Antihelminth compound niclosamide downregulates Wnt signaling and elicits antitumor responses in tumors with activating APC mutations

Cancer Research

Volumn 71, Issue 12, 2011, Pages 4172-4182

  Osada, Takuya ^a   Chen, Minyong ^a   Yang, Xiao Yi ^a   Spasojevic, Ivan ^a   Vandeusen, Jeffrey B ^a   Hsu, David ^a   Clary, Bryan M ^a   Clay, Timothy M ^a   Chen, Wei ^a   Morse, Michael A ^a   Lyerly, H Kim ^a  

^a DUKE UNIVERSITY MEDICAL CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

6 CHLORO 8 NICOTINAMIDO BETA CARBOLINE; APC PROTEIN; BETA CATENIN; DISHEVELLED 2; EVEROLIMUS; FRIZZLED PROTEIN; IMMUNOGLOBULIN ENHANCER BINDING PROTEIN; MAMMALIAN TARGET OF RAPAMYCIN; NICLOSAMIDE; OXALIPLATIN; TUMOR NECROSIS FACTOR ALPHA; WNT PROTEIN;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CANCER CELL CULTURE; CELL PROLIFERATION; CELL VIABILITY; COLORECTAL CANCER; COLORECTAL CARCINOMA; CONTROLLED STUDY; CYTOSOL; DOWN REGULATION; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG ELIMINATION; DRUG HALF LIFE; DRUG MECHANISM; DRUG TOLERABILITY; GENE MUTATION; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; NUCLEOTIDE SEQUENCE; OPTICAL DENSITY; PRIORITY JOURNAL; PROTEIN EXPRESSION; SIGNAL TRANSDUCTION; TIME TO MAXIMUM PLASMA CONCENTRATION; TOXICITY TESTING;

ADAPTOR PROTEINS, SIGNAL TRANSDUCING; ANIMALS; ANTHELMINTICS; ANTINEOPLASTIC AGENTS; BETA CATENIN; CELL LINE, TUMOR; CELL PROLIFERATION; COLORECTAL NEOPLASMS; FIBROBLASTS; GENES, APC; HUMANS; MICE; MICE, SCID; MUTATION; NF-KAPPA B; NICLOSAMIDE; ORGANOPLATINUM COMPOUNDS; PHOSPHOPROTEINS; SIGNAL TRANSDUCTION; TOR SERINE-THREONINE KINASES; WNT PROTEINS;

EID: 79958812414     PISSN: 00085472     EISSN: 15387445     Source Type: Journal    
DOI: 10.1158/0008-5472.CAN-10-3978     Document Type: Article

References (32)

