You, L. et al. Wnt-1 signal as a potential cancer therapeutic target. Drug News Perspect. 19, 27-31 (2006).
47. Kirikoshi, H., Sekihara, H. & Katoh, M. Up-regulation of Frizzled-7 (FZD7) in human gastric cancer. Int. J. Oncol. 19, 111-115 (2001).
48. Okino, K. et al. Up-regulation and overproduction of DVL-1, the human counterpart of the Drosophila dishevelled gene, in cervical squamous cell carcinoma. Oncol. Rep. 10, 1219-1223 (2003).
49. Uematsu, K. et al. Activation of the Wnt pathway in non small cell lung cancer: Evidence of dishevelled overexpression. Oncogene 22, 7218-7221 (2003).
50. Uematsu, K. et al. Wnt pathway activation in mesothelioma: Evidence of Dishevelled overexpression and transcriptional activity of β-catenin. Cancer Res. 63, 4547-4551 (2003).
51. Rubinfeld, B. et al. Stabilization of β-catenin by genetic defects in melanoma cell lines. Science 275, 1790-1792 (1997).
52. DuBois, R. N., Giardiello, F. M. & Smalley, W. E. Nonsteroidal anti-inflammatory drugs, eicosanoids, and colorectal cancer prevention. Gastroenterol. Clin. North Am. 25, 773-791 (1996).
53. Giovannucci, E. et al. Aspirin use and the risk for colorectal cancer and adenoma in male health professionals. Ann. Intern. Med. 121, 241-246 (1994).
54. Thun, M. J. Aspirin and gastrointestinal cancer. Adv. Exp. Med. Biol. 400A, 395-402 (1997).
55. Smalley, W. E. & DuBois, R. N. Colorectal cancer and nonsteroidal anti-inflammatory drugs. Adv. Pharmacol. 39, 1-20 (1997).
56. Thun, M. J., Henley, S. J. & Patrono, C. Nonsteroidal anti-inflammatory drugs as anticancer agents: Mechanistic, pharmacologic, and clinical issues. J. Natl Cancer Inst. 94, 252-266 (2002).
57. Maier, T. J., Schilling, K., Schmidt, R., Geisslinger, G. & Grosch, S. Cyclooxygenase-2 (COX-2)-dependent and-independent anticarcinogenic effects of celecoxib in human colon carcinoma cells. Biochem. Pharmacol. 67, 1469-1478 (2004).
58. Zhang, X., Morham, S. G., Langenbach, R. & Young, D. A. Malignant transformation and antineoplastic actions of nonsteroidal antiinflammatory drugs (NSAIDs) on cyclooxygenase-null embryo fibroblasts. J. Exp. Med. 190, 451-459 (1999).
59. Smith, M. L., Hawcroft, G. & Hull, M. A. The effect of non-steroidal anti-inflammatory drugs on human colorectal cancer cells: Evidence of different mechanisms of action. Eur. J. Cancer 36, 664-674 (2000).
60. Giardiello, F. M. et al. Treatment of colonic and rectal adenomas with sulindac in familial adenomatous polyposis. N. Engl. J. Med. 328, 1313-1316 (1993).
61. Koehne, C. H. & Dubois, R. N. COX-2 inhibition and colorectal cancer. Semin. Oncol. 31, 12-21 (2004).
62. Jolly, K., Cheng, K. K. & Langman, M. J. NSAIDs and gastrointestinal cancer prevention. Drugs 62, 945-956 (2002).
63. Yang, K. et al. Regional response leading to tumorigenesis after sulindac in small and large intestine of mice with Apc mutations. Carcinogenesis 24, 605-611 (2003).
64. Mahmoud, N. N. et al. The sulfide metabolite of sulindac prevents tumors and restores enterocyte apoptosis in a murine model of familial adenomatous polyposis. Carcinogenesis 19, 87-91 (1998).
65. Phillips, R. K. et al. A randomised, double blind, placebo controlled study of celecoxib, a selective cyclooxygenase 2 inhibitor, on duodenal polyposis in familial adenomatous polyposis. Gut 50, 857-860 (2002).
