A biochemical screen for identification of small-molecule regulators of the Wnt pathway using Xenopus egg extracts

Journal of Biomolecular Screening

Volumn 16, Issue 9, 2011, Pages 995-1006

  Thorne, Curtis A ^a,b   Lafleur, Bonnie ^c,d   Lewis, Michelle ^a   Hanson, Alison J ^a   Jernigan, Kristin K ^a   Weaver, David C ^a   Huppert, Kari A ^a,e   Chen, Tony W ^a   Wichaidit, Chonlarat ^b   Cselenyi, Christopher S ^a   Tahinci, Emilios ^a   Meyers, Kelly C ^a   Waskow, Emily ^a   Orton, Darren ^f   Salic, Adrian ^g   Lee, Laura A ^a,h   Robbins, David J ⁱ   Huppert, Stacey S ^a,e,h   Lee, Ethan ^a,h  

^a VANDERBILT UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b UNIVERSITY OF TEXAS AT DALLAS   (United States)

^c VANDERBILT UNIVERSITY   (United States)

^d UNIVERSITY OF ARIZONA   (United States)

^e VANDERBILT UNIVERSITY MEDICAL CENTER   (United States)

^f StemSynergy Therapeutics Inc   (United States)

^g HARVARD MEDICAL SCHOOL   (United States)

^h VANDERBILT INGRAM CANCER CENTER   (United States)

ⁱ UNIVERSITY OF MIAMI   (United States)

Author keywords

catenin; Axin; flavonoids; LRP6; Wnt signaling; Xenopus extracts

Indexed keywords

AXIN; BETA CATENIN; HYBRID PROTEIN; LOW DENSITY LIPOPROTEIN RECEPTOR RELATED PROTEIN 6; LUCIFERASE; WNT PROTEIN;

ARTICLE; CHEMICAL ANALYSIS; CONTROLLED STUDY; CYTOPLASM; EGG PARASITOID; EMBRYO; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; NONHUMAN; PRIORITY JOURNAL; PROTEIN ANALYSIS; REGULATORY MECHANISM; RENILLA; SIGNAL TRANSDUCTION; WILD TYPE; XENOPUS;

ANIMALS; AXIN PROTEIN; BETA CATENIN; ENZYME ASSAYS; FLAVONES; HEK293 CELLS; HELA CELLS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; LUCIFERASES; REPRODUCIBILITY OF RESULTS; SMALL MOLECULE LIBRARIES; WNT SIGNALING PATHWAY; XENOPUS LAEVIS;

MAMMALIA; RENILLA LUCIFERASE;

EID: 80053540932     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057111416657     Document Type: Article

References (55)

