Platforms for high-throughput screening of Wnt/Frizzled antagonists

Drug Discovery Today

Volumn 17, Issue 23-24, 2012, Pages 1316-1322

  Koval, Alexey ^a   Katanaev, Vladimir L ^a,b  

^a UNIVERSITY OF LAUSANNE   (Switzerland)

^b INSTITUTE OF PROTEIN RESEARCH   (Russian Federation)

Author keywords

[No Author keywords available]

Indexed keywords

ADENYLATE CYCLASE; ANTINEOPLASTIC AGENT; BETA CATENIN; CALCIUM; FRIZZLED PROTEIN; G PROTEIN COUPLED RECEPTOR; GUANOSINE TRIPHOSPHATE; PROTEIN INHIBITOR; UNCLASSIFIED DRUG; WNT FZD ANTAGONIST; WNT PROTEIN; XAV 939;

ANTINEOPLASTIC ACTIVITY; BINDING SITE; CALCIUM SIGNALING; COMPLEX FORMATION; DIMERIZATION; DRUG DESIGN; DRUG PROTEIN BINDING; DRUG SCREENING; GENE EXPRESSION; GENETIC TRANSCRIPTION; HIGH THROUGHPUT SCREENING; HUMAN; LIGAND BINDING; NONHUMAN; PROMOTER REGION; PROTEIN PROTEIN INTERACTION; PROTEIN TARGETING; REVIEW; SIGNAL TRANSDUCTION;

ANIMALS; DRUG DISCOVERY; FRIZZLED RECEPTORS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; LIGANDS; PROTEIN BINDING; SIGNAL TRANSDUCTION; WNT PROTEINS;

EID: 84870326949     PISSN: 13596446     EISSN: 18785832     Source Type: Journal    
DOI: 10.1016/j.drudis.2012.07.007     Document Type: Review

References (79)