66. Steinbach, G. et al. The effect of celecoxib, a cyclooxygenase-2 inhibitor, in familial adenomatous polyposis. N. Engl. J. Med. 342, 1946-1952 (2000).
67. Labayle, D. et al. Sulindac causes regression of rectal polyps in familial adenomatous polyposis. Gastroenterology 101, 635-639 (1991).
68. Boon, E. M. et al. Sulindac targets nuclear β-catenin accumulation and Wnt signalling in adenomas of patients with familial adenomatous polyposis and in human colorectal cancer cell lines. Br. J. Cancer 90, 224-229 (2004).
69. Shao, J., Jung, C., Liu, C. & Sheng, H. Prostaglandin E2 stimulates the β-catenin/T cell factor-dependent transcription in colon cancer. J. Biol. Chem. 280, 26565-26572 (2005).
70. Castellone, M. D., Teramoto, H., Williams, B. O., Druey, K. M. & Gutkind, J. S. Prostaglandin E2 promotes colon cancer cell growth through a Gs-axin-β-catenin signaling axis. Science 310, 1504-1510 (2005).
71. Maier, T. J., Janssen, A., Schmidt, R., Geisslinger, G. & Grosch, S. Targeting the β-catenin/APC pathway: A novel mechanism to explain the cyclooxygenase-2-independent anticarcinogenic effects of celecoxib in human colon carcinoma cells. FASEB J. 19, 1353-1355 (2005).
72. Solomon, D. H. et al. Cardiovascular outcomes in new users of coxibs and nonsteroidal antiinflammatory drugs: High-risk subgroups and time course of risk. Arthritis Rheum. 54, 1378-1389 (2006).
73. Solomon, S. D. et al. Cardiovascular risk associated with celecoxib in a clinical trial for colorectal adenoma prevention. N. Engl. J. Med. 352, 1071-1080 (2005).
74. Williams, J. L. et al. Nitric oxide-releasing nonsteroidal anti-inflammatory drugs (NSAIDs) alter the kinetics of human colon cancer cell lines more effectively than traditional NSAIDs: Implications for colon cancer chemoprevention. Cancer Res. 61, 3285-3289 (2001).
75. Rigas, B. & Williams, J. L. NO-releasing NSAIDs and colon cancer chemoprevention: A promising novel approach (Review). Int. J. Oncol. 20, 885-890 (2002).
76. Fiorucci, S. & Del Soldato, P. NO-aspirin: Mechanism of action and gastrointestinal safety. Dig. Liver Dis. 35 (Suppl. 2), S9-S19 (2003).
77. Fiorucci, S. et al. Gastrointestinal safety of NO-aspirin (NCX-4016) in healthy human volunteers: A proof of concept endoscopic study. Gastroenterology 124, 600-607 (2003).
78. Williams, J. L. et al. NO-donating aspirin inhibits intestinal carcinogenesis in Min (APC(Min/+)) mice. Biochem. Biophys. Res. Commun. 313, 784-788 (2004).
79. Gao, J., Liu, X. & Rigas, B. Nitric oxide-donating aspirin induces apoptosis in human colon cancer cells through induction of oxidative stress. Proc. Natl Acad. Sci. USA 102, 17207-17212 (2005).
80. Nath, N., Kashfi, K., Chen, J. & Rigas, B. Nitric oxide-donating aspirin inhibits β-catenin/T cell factor (TCF) signaling in SW480 colon cancer cells by disrupting the nuclear β-catenin-TCF association. Proc. Natl Acad. Sci. USA 100, 12584-12589 (2003).
81. Soprano, D. R., Qin, P. & Soprano, K. J. Retinoic acid receptors and cancers. Annu. Rev. Nutr. 24, 201-221 (2004).
82. Shah, S., Hecht, A., Pestell, R. & Byers, S. W. Trans-repression of β-catenin activity by nuclear receptors. J. Biol. Chem. 278, 48137-48145 (2003).
83. Shah, S., Pishvaian, M. J., Easwaran, V., Brown, P. H. & Byers, S. W. The role of cadherin, β-catenin, and AP-1 in retinoid-regulated carcinoma cell differentiation and proliferation. J. Biol. Chem. 277, 25313-25322 (2002).
