Identification of RAS-mitogen-activated protein kinase signaling pathway modulators in an ERF1 Redistribution® screen

Journal of Biomolecular Screening

Volumn 11, Issue 4, 2006, Pages 423-434

  Grånäs, Charlotta ^a   Lundholt, Betina Kerstin ^a   Loechel, Frosty ^a   Pedersen, Hans Christian ^a   Bjørn, Sara Petersen ^a   Linde, Viggo ^a   Krogh Jensen, Christian ^a   Nielsen, Eva Maria Damsgaard ^a   Præstegaard, Morten ^a   Nielsen, Søren Jensby ^a  

^a BioImage AS   (Denmark)

Author keywords

High content; MAPK; Redistribution ; Screen

Indexed keywords

MITOGEN ACTIVATED PROTEIN KINASE; MITOGEN ACTIVATED PROTEIN KINASE KINASE; RAF PROTEIN; RAS PROTEIN;

AMINO ACID SEQUENCE; ANIMAL CELL; ARTICLE; ASSAY; CANCER CELL; CELL MEMBRANE PERMEABILITY; CELL PROLIFERATION; CONTROLLED STUDY; ENZYME ASSAY; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; MELANOMA CELL; NONHUMAN; NUCLEOTIDE SEQUENCE; PRIORITY JOURNAL;

ANIMALS; CELL LINE; CELL LINE, TUMOR; CELL PROLIFERATION; CRICETINAE; DNA-BINDING PROTEINS; DRUG EVALUATION, PRECLINICAL; HUMANS; MAP KINASE SIGNALING SYSTEM; MOLECULAR STRUCTURE; PHOSPHORYLATION; REPRESSOR PROTEINS; RNA, SMALL INTERFERING; TRANSCRIPTION FACTORS; TRANSFECTION;

EID: 33744936336     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057106287136     Document Type: Article

References (42)