1. Nusse R. Wnt Signaling in Disease and in Development. Cell Res. 2005 ; 15: 28-32 (Pubitemid 41653961)
2. Clevers H. Wnt/Beta-Catenin Signaling in Development and Disease. Cell. 2006 ; 127: 469-480
3. Lee E., Salic A., Kruger R., Heinrich R., Kirschner M. W. The Roles of APC and Axin Derived from Experimental and Theoretical Analysis of the Wnt Pathway. PLoS. Biol. 2003 ; 1: E10
4. MacDonald B. T., Tamai K., He X. Wnt/Beta-Catenin Signaling: Components, Mechanisms, and Diseases. Dev. Cell. 2009 ; 17: 9-26
5. Amit S., Hatzubai A., Birman Y., Andersen J. S., Ben-Shushan E., Mann M., Ben-Neriah Y., Alkalay I. Axin-mediated CKI phosphorylation of beta-catenin at Ser 45: a molecular switch for the Wnt pathway. Genes Dev. 2002 ; 16: 1066-1076 (Pubitemid 34507196)
6. Liu C., Li Y., Semenov M., Han C., Baeg G. H., Tan Y., Zhang Z., Lin X., He X. Control of Beta-Catenin Phosphorylation/Degradation by a Dual-Kinase Mechanism. Cell. 2002 ; 108: 837-847 (Pubitemid 34327534)
7. Latres E., Chiaur D. S., Pagano M. The Human F Box Protein Beta-Trcp Associates with the Cul1/Skp1 Complex and Regulates the Stability of Beta-Catenin. Oncogene. 1999 ; 18: 849-854 (Pubitemid 29086261)
8. Yamamoto H., et al. Phosphorylation of Axin, a Wnt Signal Negative Regulator, by Glycogen Synthase Kinase-3beta Regulates Its Stability. J. Biol. Chem. 1999 ; 274: 10681-10684
9. Huang S. M., et al. Tankyrase Inhibition Stabilizes Axin and Antagonizes Wnt Signalling. Nature. 2009 ; 461: 614-620
10. De Robertis E. M. Spemann's Organizer and Self-Regulation in Amphibian Embryos. Nat. Rev. Mol. Cell Biol. 2006 ; 7: 296-302
11. Sokol S., Christian J. L., Moon R. T., Melton D. A. Injected Wnt RNA Induces a Complete Body Axis in Xenopus Embryos. Cell. 1991 ; 67: 741-752 (Pubitemid 121001487)
12. Kinzler K. W., et al. Identification of FAP Locus Genes from Chromosome 5q21. Science. 1991 ; 253: 661-665 (Pubitemid 21917199)
13. Heasman J., et al. Overexpression of Cadherins and Underexpression of Beta-Catenin Inhibit Dorsal Mesoderm Induction in Early Xenopus Embryos. Cell. 1994 ; 79: 791-803 (Pubitemid 24371970)
14. He X., Saint-Jeannet J. P., Woodgett J. R., Varmus H. E., Dawid I. B. Glycogen Synthase Kinase-3 and Dorsoventral Patterning in Xenopus Embryos. Nature. 1995 ; 374: 617-622
15. Niemann S., et al. Homozygous WNT3 Mutation Causes Tetra-Amelia in a Large Consanguineous Family. Am. J. Hum. Genet. 2004 ; 74: 558-563 (Pubitemid 38325926)
16. Boyden L. M., et al. High Bone Density due to a Mutation in LDL-Receptor-Related Protein 5. N. Engl. J. Med. 2002 ; 346: 1513-1521 (Pubitemid 34755690)
17. Gong Y., et al. LDL Receptor-Related Protein 5 (LRP5) Affects Bone Accrual and Eye Development. Cell. 2001 ; 107: 513-523 (Pubitemid 33152786)
18. Toomes C., et al. Mutations in LRP5 or FZD4 Underlie the Common Familial Exudative Vitreoretinopathy Locus on Chromosome 11q. Am. J. Hum. Genet. 2004 ; 74: 721-730 (Pubitemid 38420101)
19. Xu Q., et al. Vascular Development in the Retina and Inner Ear: Control by Norrin and Frizzled-4, a High-Affinity Ligand-Receptor Pair. Cell. 2004 ; 116: 883-895 (Pubitemid 38410732)
20. Lammi L., et al. Mutations in AXIN2 Cause Familial Tooth Agenesis and Predispose to Colorectal Cancer. Am. J. Hum. Genet. 2004 ; 74: 1043-1050 (Pubitemid 38568974)
21. Nusse R. Wnt Signaling and Stem Cell Control. Cell Res. 2008 ; 18: 523-527 (Pubitemid 351630946)
22. Cohen E. D., Tian Y., Morrisey E. E. Wnt Signaling: An Essential Regulator of Cardiovascular Differentiation, Morphogenesis and Progenitor Self-renewal. Development. 2008 ; 135: 789-798 (Pubitemid 351524132)
23. De Ferrari G. V., Moon R. T. The Ups and Downs of Wnt Signaling in Prevalent Neurological Disorders. Oncogene. 2006 ; 25: 7545-7553 (Pubitemid 44885754)
24. Welters H. J., Kulkarni R. N. Wnt Signaling: Relevance to Beta-Cell Biology and Diabetes. Trends Endocrinol. Metab. 2008 ; 19: 349-355
25. Kinzler K. W., Vogelstein B. Lessons from Hereditary Colorectal Cancer. Cell. 1996 ; 87: 159-170 (Pubitemid 26358996)
26. Klaus A., Birchmeier W. Wnt Signalling and Its Impact on Development and Cancer. Nat. Rev. Cancer. 2008 ; 8: 387-398 (Pubitemid 351589714)
27. Ma L., Cantley L. C., Janmey P. A., Kirschner M. W. Corequirement of Specific Phosphoinositides and Small GTP-Binding Protein Cdc42 in Inducing Actin Assembly in Xenopus Egg Extracts. J. Cell. Biol. 1998 ; 140: 1125-1136 (Pubitemid 28128872)
28. Theriot J. A., Rosenblatt J., Portnoy D. A., Goldschmidt-Clermont P. J., Mitchison T. J. Involvement of Profilin in the Actin-Based Motility of L. Monocytogenes in Cells and in Cell-Free Extracts. Cell. 1994 ; 76: 505-517 (Pubitemid 24064171)
