Use of red-shifted dyes in a fluorescence polarization AKT kinase assay for detection of biological activity in natural product extracts

Journal of Biomolecular Screening

Volumn 9, Issue 1, 2004, Pages 52-61

  Turek Etienne, Tammy C ^a   Lei, Ming ^a   Terracciano, Joseph S ^a   Langsdorf, Erik F ^a   Bryant, Robert W ^a   Hart, Richard F ^a   Horan, Ann C ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Fluorescence polarization; Kinase assay; Natural product extracts; Red shifted Cy dyes

Indexed keywords

ADENOSINE TRIPHOSPHATE; ANTINEOPLASTIC AGENT; BRYOSTATIN 1; CARBAZOLE DERIVATIVE; DACTINOMYCIN; DOXORUBICIN; EPOTHILONE A; EPOTHILONE B; FLUORESCENT DYE; IMATINIB; INDOLOCARBAZOLE; NATURAL PRODUCT; PACLITAXEL; PROTEIN KINASE B; STAUROSPORINE; TENIPOSIDE; UNCLASSIFIED DRUG; VINBLASTINE; BIOLOGICAL FACTOR; ONCOPROTEIN; PROTEIN SERINE THREONINE KINASE;

ACCURACY; ACTINOBACTERIA; ARTICLE; BACTERIUM CULTURE; CONCENTRATION (PARAMETERS); DRUG SCREENING; FLUORESCENCE POLARIZATION; PRIORITY JOURNAL; CHEMISTRY; FERMENTATION; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; METABOLISM; METHODOLOGY; ULTRAVIOLET SPECTROPHOTOMETRY;

ACTINOBACTERIA (CLASS);

BIOLOGICAL FACTORS; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; FERMENTATION; FLUORESCENCE POLARIZATION; FLUORESCENT DYES; PROTEIN-SERINE-THREONINE KINASES; PROTO-ONCOGENE PROTEINS; PROTO-ONCOGENE PROTEINS C-AKT; SPECTROPHOTOMETRY, ULTRAVIOLET;

EID: 2442521478     PISSN: 10870571     EISSN: None     Source Type: Journal    
DOI: 10.1177/1087057103259346     Document Type: Article

References (39)