1. Robinson MJ, Cobb MH: Mitogen-activated protein kinase pathways. Curr Opin Cell Biol 1997;9(2):180-186.
2. Downward J: Targeting RAS signalling pathways in cancer therapy. Nat Rev Cancer 2003;3(1):11-22.
3. Hilger RA, Scheulen ME, Strumberg D: The Ras-Raf-MEK-ERK pathway in the treatment of cancer. Onkologie 2002;25:511-518.
4. Davies H, Bignell GR, Cox C, Stephens P, Edkins S, Clegg S, et al: Mutations of the BRAF gene in human cancer. Nature 2002;417:949-954.
5. Marais R, Light Y, Paterson HF, Marshall CJ: Ras recruits Raf-1 to the plasma membrane for activation by tyrosine phosphorylation. Embo J 1995;14:3136-3145.
6. Reiser V, Ammerer G, Ruis H: Nucleocytoplasmic traffic of MAP kinases. Gene Expr 1999;7(4-6):247-254.
7. Whitehurst AW, Wilsbacher JL, You Y, Luby-Phelps K, Moore MS, Cobb MH: ERK2 enters the nucleus by a carrier-independent mechanism. Proc Natl Acad Sci USA 2002;99:7496-7501.
8. Whitehurst AW, Robinson FL, Moore MS, Cobb MH: The death effector domain protein PEA-15 prevents nuclear entry of ERK2 by inhibiting required interactions. J Biol Chem 2004;279:12840-12847. Epub 12004 Jan 12845.
9. Pruitt K, Der CJ: Ras and Rho regulation of the cell cycle and oncogenesis. Cancer Lett 2001;171(1):1-10.
10. Camps M, Nichols A, Arkinstall S: Dual specificity phosphatases: a gene family for control of MAP kinase function. Faseb J 2000;14(1):6-16.
11. Keyse SM: Protein phosphatases and the regulation of mitogen-activated protein kinase signalling. Curr Opin Cell Biol 2000;12(2):186-192.
12. Volmat V, Camps M, Arkinstall S, Pouyssegur J, Lenormand P: The nucleus, a site for signal termination by sequestration and inactivation of p42/p44 MAP kinases. J Cell Sci 2001;114(Pt 19):3433-3443.
13. Le Gallic L, Sgouras D, Beal G Jr, Mavrothalassitis G: Transcriptional repressor ERF is a Ras/mitogen-activated protein kinase target that regulates cellular proliferation. Mol Cell Biol 1999;19:4121-4133.
14. Mavrothalassitis G, Ghysdael J: Proteins of the ETS family with transcriptional repressor activity. Oncogene 2000;19:6524-6532.
15. Le Gallic L, Virgilio L, Cohen P, Biteau B, Mavrothalassitis G: ERF nuclear shuttling, a continuous monitor of Erk activity that links it to cell cycle progression. Mol Cell Biol 2004;24:1206-1218.
16. Zhang JH, Chung TD, Oldenburg KR: A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 1999;4:67-73.
17. Lundholt BK, Linde V, Loechel F, Pedersen HC, Moller S, Praestegaard M, et al: Identification of Akt pathway inhibitors using redistribution screening on the FLIPR and the IN Cell 3000 Analyzer. J Biomol Screen 2005;10(1):20-29.
18. Taparowsky E, Suard Y, Fasano O, Shimizu K, Goldfarb M, Wigler M: Activation of the T24 bladder carcinoma transforming gene is linked to a single amino acid change. Nature 1982;300:762-765.
19. Favata MF, Horiuchi KY, Manos EJ, Daulerio AJ, Stradley DA, Feeser WS, et al: Identification of a novel inhibitor of mitogen-activated protein kinase kinase. J Biol Chem 1998;273:18623-18632.
20. Lipinski CA, Lombardo F, Dominy BW, Feeney PJ: Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev 2001;46(1-3):3-26.
21. Almholt DL, Loechel F, Nielsen SJ, Krog-Jensen C, Terry R, Bjorn SP, et al: Nuclear export inhibitors and kinase inhibitors identified using a MAPK-activated protein kinase 2 redistribution screen. Assay Drug Dev Technol 2004;2(1):7-20.
22. Meissner T, Krause E, Vinkemeier U: Ratjadone and leptomycin B block CRM1-dependent nuclear export by identical mechanisms. FEBS Lett 2004;576(1-2):27-30.
23. Karasarides M, Chiloeches A, Hayward R, Niculescu-Duvaz D, Scanlon I, Friedlos F, et al: B-RAF is a therapeutic target in melanoma. Oncogene 2004;21:21.
24. Davies SP, Reddy H, Caivano M, Cohen P: Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J 2000;351(Pt 1):95-105.
25. Crabtree GR, Olson EN: NFAT signaling: choreographing the social lives of cells. Cell 2002;109(Suppl):S67-S79.
26. Darnell JE Jr: Transcription factors as targets for cancer therapy. Nat Rev Cancer 2002;2:740-749.
27. Torrance CJ, Agrawal V, Vogelstein B, Kinzler KW: Use of isogenic human cancer cells for high-throughput screening and drug discovery. Nat Biotechnol 2001;19:940-945.
28. Weinstein-Oppenheimer CR, Blalock WL, Steelman LS, Chang F, McCubrey JA: The Raf signal transduction cascade as a target for chemotherapeutic intervention in growth factor-responsive tumors. Pharmacol Ther 2000;88(3):229-279.
29. Sebti SM: Blocked pathways: FTIs shut down oncogene signals. Oncologist 2003;8(Suppl 3):30-38.
30. Zhang YA, Nemunaitis J, Scanlon KJ, Tong AW: Anti-tumorigenic effect of a K-ras ribozyme against human lung cancer cell line heterotransplants in nude mice. Gene Ther 2000;7:2041-2050.
31. Perry DA, Narla RK, Navara CS, Uckun FM: Ras endoprotease inhibitors are potent antileukemic agents. Clin Cancer Res 1999;5(11 Suppl): 3789S.
32. End DW, Smets G, Todd AV, Applegate TL, Fuery CJ, Angibaud P, et al: Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro. Cancer Res 2001;61(1):131-137.
33. Kato-Stankiewicz J, Guo L, Paulmurugan R, Gambhir SS, Khazak V, Golemis EA, et al: The small molecule compound, MCP1, inhibits Ras-Raf interaction in mammalian cells and induces apoptosis in various hematopoietic cancer cells [abstract 5627]. Proc Am Assoc Cancer Res 2004;45.
34. Lackner MR, Kindt RM, Carroll PM, Brown K, Cancilla MR, Chen C, et al: Chemical genetics identifies Rab geranylgeranyl transferase as an apoptotic target of farnesyl transferase inhibitors. Cancer Cell 2005;7:325-336.
35. Hilger RA, Kredke S, Hedley D, Moeller JG, Bauer RJ, Stellberg W, et al: ERK1/2 phosphorylation: a biomarker analysis within a phase I study with the new Raf kinase inhibitor BAY43-9006. Int J Clin Pharmacol Ther 2002;40:567-568.
36. Wilhelm SM, Carter C, Tang L, Wilkie D, McNabola A, Rong H, et al: BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res 2004;64:7099-7109.
37. O'Dwyer PJ, Rosen M, Gallagher M, Schwartz B, Flaherty KT: Pharmacodynamic study of BAY 43-9006 in patients with metastatic renal cell carcinoma [abstract 3005]. Proc Am Soc Clin Oncol 2005;24.
38. Rudin CM, Marshall JL, Huang CH, Kindler HL, Zhang C, Kumar D, et al: Delivery of a liposomal c-raf-1 antisense oligonucleotide by weekly bolus dosing in patients with advanced solid tumors: a phase I study. Clin Cancer Res 2004;10:7244-7251.
39. Allen LF, Sebolt-Leopold J, Meyer MB: CI-1040 (PD184352), a targeted signal transduction inhibitor of MEK (MAPKK). Semin Oncol 2003;30 (5 Suppl 16):105-116.
40. Lorusso P, Krishnamurthi S, Rinehart JR, Nabell L, Croghan G, Varterasian M, et al: A phase 1-2 clinical study of a second generation oral MEK inhibitor, PD 0325901 in patients with advanced cancer [abstract 3011]. Proc Am Soc Clin Oncol 2005;24.
41. Sebolt-Leopold JS, Herrera R: Targeting the mitogen-activated protein kinase cascade to treat cancer. Nat Rev Cancer 2004;4:937-947.
42. Kau TR, Schroeder F, Ramaswamy S, Wojciechowski CL, Zhao JJ, Roberts TM, et al: A chemical genetic screen identifies inhibitors of regulated nuclear export of a Forkhead transcription factor in PTEN-deficient tumor cells. Cancer Cell 2003;4:463-476.