1. C.Y. Logan, and R. Nusse The Wnt signaling pathway in development and disease Annu. Rev. Cell Dev. Biol. 20 2004 781 810 (Pubitemid 39488658)
2. C.V. Cabrera Phenocopies induced with antisense RNA identify the wingless gene Cell 50 4 1987 659 663
3. F. Rijsewijk The Drosophila homolog of the mouse mammary oncogene int-1 is identical to the segment polarity gene wingless Cell 50 1987 649 657
4. C.R. Vinson A Drosophila tissue polarity locus encodes a protein containing seven potential transmembrane domains Nature 338 1989 263 264
5. C.C. Malbon G proteins in development Nat. Rev. Mol. Cell Biol. 6 2005 689 701 (Pubitemid 41742793)
6. D. Egger-Adam, and V.L. Katanaev Trimeric G protein-dependent signaling by Frizzled receptors in animal development Front. Biosci. 13 2008 4740 4755 (Pubitemid 351589194)
7. G. Schulte International Union of Basic and Clinical Pharmacology. LXXX. The class Frizzled receptors Pharmacol. Rev. 62 2010 632 667
8. V. Budnik, and P.C. Salinas Wnt signaling during synaptic development and plasticity Curr. Opin. Neurobiol. 21 2011 151 159
9. J. Zhao Tipping the balance: modulating the Wnt pathway for tissue repair Trends Biotechnol. 27 2009 131 136
10. V.A. van de Schans The Wnt/frizzled pathway in cardiovascular development and disease: friend or foe? Eur. J. Pharmacol. 585 2008 338 345
11. N. Barker, and H. Clevers Mining the Wnt pathway for cancer therapeutics Nat. Rev. Drug Discov. 5 2006 997 1014 (Pubitemid 44835127)
12. P. Polakis Wnt signaling in cancer Cold Spring Harb. Perspect. Biol. 14 2012 1837 1851 10.1101/cshperspect.a008052
13. R.H. Giles Caught up in a Wnt storm: Wnt signaling in cancer Biochim. Biophys. Acta 1653 2003 1 24 (Pubitemid 36627817)
14. G. Turashvili Wnt signaling pathway in mammary gland development and carcinogenesis Pathobiology 73 2006 213 223 (Pubitemid 46332829)
15. T.D. King The Wnt/beta-catenin signaling pathway: a potential therapeutic target in the treatment of triple negative breast cancer J. Cell. Biochem. 113 2012 13 18
16. J.R. Jessen Noncanonical Wnt signaling in tumor progression and metastasis Zebrafish 6 2009 21 28
17. H.J. Lee Inhibiting the Wnt signaling pathway with small molecules K.H. Goss, M. Kahn, Targeting the Wnt Pathway in Cancer 2011 Springer New York 183 209
18. W. Chen Development of small molecules targeting the Wnt pathway for the treatment of colon cancer: a high-throughput screening approach Am. J. Physiol. Gastrointest. Liver Physiol. 299 2010 G293 G300
19. M. Simons, and M. Mlodzik Planar cell polarity signaling: from fly development to human disease Annu. Rev. Genet. 42 2008 517 540
20. V.L. Katanaev, and A. Tomlinson Multiple roles of a trimeric G protein in Drosophila cell polarization Cell Cycle 5 2006 2464 2472 (Pubitemid 44785823)
21. P. Lapebie Dissecting the PCP pathway: one or more pathways?: Does a separate Wnt-Fz-Rho pathway drive morphogenesis? Bioessays 33 2011 759 768
22. V. Purvanov A direct and functional interaction between Go and Rab5 during G protein-coupled receptor signaling Sci. Signal. 3 136 2010 ra65
23. C.M. Freisinger Calcium dynamics integrated into signalling pathways that influence vertebrate axial patterning Philos. Trans. R. Soc. Lond. B: Biol. Sci. 363 2008 1377 1385 (Pubitemid 351311839)
24. R. van Amerongen, and R. Nusse Towards an integrated view of Wnt signaling in development Development 136 2009 3205 3214
25. M. Katoh, and M. Katoh WNT signaling pathway and stem cell signaling network Clin. Cancer Res. 13 2007 4042 4045 (Pubitemid 47105963)
26. C. Gao, and Y.G. Chen Dishevelled: the hub of Wnt signaling Cell. Signal. 22 2010 717 727
27. F. Verkaar, and G.J.R. Zaman New avenues to target Wnt/β-catenin signaling Drug Discov. Today 16 2011 35 41
28. S.M. Huang Tankyrase inhibition stabilizes Axin and antagonizes Wnt signalling Nature 461 2009 614 620