84. Xiao, J. H. et al. Adenomatous polyposis coli (APC)-independent regulation of β-catenin degradation via a retinoid X receptor-mediated pathway. J. Biol. Chem. 278, 29954-29962 (2003).
85. Hoosein, N. M. et al. Comparison of the antiproliferative effects of transforming growth factor-β, N,N-dimethylformamide and retinoic acid on a human colon carcinoma cell line. Cancer Lett. 40, 219-232 (1988).
86. O'Dwyer, P. J., Ravikumar, T. S., McCabe, D. P. & Steele, G., Jr. Effect of 13-cis-retinoic acid on tumor prevention, tumor growth, and metastasis in experimental colon cancer. J. Surg. Res. 43, 550-557 (1987).
87. Mollersen, L., Paulsen, J. E., Olstorn, H. B., Knutsen, H. K. & Alexander, J. Dietary retinoic acid supplementation stimulates intestinal tumour formation and growth in multiple intestinal neoplasia (Min)/+ mice. Carcinogenesis 25, 149-153 (2004).
88. Giovannucci, E., and Platz, E. A. Vitamin D, (Elsevier Academic Press, Burlington, MA, 2005).
89. Akhter, J., Chen, X., Bowrey, P., Bolton, E. J. & Morris, D. L. Vitamin D3 analog, EB1089, inhibits growth of subcutaneous xenografts of the human colon cancer cell line, LoVo, in a nude mouse model. Dis. Colon Rectum 40, 317-321 (1997).
90. VanWeelden, K., Flanagan, L., Binderup, L., Tenniswood, M. & Welsh, J. Apoptotic regression of MCF-7 xenografts in nude mice treated with the vitamin D3 analog, EB1089. Endocrinology 139, 2102-2110 (1998).
91. Harris, D. M. & Go, V. L. Vitamin D and colon carcinogenesis. J. Nutr. 134, 3463S-3471S (2004).
92. Palmer, H. G. et al. Vitamin D(3) promotes the differentiation of colon carcinoma cells by the induction of E-cadherin and the inhibition of β-catenin signaling. J. Cell Biol. 154, 369-387 (2001).
93. Shah, S. et al. The molecular basis of vitamin D receptor and β-catenin crossregulation. Mol. Cell 21, 799-809 (2006).
94. Binderup E., C. M. J., Binderup L. Synthesis and biological activity of 1-hydroxylated vitamin D analogs with polyunsaturated side chains. Vitamin D, Gene Regulation, Structure-Function Analysis and Clinical Application, 192-193 (1991).
95. Vandewalle, B., Adenis, A., Hornez, L., Revillion, F. & Lefebvre, J. 1, 25-dihydroxyvitamin D3 receptors in normal and malignant human colorectal tissues. Cancer Lett. 86, 67-73 (1994).
96. Kallay, E. et al. Vitamin D receptor activity and prevention of colonic hyperproliferation and oxidative stress. Food Chem. Toxicol. 40, 1191-1196 (2002).
97. He, B. et al. A monoclonal antibody against Wnt-1 induces apoptosis in human cancer cells. Neoplasia 6, 7-14 (2004).
98. Holcombe, R. F. et al. Expression of Wnt ligands and Frizzled receptors in colonic mucosa and in colon carcinoma. Mol. Pathol. 55, 220-226 (2002).
99. Vider, B. Z. et al. Evidence for the involvement of the Wnt 2 gene in human colorectal cancer. Oncogene 12, 153-158 (1996).
100. Smith, K. et al. Up-regulation of macrophage wnt gene expression in adenoma-carcinoma progression of human colorectal cancer. Br. J. Cancer 81, 496-502 (1999).
101. You, L. et al. An anti-Wnt-2 monoclonal antibody induces apoptosis in malignant melanoma cells and inhibits tumor growth. Cancer Res. 64, 5385-5389 (2004).