1. Fabbro D, Garcia-Echeverria C: Targeting protein kinases in cancer therapy. Curr Opin Drug Discov Dev 2002;5:701-712.
2. Orchard S: Kinases as targets: prospects for chronic therapy. Curr Opin Drug Discov Dev 2002;5:713-717.
3. Traxler P, Bold G, Buchdunger E, Caravatti G, Furet P, Manley P, et al: Tyrosine kinase inhibitors: from rational design to clinical trials. Med Res Rev 2001;21:499-512.
4. Hernandez-Boluda J, Cervantes F: Imatinib mesylate (Gleeve/Glivec): a new therapy for chronic myeloid leukemia and other malignancies. Drugs Today 2002;38:601-613.
5. Zimmermann J: Glivec: a new treatment modality for CML: a case history. Chimia 2002;56:428-431.
6. Brazil DP, Park J, Hemmings BA: PKB binding proteins: getting in on the AKT. Cell 2002;111:293-303.
7. Kandel ES, Hay N: The regulation and activities of the multifunctional serine/ threonine kinase AKT/PKB. Exp Cell Res 1999;253:210-229.
8. Blume-Jensen P, Hunter T: Oncogenic kinase signalling. Nature 2001;411:355-365.
9. Datta SR, Brunet A, Greenberg ME: Cellular survival: a play in three AKTs. Genes Dev 1999;13:2905-2927.
10. Datta SR, Dudek H, Tao X, Master S, Fu H, Gotoh Y, et al: AKT phosphorylation of BAD couples survival signals to the cell-intrinsic death machinery. Cell 1997;91:231-241.
11. Kim AH, Khursigara G, Sun X, Franke TF, Chao MV: AKT phosphorylates and negatively regulates apoptosis signal-regulating kinase 1. Mol Cell Biol 2001;21:893-901.
12. Lee M-J, Thangada S, Paik J-H, Sapkota GP, Ancellin N, Chae S-S, et al: AKT-mediated phosphorylation of the G protein-coupled receptor EDG-1 is required for endothelial cell chemotaxis. Mol Cell 2001;8:693-704.
13. Cheng J, Ruggeri B, Klein W, Sonoda G, Altomare D, Watson D, et al: Amplification of AKT2 in human pancreatic cancer cells and inhibition of AKT2 expression and tumorigenicity by antisense RNA. Proc Natl Acad Sci USA 1996;93:3636-3641.
14. Chun K-H, Kosmeder JW, Sun S, Pezzuto JM, Lotan R, Hong WK, et al: Effects of deguelin on the phosphatidylinositol 3-kinase/AKT pathway and apoptosis in premalignant human bronchial epithelial cells. J Natl Cancer Inst 2003;95:291-302.
15. Nakatani K, Thompson DA, Barthel A, Sakaue H, Liu W, Weigel RJ, et al: Up-regulation of AKT3 in estrogen receptor-deficient breast cancers and androgen-independent prostate cancer lines. J Biol Chem 1999;274:21528-21532.
16. Cragg GM, Newman DJ, Snader KM: Natural products in drug discovery and development. J Nat Prod 1997;60:52-60.
17. Shu Y-Z: Recent natural products based drug development: a pharmaceutical industry perspective. J Nat Prod 1998;61:1053-1071.
18. Mann J: Natural products in cancer chemotherapy: past, present and future. Nat Rev Cancer 2002;2:143-148.
19. Henkel T, Brunne RM, Muller H, Reichel F: Statistical investigation into the structure complementarity of natural products and synthetic compounds. Angew Chem Int Ed 1999;38:643-647.
20. Frormann S, Jas G: Natural products and combinatorial chemistry-the comeback of nature in drug discovery. Business Briefing: Future Drug Discov 2002;84-90.
21. Bindseil KU, Jakupovic J, Wolf D, Lavayre J, Leboul J, van der Pyl D: Pure compound libraries: a new perspective for natural product based drug discovery. Drug Discov Today 2001;6:840-847.
22. Eldridge GR, Vervoort HC, Lee CM, Cremin PA, Williams CT, Hart SM, et al: High-throughput method for the production and analysis of large natural product libraries for drug discovery. Anal Chem 2002;74:3963-3971.
23. Harvey A: Strategies for discovering drugs from previously unexplored natural products. Drug Discov Today 2000;5:294-300.
24. Seethala R, Menzel R: A homogeneous, fluorescence polarization assay for src-family tyrosine kinases. Anal Biochem 1997;253:210-218.
25. Seethala R, Menzel R: A fluorescence polarization competition immunoassay for tyrosine kinases. Anal Biochem 1998;255:257-262.
26. Deshpande SS, Mineyev I, Owicki JC: A robust, versatile tyrosine kinase assay for HTS in drug discovery. Prog Biomed Optics (SPIE) 1999;3603:251-261.
27. Wu JJ, Yarwood DR, Pham Q, Sills MA: Identification of a high-affinity antiphosphoserine antibody for the development of a homogeneous fluorescence polarization assay of protein kinase c. J Biomol Screen 2000;5:23-30.
28. Parker GJ, Law TL, Lenoch FJ, Bolger RE: Development of high throughput screening assays using fluorescence polarization: nuclear receptor-ligand- binding and kinase*/phosphatase assays. J Biomol Screen 2000;5:77-88.
29. Turek TC, Small EC, Bryant RW, Hill AGW: Development and validation of a competitive AKT serine/threonine kinase fluorescence polarization assay using a product-specific anti-phospho-serine antibody. Anal Biochem 2001;299:45-53.
30. Sills MA, Weiss D, Pham Q, Schweitzer R, Wu X, Wu JJ: Comparison of assay technologies for a tyrosine kinase assay generates different results in high-throughput screening. J Biomol Screen 2002;7:191-214.
31. Turek-Etienne TC, Small EC, Soh SC, Xin TA, Gaitonde PV, Barrabee EB, et al: Evaluation of fluorescent compound interference in 4 fluorescence polarization assays: 2 kinases, 1 protease, and 1 phosphatase. J Biomol Screen 2003;8:176-184.
32. McDonald OB, Chen WJ, Ellis B, Hoffman C, Overton L, Rink M, et al: A scintillation proximity assay for the Raf/MEK/ERK kinase cascade: high-throughput screening and identification of selective enzyme inhibitors. Anal Biochem 1999;268:318-329.
33. Park Y-W, Cummings RT, Wu L, Zheng S, Cameron PM, Woods A, et al: Homogeneous proximity tyrosine kinase assays: scintillation proximity assay versus homogeneous time-resolved fluorescence. Anal Biochem 1999;269:94-104.
34. Ohmi N, Wingfield JM, Yazawa H, Inagaki O: Development of a homogeneous time-resolved fluorescence assay for high throughput screening to identify Lck inhibitors: comparison with scintillation proximity assay and streptavidin-coated plate assay. J Biomol Screen 2000;5:463-470.
35. Earnshaw DL, Pope AJ: FlashPlate scintillation proximity assays for characterization and screening of DNA polymerase, primase, and helicase activities. J Biomol Screen 2001;6:39-46.
36. Kolb AJ, Kaplita PV, Hayes DJ, Park Y-W, Pernell C, Major JS, et al: Tyrosine kinase assays adapted to homogeneous time-resolved fluorescence. Drug Discov Today 1998;3:333-342.
37. Bader B, Butt E, Palmetshofer A, Walter U, Jarchau T, Drueckes P: A cGMP-dependent protein kinase assay for high throughput screening based on time-resolved fluorescence resonance energy transfer. J Biomol Screen 2001;6:255-264.
38. Kumar CC, Diao R, Yin Z, Liu Y-H, Samatar AA, Madison V, et al: Expression, purification, characterization and homology modeling of active AKT/PKB, a key enzyme involved in cell survival signaling. Biochim Biophys Acta 2001;1526:257-268.
39. Matson JA, Claridge C, Bush JA, Titus J, Bradner WT, Doyle TW, et al: AT2433-A1, AT2433-A2, AT2433-B1, and AT2433-B2 novel antitumor antibiotic compounds produced by Actinomadura melliaura: taxonomy, fermentation, isolation and biological properties. J Antibiot 1989;42:1547-1555.