29. J.A. Low, and F.J. de Sauvage Clinical experience with Hedgehog pathway inhibitors J. Clin. Oncol. 28 2010 5321 5326
30. B.K. Atwood Expression of G protein-coupled receptors and related proteins in HEK293, AtT20 BV2, and N18 cell lines as revealed by microarray analysis BMC Genomics 12 2011 14
31. C. Liu, and X. He Destruction of a destructor: a new avenue for cancer therapeutics targeting the Wnt pathway J. Mol. Cell. Biol. 2 2010 70 73
32. M. Lepourcelet Small-molecule antagonists of the oncogenic Tcf/beta-catenin protein complex Cancer Cell 5 2004 91 102 (Pubitemid 38121599)
33. Y. Wang Wnt/Planar cell polarity signaling: a new paradigm for cancer therapy Mol. Cancer Ther. 8 2009 2103 2109
34. H. Suzuki Epigenetic inactivation of SFRP genes allows constitutive WNT signaling in colorectal cancer Nat. Genet. 36 2004 417 422 (Pubitemid 38437267)
35. B. He Blockade of Wnt-1 signaling induces apoptosis in human colorectal cancer cells containing downstream mutations Oncogene 24 2005 3054 3058 (Pubitemid 40675537)
36. D.B. Bylund, and M.L. Toews Radioligand binding methods: practical guide and tips Am. J. Physiol. 265 5 Pt 1 1993 L421 L429
37. A. Safholm A formylated hexapeptide ligand mimics the ability of Wnt-5a to impair migration of human breast epithelial cells J. Biol. Chem. 281 2006 2740 2749 (Pubitemid 43845737)
38. K. Kajiwara A synthetic peptide corresponding to residues 301-320 of human Wnt-1 promotes PC12 cell adhesion and hippocampal neural stem cell differentiation Peptides 29 2008 1479 1485
39. A. Blagodatski, and V.L. Katanaev Technologies of directed protein evolution in vivo Cell. Mol. Life Sci. 68 2011 1207 1214
40. C.H. Wu, and R. Nusse Ligand receptor interactions in the Wnt signaling pathway in Drosophila J. Biol. Chem. 277 2002 41762 41769 (Pubitemid 35257485)
41. C.M. Chen Evidence that the cysteine-rich domain of Drosophila Frizzled family receptors is dispensable for transducing Wingless Proc. Natl. Acad. Sci. U.S.A. 101 2004 15961 15966
42. R.M. Eglen Emerging concepts of guanine nucleotide-binding protein-coupled receptor (GPCR) function and implications for high throughput screening ASSAY Drug Dev. Technol. 5 2007 425 452
43. A. Koval Yellow submarine of the Wnt/Frizzled signaling: submerging from the G protein harbor to the targets Biochem. Pharmacol. 82 2011 1311 1319
44. V.L. Katanaev Trimeric G protein-dependent frizzled signaling in Drosophila Cell 120 2005 111 122 (Pubitemid 40094607)
45. T. Liu G protein signaling from activated rat frizzled-1 to the beta-catenin-Lef-Tcf pathway Science 292 2001 1718 1722 (Pubitemid 32506245)
46. D.S. Bredt A simple, sensitive, and specific radioreceptor assay for inositol 1,4,5-trisphosphate in biological tissues Biochem. Biophys. Res. Commun. 159 1989 976 982 (Pubitemid 19101078)
47. K. Liu Comparison on functional assays for Gq-coupled GPCRs by measuring inositol monophospate-1 and intracellular calcium in 1536-well plate format Curr. Chem. Genomics 1 2008 70 71
48. A. Takahashi Measurement of intracellular calcium Physiol. Rev. 79 1999 1089 1125 (Pubitemid 29473312)
49. D.C. Slusarski Interaction of Wnt and a Frizzled homologue triggers G-protein-linked phosphatidylinositol signalling Nature 390 1997 410 413 (Pubitemid 28027323)
50. A. Koval, and V.L. Katanaev Wnt3a stimulation elicits G-protein-coupled receptor properties of mammalian Frizzled proteins Biochem. J. 433 2011 435 440
51. M.B. Kilander WNT-5A stimulates the GDP/GTP exchange at pertussis toxin-sensitive heterotrimeric G proteins Cell. Signal. 23 2011 550 554
52. K.K. Jernigan Gbetagamma activates GSK3 to promote LRP6-mediated beta-catenin transcriptional activity Sci. Signal. 3 2010 ra37
53. M.B.C. Kilander Recombinant WNTs differentially activate β-catenin-dependent and -independent signalling in mouse microglia-like cells Acta Physiol. 203 2011 363 372
54. J. von Maltzahn Wnt7a-Fzd7 signalling directly activates the Akt/mTOR anabolic growth pathway in skeletal muscle Nat. Cell Biol. 14 2012 186 191