102. Taketo, M. M. Shutting down Wnt signal-activated cancer. Nature Genet. 36, 320-322 (2004).
103. Berg, T. et al. Small-molecule antagonists of Myc/Max dimerization inhibit Myc-induced transformation of chicken embryo fibroblasts. Proc. Natl Acad. Sci. USA 99, 3830-3835 (2002).
104. Chen, J. K., Taipale, J., Young, K. E., Maiti, T. & Beachy, P. A. Small molecule modulation of Smoothened activity. Proc. Natl Acad. Sci. USA 99, 14071-14076 (2002).
105. Graham, T. A., Ferkey, D. M., Mao, F., Kimelman, D. & Xu, W. Tcf4 can specifically recognize β-catenin using alternative conformations. Nature Struct. Biol. 8, 1048-1052 (2001).
106. Graham, T. A., Weaver, C., Mao, F., Kimelman, D. & Xu, W. Crystal structure of a β-catenin/Tcf complex. Cell 103, 885-896 (2000).
107. Poy, F., Lepourcelet, M., Shivdasani, R. A. & Eck, M. J. Structure of a human Tcf4- β-catenin complex. Nature Struct. Biol. 8, 1053-1057 (2001).
108. Fasolini, M. et al. Hot spots in Tcf4 for the interaction with β-catenin. J. Biol. Chem. 278, 21092-21098 (2003).
109. Knapp, S. et al. Thermodynamics of the high-affinity interaction of TCF4 with β-catenin. J. Mol. Biol. 306, 1179-1189 (2001).
110. Omer, C. A., Miller, P. J., Diehl, R. E. & Kral, A. M. Identification of Tcf4 residues involved in high-affinity β-catenin binding. Biochem. Biophys. Res. Commun. 256, 584-590 (1999).
111. von Kries, J. P. et al. Hot spots in β-catenin for interactions with LEF-1, conductin and APC. Nature Struct. Biol. 7, 800-807 (2000).
112. Huber, A. H. & Weis, W. I. The structure of the β-catenin/E-cadherin complex and the molecular basis of diverse ligand recognition by β-catenin. Cell 105, 391-402 (2001).
113. Xing, Y. et al. Crystal structure of a β-catenin/APC complex reveals a critical role for APC phosphorylation in APC function. Mol. Cell 15, 523-533 (2004).
114. Molenaar, M. et al. XTcf-3 transcription factor mediates β-catenin-induced axis formation in Xenopus embryos. Cell 86, 391-399 (1996).
115. Lepourcelet, M. et al. Small-molecule antagonists of the oncogenic Tcf/ β-catenin protein complex. Cancer Cell 5, 91-102 (2004).
116. Trosset, J. Y. et al. Inhibition of protein-protein interactions: The discovery of druglike β-catenin inhibitors by combining virtual and biophysical screening. Proteins 64, 60-67 (2006).
117. Hecht, A., Vleminckx, K., Stemmler, M. P., van Roy, F. & Kemler, R. The p300/CBP acetyltransferases function as transcriptional coactivators of β-catenin in vertebrates. EMBO J. 19, 1839-1850 (2000).
118. Takemaru, K. I. & Moon, R. T. The transcriptional coactivator CBP interacts with β-catenin to activate gene expression. J. Cell Biol. 149, 249-254 (2000).
119. Hoffmans, R., Stadeli, R. & Basler, K. Pygopus and legless provide essential transcriptional coactivator functions to armadillo/β-catenin. Curr. Biol. 15, 1207-1211 (2005).
120. Kramps, T. et al. Wnt/wingless signaling requires BCL9/legless-mediated recruitment of pygopus to the nuclear β-catenin-TCF complex. Cell 109, 47-60 (2002).
121. Stadeli, R. & Basler, K. Dissecting nuclear Wingless signalling: recruitment of the transcriptional co-activator Pygopus by a chain of adaptor proteins. Mech. Dev. 122, 1171-1182 (2005).
122. Emami, K. H. et al. A small molecule inhibitor of β-catenin/ CREB-binding protein transcription [corrected]. Proc. Natl Acad. Sci. USA 101, 12682-12687 (2004).