1. Fuerer C, Nusse R, Ten Berge D. Wnt signalling in development and disease. Max Delbruck Center for Molecular Medicine meeting on Wnt signaling in development and disease. EMBO Rep 2008;9: 134-8.
2. Chien AJ, Conrad WH, Moon RT. A Wnt survival guide: from flies to human disease. J Invest Dermatol 2009:129;1614-27.
3. Nusse R. Wnt signaling in disease and in development. Cell Res 2005;15:28-32. (Pubitemid 41653961)
4. Katoh M, Katoh M. WNT signaling pathway and stem cell signaling network. Clin Cancer Res 2007;13:4042-5. (Pubitemid 47105963)
5. Katoh M. WNT signaling in stem cell biology and regenerative medicine. Curr Drug Targets 2008;9:565-70.
6. Chen W, ten Berge D, Brown J, Ahn S, Hu LA, Miller WE, et al. Dishevelled 2 recruits beta-arrestin 2 to mediate Wnt5A-stimulated endocytosis of Frizzled 4. Science 2003;301:1391-4.
7. Moon RT, Kohn AD, De Ferrari GV, Kaykas A. WNT and beta-catenin signalling: diseases and therapies. Nat Rev Genet 2004;5:691-701. (Pubitemid 39150127)
8. Segditsas S, Tomlinson I. Colorectal cancer and genetic alterations in the Wnt pathway. Oncogene 2006;25:7531-37. (Pubitemid 44885752)
9. Schneikert J, Behrens J. The canonical Wnt signalling pathway and its APC partner in colon cancer development. Gut 2007;56:417-25. (Pubitemid 46579774)
10. Bafico A, Liu G, Goldin L, Harris V, Aaronson SA. An autocrine mechanism for constitutive Wnt pathway activation in human cancer cells. Cancer Cell 2004;6:497-506. (Pubitemid 39469985)
11. He B, Reguart N, You L, Mazieres J, Xu Z, Lee AY, et al. Blockade of Wnt-1 signaling induces apoptosis in human colorectal cancer cells containing downstream mutations. Oncogene 2005;24: 3054-8. (Pubitemid 40675537)
12. Suzuki H, Watkins DN, Jair KW, Schuebel KE, Markowitz SD, Chen WD, et al. Epigenetic inactivation of SFRP genes allows constitutive WNT signaling in colorectal cancer. Nat Genet 2004;36:417-22. (Pubitemid 38437267)
13. Ding S, Wu TY, Brinker A, Peters EC, Hur W, Gray NS, et al. Synthetic small molecules that control stem cell fate. Proc Natl Acad Sci U S A 2003;100:7632-7. (Pubitemid 36760021)
14. Lepourcelet M, Chen YN, France DS, Wang H, Crews P, Petersen F, et al. Small-molecule antagonists of the oncogenic Tcf/beta-catenin protein complex. Cancer Cell 2004;5:91-102. (Pubitemid 38121599)
15. Shan J, Shi DL, Wang J, Zheng J. Identification of a specific inhibitor of the Dishevelled PDZ domain. Biochemistry 2005;44: 15495-503. (Pubitemid 41706133)
16. Zhang Q, Major MB, Takanashi S, Camp ND, Nishiya N, Peters EC, et al. Small-molecule synergist of the Wnt/beta-catenin signaling pathway. Proc Natl Acad Sci U S A 2007;104:7444-8. (Pubitemid 47185925)
17. Chen M, Wang J, Lu J, Bond MC, Ren XR, Lyerly HK, et al. The antihelminthic niclosamide inhibits Wnt/Frizzled1 signaling. Biochemistry 2009;48:10267-74.
18. Osada T, Hsu D, Hammond S, Hobeika A, Devi G, Clay TM, et al. Metastatic colorectal cancer cells from patients previously treated with chemotherapy are sensitive to T-cell killing mediated by CEA/ CD3-bispecific T-cell-engaging BiTE antibody. Br J Cancer 2010;102:124-33.
19. Groves C, Lamlum H, Crabtree M, Williamson J, Taylor C, Bass S, et al. Mutation cluster region, association between germline and somatic mutations and genotype-phenotype correlation in upper gastrointestinal familial adenomatous polyposis. Am J Pathol 2002;160:2055-61. (Pubitemid 34663398)
20. Rakheja D, Cunningham JC, Mitui M, Patel AS, Tomlinson GE, Weinberg AG. Asubset of cranial fasciitis is associated with dysregulation of the Wnt/beta-catenin pathway. Mod Pathol 2008;21:1330-6.
21. Beuvink I, Boulay A, Fumagalli S, Zilbermann F, Ruetz S, O'Reilly T, et al. The mTOR inhibitor RAD001 sensitizes tumor cells to DNA-damaged induced apoptosis through inhibition of p21 translation. Cell 2005;120:747-59. (Pubitemid 40568794)
22. Yemelyanov A, Gasparian A, Lindholm P, Dang L, Pierce JW, Kisseljov F, et al. Effects of IKK inhibitor PS1145 on NF-kB function, proliferation, apoptosis and invasion activity in prostate carcinoma cells. Oncogene 2006;25:387-98. (Pubitemid 43117624)
23. Mikels AJ, Nusse R. Purified Wnt5a protein activates or inhibits beta-catenin- TCF signaling depending on receptor context. PLoS Biol 2006;4:e115.
24. Wang X, Osada T, Wang Y, Yu L, Sakakura K, Katayama A, et al. CSPG4 protein as a new target for antibody-based immunotherapy of triple-negative breast cancer. J Natl Cancer Inst 2010;102:1-17.
25. Chang YW, Yeh TK, Lin KT, Chen WC, Yao HT, Lan SJ, et al. Pharmacokinetics of anti-SARS-CoV agent niclosamide and its analogs in rats. J. Food Drug Anal 2006;14:329-33.
26. Jin Y, Lu Z, Ding K, Li J, Du X, Chen C, et al. Antineoplastic mechanisms of niclosamide in acute myelogenous leukemia stem cells: inactivation of the NF-{kappa}B pathway and generation of reactive oxygen species. Cancer Res 2010;70:2516-27.
27. Balgi AD, Fonseca BD, Donohue E, Tsang TC, Lajoie P, Proud CG, et al. Screen for chemical modulators of autophagy reveals novel therapeutic inhibitors of mTORC1 signaling. PLoS One 2009;4: e7124.
28. Pearson RD, Hewlett EL. Niclosamide therapy for tapeworm infections. Ann Intern Med 1985;102:550-1.
29. Wu ZS, Wang TG, Zhang XS, Zhong B, Xu L, Gao GB, et al. [Snail control by using soil pasting mixed with niclosamide]. Zhonghua Yu Fang Yi Xue Za Zhi 2008;42:569-73.
30. Weinbach EC, Garbus J. Mechanism of action of reagents that uncouple oxidative phosphorylation. Nature 1969;221:1016-8.
31. Wu CJ, Jan JT, Chen CM, Hsieh HP, Hwang DR, Liu HW, et al. Inhibition of severe acute respiratory syndrome coronavirus replication by niclosamide. Antimicrob Agents Chemother 2004;48:2693-6.
32. Angers S, Thorpe CJ, Biechele TL, Goldenberg SJ, Zheng N, Mac- Coss MJ, et al. The KLHL12-Cullin-3 ubiquitin ligase negatively regulates the Wnt-β-catenin pathway by targeting Dishevelled for degradation. Nat Cell Biol 2006;8:348-57.