29. Kornbluth S., Dasso M., Newport J. Evidence for a Dual Role for TC4 Protein in Regulating Nuclear Structure and Cell Cycle Progression. J. Cell Biol. 1994 ; 125: 705-719 (Pubitemid 24151168)
30. Blow J. J., Watson J. V. Nuclei Act as Independent and Integrated Units of Replication in a Xenopus Cell-Free DNA Replication System. EMBO. J. 1987 ; 6: 1997-2002
31. Gard D. L., Kirschner M. W. Microtubule Assembly in Cytoplasmic Extracts of Xenopus Oocytes and Eggs. J. Cell Biol. 1987 ; 105: 2191-2201
32. Murray A. W., Kirschner M. W. Cyclin Synthesis Drives the Early Embryonic Cell Cycle. Nature. 1989 ; 339: 275-280
33. Lupardus P. J., Byun T., Yee M. C., Hekmat-Nejad M., Cimprich K. A. A Requirement for Replication in Activation of the ATR-Dependent DNA Damage Checkpoint. Genes Dev. 2002 ; 16: 2327-2332 (Pubitemid 35034401)
34. Evans E. K., et al. Reaper-Induced Apoptosis in a Vertebrate System. EMBO. J. 1997 ; 16: 7372-7381 (Pubitemid 28010497)
35. Ivan M., et al. HIFalpha Targeted for VHL-Mediated Destruction by Proline Hydroxylation: Implications for O2 Sensing. Science. 2001 ; 292: 464-468 (Pubitemid 32335941)
36. Verma R., et al. Ubistatins Inhibit Proteasome-Dependent Degradation by Binding the Ubiquitin Chain. Science. 2004 ; 306: 117-120 (Pubitemid 39451952)
37. Peterson J. R., Lokey R. S., Mitchison T. J., Kirschner M. W. A Chemical Inhibitor of N-WASP Reveals a New Mechanism for Targeting Protein Interactions. Proc. Natl. Acad. Sci. U. S. A. 2001 ; 98: 10624-10629 (Pubitemid 32878671)
38. Wignall S. M., et al. Identification of a Novel Protein Regulating Microtubule Stability through a Chemical Approach. Chem. Biol. 2004 ; 11: 135-146 (Pubitemid 38203998)
39. Salic A., Lee E., Mayer L., Kirschner M. W. Control of Beta-Catenin Stability: Reconstitution of the Cytoplasmic Steps of the Wnt Pathway in Xenopus Egg Extracts. Mol. Cell. 2000 ; 5: 523-532
40. Salic A., King R. W. Identifying Small Molecule Inhibitors of the Ubiquitin-Proteasome Pathway in Xenopus Egg Extracts. Methods Enzymol. 2005 ; 399: 567-585 (Pubitemid 41772754)
41. Thorne C. A., et al. Small-Molecule Inhibition of Wnt Signaling through Activation of Casein Kinase 1alpha. Nat. Chem. Biol. 2010 ; 6: 829-836
42. Murray A. W. Cell Cycle Extracts. Methods Cell. Biol. 1991 ; 36: 581-605
43. Malo N., Hanley J. A., Cerquozzi S., Pelletier J., Nadon R. Statistical Practice in High-Throughput Screening Data Analysis. Nat. Biotechnol. 2006 ; 24: 167-175 (Pubitemid 43221699)
44. Tukey J. W. Contributions to Probability and Statistics. Olkin I., ed. Stanford, CA: Stanford University Press ; 1960 :
45. Peng H. B. Xenopus laevis: Practical Uses in Cell and Molecular Biology. Solutions and Protocols. Methods Cell. Biol. 1991 ; 36: 657-662
46. Naik S., Piwnica-Worms D. Real-Time Imaging of Beta-Catenin Dynamics in Cells and Living Mice. Proc. Natl. Acad. Sci. U. S. A. 2007 ; 104: 17465-17470 (Pubitemid 350219861)
47. Kofron M., et al. Wnt11/Beta-Catenin Signaling in Both Oocytes and Early Embryos Acts through LRP6-Mediated Regulation of Axin. Development. 2007 ; 134: 503-513 (Pubitemid 46332487)
48. King R. W., et al. A 20S Complex Containing CDC27 and CDC16 Catalyzes the Mitosis-Specific Conjugation of Ubiquitin to Cyclin B. Cell. 1995 ; 81: 279-288
49. Tukey J. W. Exploratory Data Analysis. Reading, MA: Addison-Wesley ; 1977 :
50. Chen B., et al. Small Molecule-Mediated Disruption of Wnt-Dependent Signaling in Tissue Regeneration and Cancer. Nat. Chem. Biol. 2009 ; 5: 100-107
51. Bafico A., Liu G., Goldin L., Harris V., Aaronson S. A. An Autocrine Mechanism for Constitutive Wnt Pathway Activation in Human Cancer Cells. Cancer Cell. 2004 ; 6: 497-506 (Pubitemid 39469985)
52. Lee J. H., Park C. H., Jung K. C., Rhee H. S., Yang C. H. Negative Regulation of Beta-Catenin/Tcf Signaling by Naringenin in AGS Gastric Cancer Cell. Biochem. Biophys. Res. Commun. 2005 ; 335: 771-776 (Pubitemid 41188265)
53. Park C. H., et al. Quercetin, a Potent Inhibitor against Beta-Catenin/Tcf Signaling in SW480 Colon Cancer Cells. Biochem. Biophys. Res. Commun. 2005 ; 328: 227-234 (Pubitemid 40164659)
54. Shukla S., et al. Blockade of Beta-Catenin Signaling by Plant Flavonoid Apigenin Suppresses Prostate Carcinogenesis in TRAMP Mice. Cancer Res. 2007 ; 67: 6925-6935 (Pubitemid 47105540)
55. Takebe N., Harris P. J., Warren R. Q., Ivy S. P. Targeting Cancer Stem Cells by Inhibiting Wnt, Notch, and Hedgehog Pathways. Nat. Rev. Clin. Oncol. 2011 ; 8: 97-106