123. Hecht, A., Litterst, C. M., Huber, O. & Kemler, R. Functional characterization of multiple transactivating elements in β-catenin, some of which interact with the TATA-binding protein in vitro. J. Biol. Chem. 274, 18017-18025 (1999).
124. Barker, N. et al. The chromatin remodelling factor Brg-1 interacts with β-catenin to promote target gene activation. EMBO J. 20, 4935-4943 (2001).
125. Kim, S., Xu, X., Hecht, A. & Boyer, T. G. Mediator is a transducer of Wnt/β-catenin signaling. J. Biol. Chem. 281, 14066-14075 (2006).
126. Mosimann, C., Hausmann, G. & Basler, K. Parafibromin/Hyrax activates Wnt/ Wg target gene transcription by direct association with β-catenin/ Armadillo. Cell 125, 327-341 (2006).
127. He, X. & Axelrod, J. D. A WNTer wonderland in Snowbird. Development 133, 2597-2603 (2006).
128. Shan, J., Shi, D. L., Wang, J. & Zheng, J. Identification of a specific inhibitor of the dishevelled PDZ domain. Biochemistry 44, 15495-15503 (2005).
129. Cong, F., Schweizer, L. & Varmus, H. Wnt signals across the plasma membrane to activate the β-catenin pathway by forming oligomers containing its receptors, Frizzled and LRP. Development 131, 5103-5115 (2004).
130. Wong, H. C. et al. Direct binding of the PDZ domain of Dishevelled to a conserved internal sequence in the C-terminal region of Frizzled. Mol. Cell 12, 1251-1260 (2003).
131. Zhang, L., Gao, X., Wen, J., Ning, Y. & Chen, Y. G. Dapper 1 antagonizes Wnt signaling by promoting dishevelled degradation. J. Biol. Chem. 281, 8607-8612 (2006).
132. Kaplan, J. M. Adenovirus-based cancer gene therapy. Curr. Gene Ther. 5, 595-605 (2005).
133. Chen, R. H. & McCormick, F. Selective targeting to the hyperactive β-catenin/T-cell factor pathway in colon cancer cells. Cancer Res. 61, 4445-4449 (2001).
134. Lipinski, K. S. et al. Optimization of a synthetic β-catenin-dependent promoter for tumor-specific cancer Gene Therapy. Mol Ther 10, 150-161 (2004).
135. Kwong, K. Y., Zou, Y., Day, C. P. & Hung, M. C. The suppression of colon cancer cell growth in nude mice by targeting β-catenin/TCF pathway. Oncogene 21, 8340-8346 (2002).
136. Brunori, M., Malerba, M., Kashiwazaki, H. & Iggo, R. Replicating adenoviruses that target tumors with constitutive activation of the wnt signaling pathway. J. Virol. 75, 2857-2865 (2001).
137. Fuerer, C. & Iggo, R. Adenoviruses with Tcf binding sites in multiple early promoters show enhanced selectivity for tumour cells with constitutive activation of the wnt signalling pathway. Gene Ther. 9, 270-281 (2002).
138. Toth, K. et al. An oncolytic adenovirus vector combining enhanced cell-to-cell spreading, mediated by the ADP cytolytic protein, with selective replication in cancer cells with deregulated wnt signaling. Cancer Res. 64, 3638-3644 (2004).
139. Fuerer, C. & Iggo, R. 5-Fluorocytosine increases the toxicity of Wnt-targeting replicating adenoviruses that express cytosine deaminase as a late gene. Gene Ther. 11, 142-151 (2004).
140. Lukashev, A. N., Fuerer, C., Chen, M. J., Searle, P. & Iggo, R. Late expression of nitroreductase in an oncolytic adenovirus sensitizes colon cancer cells to the prodrug CB1954. Hum Gene Ther. 16, 1473-1483 (2005).
141. Dang, C. V. c-Myc target genes involved in cell growth, apoptosis, and metabolism. Mol. Cell. Biol. 19, 1-11 (1999).
142. Chen, J. P., Chen, L., Leek, J. & Lin, C. Antisense c-myc fragments induce normal differentiation cycles in HL-60 cells. Eur. J. Clin. Invest. 36, 49-57 (2006).