55. J.B. Regard Wnt/beta-catenin signaling is differentially regulated by Galpha proteins and contributes to fibrous dysplasia Proc. Natl. Acad. Sci. U.S.A. 108 2011 20101 20106
56. C. Hansen Wnt-5a-induced phosphorylation of DARPP-32 inhibits breast cancer cell migration in a CREB-dependent manner J. Biol. Chem. 284 2009 27533 27543
57. P.A. Insel, and R.S. Ostrom Forskolin as a tool for examining adenylyl cyclase expression, regulation, and G protein signaling Cell. Mol. Neurobiol. 23 2003 305 314 (Pubitemid 36676277)
58. C. Williams cAMP detection methods in HTS: selecting the best from the rest Nat. Rev. Drug Discov. 3 2004 125 135 (Pubitemid 38239774)
59. S. Titus Quantitative high-throughput screening using a live-cell cAMP assay identifies small-molecule agonists of the TSH receptor J. Biomol. Screen. 13 2008 120 127 (Pubitemid 351248693)
60. M. Bickle The beautiful cell: high-content screening in drug discovery Anal. Bioanal. Chem. 398 2010 219 226
61. R. Zhang, and X. Xie Tools for GPCR drug discovery Acta Pharmacol. Sin. 33 2012 372 384
62. G. Schulte beta-Arrestins - scaffolds and signalling elements essential for WNT/Frizzled signalling pathways? Br. J. Pharmacol. 159 2010 1051 1058
63. D. Calebiro Imaging of persistent cAMP signaling by internalized G protein-coupled receptors J. Mol. Endocrinol. 45 2010 1 8
64. M. Chen The anti-helminthic niclosamide inhibits Wnt/Frizzled1 signaling Biochemistry 48 2009 10267 10274
65. A. Heding Use of the BRET 7TM receptor/beta-arrestin assay in drug discovery and screening Expert Rev. Mol. Diagn. 4 2004 403 411 (Pubitemid 38684715)
66. W. Chen Dishevelled 2 recruits beta-arrestin 2 to mediate Wnt5A-stimulated endocytosis of Frizzled 4 Science 301 2003 1391 1394 (Pubitemid 37075817)
67. V. Bryja Beta-arrestin is a necessary component of Wnt/beta-catenin signaling in vitro and in vivo Proc. Natl. Acad. Sci. U.S.A. 104 2007 6690 6695 (Pubitemid 47175562)
68. N. Fujii An antagonist of Dishevelled protein-protein interaction suppresses beta-catenin-dependent tumor cell growth Cancer Res. 67 2007 573 579 (Pubitemid 46192194)
69. C. Carron Frizzled receptor dimerization is sufficient to activate the Wnt/β-catenin pathway J. Cell Sci. 116 2003 2541 2550 (Pubitemid 36790135)
70. A.A. Kaczor, and J. Selent Oligomerization of g protein-coupled receptors: biochemical and biophysical methods Curr. Med. Chem. 18 2011 4606 4634
71. Katanaev, V. and Büstorf, S. (2009) Frizzled Proteins are bona fide G Protein-Coupled Receptors. Available from Nature Precedings http://hdl.handle.net/10101/npre.2009.2765.1
72. V. Katanaev US8119354: Cell-Free Assay Product and Method of Use Thereof for Measuring Activity of Frizzled Receptors 2012 Universitaet Konstanz Constance, Germany
73. H. Frang Nonradioactive GTP binding assay to monitor activation of G protein-coupled receptors ASSAY Drug Dev. Technol. 1 2003 275 280
74. D.P. McEwen Fluorescent BODIPY-GTP analogs: real-time measurement of nucleotide binding to G proteins Anal. Biochem. 291 2001 109 117 (Pubitemid 32324531)
75. A. Koval Europium-labeled GTP as a general nonradioactive substitute for [35S]GTPγS in high-throughput G protein studies Anal. Biochem. 397 2010 202 207
76. F. Mancia, and W.A. Hendrickson Expression of recombinant G-protein coupled receptors for structural biology Mol. Biosyst. 3 2007 723 734 (Pubitemid 47449626)
77. C. Klammt Cell-free production of G protein-coupled receptors for functional and structural studies J. Struct. Biol. 158 2007 482 493 (Pubitemid 46764576)
78. G. Milligan Novel pharmacological applications of G-protein-coupled receptor-G protein fusions Curr. Opin. Pharmacol. 7 2007 521 526 (Pubitemid 47560218)
79. L. Ring Reporter gene HEK 293 cells and WNT/Frizzled fusion proteins as tools to study WNT signaling pathways Biol. Chem. 392 2011 1011 1020