Development and Implementation of Three Mitogen-Activated Protein Kinase (MAPK) Signaling Pathway Imaging Assays to Provide MAPK Module Selectivity Profiling for Kinase Inhibitors: MK2-EGFP Translocation, c-Jun, and ERK Activation

Methods in Enzymology

Volumn 414, Issue , 2006, Pages 389-418

  Nickischer, Debra ^a   Laethem, Carmen ^a   Trask Jr , Oscar J ^a   Williams, Rhonda Gates ^a   Kandasamy, Ramani ^a   Johnston, Patricia A ^a   Johnston, Paul A ^a  

^a NONE

Author keywords

[No Author keywords available]

Indexed keywords

1,4 DIAMINO 1,4 BIS(2 AMINOPHENYLTHIO) 2,3 DICYANOBUTADIENE; 2 (2 AMINO 3 METHOXYPHENYL)CHROMONE; 5 (2,6 DICHLOROPHENYL) 2 (2,4 DIFLUOROPHENYLTHIO)PYRIMIDO[1,6 B]PYRIDAZIN 6 ONE; ADENOSINE TRIPHOSPHATE; ANTHRA[1,9 CD]PYRAZOL 6(2H) ONE; MITOGEN ACTIVATED PROTEIN KINASE; MITOGEN ACTIVATED PROTEIN KINASE P38; PHOSPHOTRANSFERASE INHIBITOR; SB 242235; STAUROSPORINE; STRESS ACTIVATED PROTEIN KINASE; UNCLASSIFIED DRUG; WORTMANNIN;

CELL STRUCTURE; CYTOTOXICITY; DEVELOPMENT; DRUG SCREENING; ENZYME INHIBITION; HUMAN; IC 50; IMAGING SYSTEM; PRIORITY JOURNAL; REVIEW;

EID: 33750797845     PISSN: 00766879     EISSN: None     Source Type: Book Series    
DOI: 10.1016/S0076-6879(06)14022-7     Document Type: Chapter

References (14)

1. Almholt D.L., Loechel F., Nielsen S.J., Krog-Jensen C., Terry R., Bjorn S.P., Pedersen H.C., Praestegaard M., Moller S., Heide M., Pagliaro L., Mason A.J., Butcher S., and Dahl S.W. Nuclear export inhibitors and kinase inhibitors identified using a MAPK-activated protein kinase 2 redistribution screen. Assay Drug Dev. Technol. 2 (2004) 7-20
2. Cowan K.J., and Storey K.B. Mitogen-activated protein kinases: New signaling pathways functioning in cellular responses to environmental stress. J. Exp. Biol. 206 (2003) 1107-1115
3. English J.M., and Cobb M.H. Pharmacological inhibitors of MAPK pathways. Trends Pharmacol. Sci. 23 (2002) 40-45
4. Fabbro D., Ruetz S., Buchdunger E., Cowan-Jacob S.W., Fendrich G., Liebetanz J., Mestan J., O'Reilly T., Traxler P., Chaudhuri B., Fretz H., Zimmermann J., Meyer T., Caravatti G., Furet P., and Manley P.W. Protein kinases as targets for anticancer agents: From inhibitors to useful drugs. Pharmacol. Ther. 93 (2002) 79-98
5. Garrington T.P., and Johnson G.L. Organization and regulation of mitogen activated protein kinase signaling pathways. Curr. Opin. Cell Biol. 11 (1999) 211-218
6. Giuliano K.A., DeBiasio R.L., Dunlay R.T., Gough A., Volosky J.M., Zock J., Pavlakis G.N., and Taylor D.L. High-content screening: A new approach to easing key bottlenecks in the drug discovery process. J. Biomol. Screen. 2 (1997) 249-259
7. Johnson G.L., and Lapadat R. Mitogen-activated protein kinase pathways mediated by ERK, JNK and p38 protein kinases. Science 298 (2002) 1911-1912
8. Mitchison T.J. Small-molecule screening and profiling by using automated microscopy. Chembiochem. 6 (2005) 33-39
9. Noble M.E.M., Endicott J.A., and Johnson L.N. Protein kinase inhibitors: Insights into drug design and structure. Science 303 (2004) 1800-1805
10. Ono K., and Han J. The p38 signal transduction pathway, activation and function. Cell. Signal. 12 (2000) 1-13
11. Regan J., Breitfelder S., Cirillo P., Gilmore T., Graham A.G., Hickey E., Klaus B., Madwed J., Moriak M., Moss N., Pargellis C., Pav S., Proto A., Swinamer A., Tong L., and Torcellini C. Pyrazole urea-based inhibitors of p38 MAP kinase: From lead compound to clinical candidate. J. Med. Chem. 45 (2002) 2994-3008
12. Trask Jr. O.J., Baker A., Williams R.G., Kickischer D., Kandasamy R., Laethem C., Johnston P.A., and Johnston P.A. Assay development and case history of a 32K-biased library high-content MK2-EGFP translocation screen to identify p38 MAPK inhibitors on the ArrayScan 3.1 imaging platform. Methods Enzymol. 414 (2006) (this volume)
13. Williams R.G., Kandasamy R., Nickischer D., Trask Jr. O.J., Laethem C., Johnston P.A., and Johnston P.A. Generation and characterization of a stable MK2-EGFP cell line and subsequent development of a high-content imaging assay on the Cellomics ArrayScan platform to screen for p38 mitogen-activated protein kinase inhibitors. Methods Enzymol. 414 (2006) (this volume)
14. Zhang J.H., Chung T.D., and Oldenburg K.R. A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J. Biomol. Screen. 4 (1999) 67-73