143. Iversen, P. L., Arora, V., Acker, A. J., Mason, D. H. & Devi, G. R. Efficacy of antisense morpholino oligomer targeted to c-myc in prostate cancer xenograft murine model and a Phase I safety study in humans. Clin. Cancer Res. 9, 2510-2519 (2003).
144. Arango, D., Corner, G. A., Wadler, S., Catalano, P. J. & Augenlicht, L. H. c-myc/p53 interaction determines sensitivity of human colon carcinoma cells to 5-fluorouracil in vitro and in vivo. Cancer Res. 61, 4910-4915 (2001).
145. Arango, D. et al. c-Myc overexpression sensitises colon cancer cells to camptothecin-induced apoptosis. Br. J. Cancer 89, 1757-1765 (2003).
146. Bressin, C. et al. Decrease in c-Myc activity enhances cancer cell sensitivity to vinblastine. Anticancer Drugs 17, 181-187 (2006).
147. Sansom, O. J. et al. Cyclin D1 is not an immediate target of β-catenin following Apc loss in the intestine. J. Biol. Chem. 280, 28463-28467 (2005).
148. Whittaker, S. R., Walton, M. I., Garrett, M. D. & Workman, P. The Cyclin-dependent kinase inhibitor CYC202 (R-roscovitine) inhibits retinoblastoma protein phosphorylation, causes loss of Cyclin D1, and activates the mitogen-activated protein kinase pathway. Cancer Res. 64, 262-272 (2004).
149. Batlle, E. et al. EphB receptor activity suppresses colorectal cancer progression. Nature 435, 1126-1130 (2005).
150. van Es, J. H. & Clevers, H. Notch and Wnt inhibitors as potential new drugs for intestinal neoplastic disease. Trends Mol. Med. 11, 496-502 (2005).
151. Terasaki, H., Saitoh, T., Shiokawa, K. & Katoh, M. Frizzled-10, up-regulated in primary colorectal cancer, is a positive regulator of the WNT-β-catenin-TCF signaling pathway. Int. J. Mol. Med. 9, 107-112 (2002).
152. Nagayama, S. et al. Therapeutic potential of antibodies against FZD 10, a cell-surface protein, for synovial sarcomas. Oncogene 24, 6201-6212 (2005).
153. Esteller, M. et al. Analysis of adenomatous polyposis coli promoter hypermethylation in human cancer. Cancer Res. 60, 4366-4371 (2000).
154. Kinzler, K. W. & Vogelstein, B. Lessons from hereditary colorectal cancer. Cell 87, 159-170 (1996).
155. Bienz, M. & Clevers, H. Linking colorectal cancer to Wnt signaling. Cell 103, 311-320 (2000).
156. Ishizaki, Y. et al. Immunohistochemical analysis and mutational analyses of β-catenin, Axin family and APC genes in hepatocellular carcinomas. Int. J. Oncol. 24, 1077-1083 (2004).
157. Taniguchi, K. et al. Mutational spectrum of β-catenin, AXIN1, and AXIN2 in hepatocellular carcinomas and hepatoblastomas. Oncogene 21, 4863-4871 (2002).
158. Koinuma, K. et al. Epigenetic silencing of AXIN2 in colorectal carcinoma with microsatellite instability. Oncogene 25, 139-146 (2006).
159. Boyden, L. M. et al. High bone density due to a mutation in LDL-receptor-related protein 5. N. Engl. J. Med. 346, 1513-1521 (2002).
160. Little, R. D. et al. A mutation in the LDL receptor-related protein 5 gene results in the autosomal dominant high-bone-mass trait. Am. J. Hum. Genet. 70, 11-19 (2002).
161. Amit, S. et al. Axin-mediated CKI phosphorylation of β-catenin at Ser 45: A molecular switch for the Wnt pathway. Genes Dev. 16, 1066-1076 (2002).
162. Liu, C. et al. Control of β-catenin phosphorylation/ degradation by a dual-kinase mechanism. Cell 108, 837-847 (2002).
163. Kitagawa, M. et al. An F-box protein, FWD1, mediates ubiquitin-dependent proteolysis of β-catenin. EMBO J. 18, 2401-2410 (1999).
