A high throughput luminescent assay for glycogen synthase kinase-3β inhibitors

Assay and Drug Development Technologies

Volumn 5, Issue 1, 2007, Pages 75-83

  Baki, Andrea ^a   Bielik, Attila ^a   Molnár, László ^a   Szendrei, Györgyi ^a   Keserü, György M ^a  

^a GEDEON RICHTER LTD   (Hungary)

Author keywords

[No Author keywords available]

Indexed keywords

ENZYME INHIBITOR; GLYCOGEN SYNTHASE KINASE 3B; GLYCOGEN SYNTHASE KINASE 3BETA INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; ENZYME ACTIVITY; ENZYME ASSAY; ENZYME SUBSTRATE; HIGH THROUGHPUT SCREENING; LUMINESCENCE; REPRODUCIBILITY; SENSITIVITY ANALYSIS;

CELL LINE; CHEMILUMINESCENT MEASUREMENTS; GLYCOGEN SYNTHASE KINASE 3; PROTEIN KINASE INHIBITORS;

EID: 34147216138     PISSN: 1540658X     EISSN: None     Source Type: Journal    
DOI: 10.1089/adt.2006.029     Document Type: Article

References (19)

1. Cohen P, Frame S: The renaissance of GSK3. Nat Rev Mol Cell Biol 2001;2:769-776.
2. Bhat RV, Budd Haeberlein SL, Avila J: Glycogen synthase kinase 3: a drug target for CNS therapies. J Neurochem 2004;89:1313-1317.
3. Gaudet EA, Huang KS, Zhang Y, Huang W, Mark D, Sportsman JR: A homogeneous fluorescence polarization assay adaptable for a range of protein serine/threonine and tyrosine kinases. J Biomol Screen 2003;8:164-175.
4. V600EBRAF in an enzyme cascade high-throughput screen. J Biomol Screen 2006;11:145-154.
5. Rodems SM, Hamman BD, Lin C, Zhao J, Shah S, Heidary D, et al.: A FRET-based assay platform for ultra-high density drug screening of protein kinases and phosphatases. Assay Drug Dev Technol 2002;1:9-19.
6. Mallari R, Swearingen E, Liu W, Ow A, Young SW, Huang SG: A generic high-throughput screening assay for kinases: protein kinase A as an example. J Biomol Screen 2003;8:164-175.
7. Granas C, Lundholt BK, Loechel F, Pedersen HC, Bjorn SP, Linde V, et al.: identification of RAS-mitogen-activated protein kinase signalling pathway modulators in an ERF1 redistribution® screen. J Biomol Screen 2006;11: 423-434.
8. Koresawa M, Okabe T: High-throughput screening with quantitation of ATP consumption: an universal non-radioisotope, homogeneous assay for protein kinase. Assay Drug Dev Technol 2004;2:153-160.
9. Coghlan MP, Culbert AA, Cross DAE, Corcoran SL, Yates JW, Pearce NJ, et al.: Selective small molecules inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem Biol 2000;7:793-803.
10. Bhat R, Xue Y, Berg S, Hellberg S, Ormö M, Nilsson Y, et al.: Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418. J Biol Chem 2003;278:45937-45945.
11. Martinez A, Alonso M, Castro A, Pérez C, Moreno. FJ: First non-ATP competitive glycogen synthase kinase 3β (GSK 3β) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease. J Med Chem 2002;45:1292-1299.
12. Bánki Z, Báthor M, Molnár L, Bielik A, Keserü GM: Scheduling a flexible, open-architecture robotic workstation under LabWindows. J Assoc Lab Automat 2005;10:149-154.
13. Zhang JH, Chung TDY, Oldenburg KR: A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 1999;4: 67-73.
14. Ferrer JC, Favre C, Gomis RR, Fernandez-Novell JM, Garcia-Rocha M, de la Iglesia N, et al.: Control of glycogen deposition. FEBS Lett 2003;546:127-132.
15. Bebbington D, Charrier J-D, Golec J, Miller A, Knegtel R: Pyrazole compounds useful as protein kinase inhibitors. Vertex patent. WO 02/057259. International publication date: July 25, 2002.
16. Dajani R, Fraser E, Roe SM, Young N, Good V, Dale TC, et al.: Crystal structure of glycogen synthase kinase 3β: structural basis for phosphate-primed substrate specificity and autoinhibition. Cell 2001;105:721-732.
17. Tagliati F, Bottom A, Bosetti A, Zatelli MC, Uberti EC: Utilization of luminescent technology to develop a kinase assay: CDK4 as a model system. J Pharm Biomed Anal 2005;39:811-814.
18. Gribbon P, Lyons R, Laflin P, Bradley J, Chambers C, Williams BS, et al.: Evaluating real-life high-throughput screening data. J Biomol Screen 2005;10:99-107.
19. Polgár T, Baki A, Szendrei IGy, Keserü GM: Comparative virtual and experimental high-throughput screening for glycogen synthase kinase-3β inhibitors. J Med Chem 2005;48:7946-7959.