164. Winston, J. T. et al. The SCFβ-TRCP-ubiquitin ligase complex associates specifically with phosphorylated destruction motifs in IkappaBalpha and β-catenin and stimulates IkappaBalpha ubiquitination in vitro. Genes Dev. 13, 270-283 (1999).
165. Cavallo, R. A. et al. Drosophila Tcf and Groucho interact to repress Wingless signalling activity. Nature 395, 604-608 (1998).
166. Roose, J. et al. The Xenopus Wnt effector XTcf-3 interacts with Groucho-related transcriptional repressors. Nature 395, 608-612 (1998).
167. Davidson, G. et al. Casein kinase 1γ couples Wnt receptor activation to cytoplasmic signal transduction. Nature 438, 867-872 (2005).
168. Zeng, X. et al. A dual-kinase mechanism for Wnt co-receptor phosphorylation and activation. Nature 438, 873-877 (2005).
169. Behrens, J. et al. Functional interaction of β-catenin with the transcription factor LEF-1. Nature 382, 638-642 (1996).
170. Daniels, D. L. & Weis, W. I. β-catenin directly displaces Groucho/TLE repressors from Tcf/Lef in Wnt-mediated transcription activation. Nature Struct. Mol. Biol. 12, 364-371 (2005).
171. He, T. C. et al. Identification of c-MYC as a target of the APC pathway. Science 281, 1509-1512 (1998).
172. Eberhart, C. E. et al. Up-regulation of cyclooxygenase 2 gene expression in human colorectal adenomas and adenocarcinomas. Gastroenterology 107, 1183-1188 (1994).
173. Turini, M. E. & DuBois, R. N. Cyclooxygenase-2: A therapeutic target. Annu. Rev. Med. 53, 35-57 (2002).
174. Takeda, H. et al. Cooperation of cyclooxygenase 1 and cyclooxygenase 2 in intestinal polyposis. Cancer Res. 63, 4872-4877 (2003).
175. Oshima, M. et al. Suppression of intestinal polyposis in Apc δ716 knockout mice by inhibition of cyclooxygenase 2 (COX-2). Cell 87, 803-809 (1996).
176. Chulada, P. C. et al. Genetic disruption of Ptgs-1, as well as Ptgs-2, reduces intestinal tumorigenesis in Min mice. Cancer Res. 60, 4705-4708 (2000).
177. Wang, D. et al. Prostaglandin E(2) promotes colorectal adenoma growth via transactivation of the nuclear peroxisome proliferator-activated receptor δ. Cancer Cell 6, 285-295 (2004).
178. Germann, A., Dihlmann, S., Hergenhahn, M., Doeberitz, M. K. & Koesters, R. Expression profiling of CC531 colon carcinoma cells reveals similar regulation of β-catenin target genes by both butyrate and aspirin. Int. J. Cancer 106, 187-197 (2003).
179. Dihlmann, S., Siermann, A. & von Knebel Doeberitz, M. The nonsteroidal anti-inflammatory drugs aspirin and indomethacin attenuate β-catenin/ TCF-4 signaling. Oncogene 20, 645-653 (2001).
180. Mahmoud, N. N. et al. Aspirin prevents tumors in a murine model of familial adenomatous polyposis. Surgery 124, 225-231 (1998).
181. Dihlmann, S., Klein, S. & Doeberitz Mv, M. K. Reduction of β-catenin/ T-cell transcription factor signaling by aspirin and indomethacin is caused by an increased stabilization of phosphorylated β-catenin. Mol. Cancer Ther. 2, 509-516 (2003).
182. Winter, C. A., Risley, E. A. & Nuss, G. W. Antiinflammatory and antipyretic activities of indomethacin, 1-(P-Chlorobenzoyl)-5-methoxy-2-methylindole-3-acetic acid. J. Pharmacol. Exp. Ther. 141, 369-376 (1963).
183. Brown, W. A., Skinner, S. A., Malcontenti-Wilson, C., Vogiagis, D. & O'Brien, P. E. Non-steroidal anti-inflammatory drugs with activity against either cyclooxygenase 1 or cyclooxygenase 2 inhibit colorectal cancer in a DMH rodent model by inducing apoptosis and inhibiting cell proliferation. Gut 48, 660-666 (2001).
184. Brown, W. A., Skinner, S. A., Vogiagis, D. & O'Brien, P. E. Inhibition of β-catenin translocation in rodent colorectal tumors: A novel explanation for the protective effect of nonsteroidal antiinflammatory drugs in colorectal cancer. Dig. Dis. Sci. 46, 2314-2321 (2001).
185. Hawcroft, G. et al. Indomethacin induces differential expression of β-catenin, γ-catenin and T-cell factor target genes in human colorectal cancer cells. Carcinogenesis 23, 107-114 (2002).
186. Hirata, K., Itoh, H. & Ohsato, K. Regression of rectal polyps by indomethacin suppository in familial adenomatous polyposis. Report of two cases. Dis. Colon Rectum 37, 943-946 (1994).
187. Hirota, C. et al. Effect of indomethacin suppositories on rectal polyposis in patients with familial adenomatous polyposis. Cancer 78, 1660-1665 (1996).
188. Chiu, C. H., McEntee, M. F. & Whelan, J. Discordant effect of aspirin and indomethacin on intestinal tumor burden in Apc(Min/+)mice. Prostaglandins Leukot. Essent. Fatty Acids 62, 269-275 (2000).
189. Gardner, S. H., Hawcroft, G. & Hull, M. A. Effect of nonsteroidal anti-inflammatory drugs on β-catenin protein levels and catenin-related transcription in human colorectal cancer cells. Br. J. Cancer 91, 153-163 (2004).
190. McEntee, M. F., Chiu, C. H. & Whelan, J. Relationship of β-catenin and Bcl-2 expression to sulindac-induced regression of intestinal tumors in Min mice. Carcinogenesis 20, 635-640 (1999).
191. Li, H. et al. Pro-apoptotic actions of exisulind and CP461 in SW480 colon tumor cells involve β-catenin and cyclin D1 down-regulation. Biochem. Pharmacol. 64, 1325-1336 (2002).
192. Rice, P. L. et al. Sulindac metabolites induce caspase- and proteasome-dependent degradation of β-catenin protein in human colon cancer cells. Mol. Cancer Ther. 2, 885-892 (2003).
193. Piazza, G. A. et al. Sulindac sulfone inhibits azoxymethane-induced colon carcinogenesis in rats without reducing prostaglandin levels. Cancer Res. 57, 2909-2915 (1997).
194. Thompson, W. J. et al. Exisulind induction of apoptosis involves guanosine 3′,5′-cyclic monophosphate phosphodiesterase inhibition, protein kinase G activation, and attenuated β-catenin. Cancer Res. 60, 3338-3342 (2000).
195. Zhu, B., Vemavarapu, L., Thompson, W. J. & Strada, S. J. Suppression of cyclic GMP-specific phosphodiesterase 5 promotes apoptosis and inhibits growth in HT29 cells. J. Cell. Biochem. 94, 336-350 (2005).
196. Chang, W. C. et al. Sulindac sulfone is most effective in modulating β-catenin-mediated transcription in cells with mutant APC. Ann. NY Acad. Sci. 1059, 41-55 (2005).
197. Li, H., Pamukcu, R. & Thompson, W. J. β-catenin signaling: Therapeutic strategies in oncology. Cancer Biol. Ther. 1, 621-625 (2002).
198. Stoner, G. D. et al. Sulindac sulfone induced regression of rectal polyps in patients with familial adenomatous polyposis. Adv. Exp. Med. Biol. 470, 45-53 (1999).
199. van Stolk, R. et al. Phase I trial of exisulind (sulindac sulfone, FGN-1) as a chemopreventive agent in patients with familial adenomatous polyposis. Clin. Cancer Res. 6, 78-89 (2000).
200. Arber, N. et al. Sporadic adenomatous polyp regression with exisulind is effective but toxic: A randomised, double blind, placebo controlled, dose-response study. Gut 55, 367-373 (2006).