A novel cell-based, high-content assay for phosphorylation of Lats2 by Aurora A

Journal of Biomolecular Screening

Volumn 16, Issue 8, 2011, Pages 925-931

  Emery, Amy ^a,b   Sorrell, David A ^a,c   Lawrence, Stacy ^a   Easthope, Emma ^a,d   Stockdale, Mark ^a,c   Jones, David O ^a,e   Zheleva, Daniella ^a   Scaerou, Frederic ^a   Glover, David M ^a,b  

^a Cylacel Ltd   (United Kingdom)

^b UNIVERSITY OF CAMBRIDGE   (United Kingdom)

^c Molecular Biotechnology Center   (United Kingdom)

^d Cellzome Ltd   (United Kingdom)

^e Domantis   (United Kingdom)

Author keywords

AZD1152 HQPA; Cellomics ArrayScan; High content screening (HCS); Image based screening; MLN8054; VX680 (MK 0457)

Indexed keywords

4 [[9 CHLORO 7 (2,6 DIFLUOROPHENYL) 5H PYRIMIDO[5,4 D][2]BENZAZEPIN 2 YL]AMINO]BENZOIC ACID; AURORA A KINASE; BARASERTIB; MONOCLONAL ANTIBODY; PROTEIN LATS2; PROTEIN SERINE THREONINE KINASE; PROTEIN SERINE THREONINE KINASE INHIBITOR; PROTEIN TACC3; TOZASERTIB; UNCLASSIFIED DRUG;

ARTICLE; CENTROSOME; COMPETITIVE INHIBITION; CONCENTRATION RESPONSE; CONTROLLED STUDY; ENZYME ACTIVITY; ENZYME SUBSTRATE; FEMALE; HELA CELL; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IMAGE ANALYSIS; IMMUNOFLUORESCENCE; MITOSIS; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN DETERMINATION; PROTEIN PHOSPHORYLATION; PROTEIN TARGETING; SENSITIVITY AND SPECIFICITY; SEQUENCE ANALYSIS; SIGNAL NOISE RATIO;

ANTIBODIES, PHOSPHO-SPECIFIC; ANTINEOPLASTIC AGENTS; AUTOMATION, LABORATORY; CENTROSOME; FEMALE; HELA CELLS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; MICROTUBULE-ASSOCIATED PROTEINS; MITOSIS; MOLECULAR IMAGING; PHOSPHORIC ACID ESTERS; PHOSPHORYLATION; PIPERAZINES; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; QUINAZOLINES; SMALL MOLECULE LIBRARIES; TUMOR SUPPRESSOR PROTEINS; UTERINE CERVICAL NEOPLASMS;

EID: 80054736913     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057111413923     Document Type: Article

References (15)

1. Gautschi, O.; Heighway, J.; Mack, P. C.; Purnell, P. R.; Lara, P. N., Jr.; Gandara, D. R. Aurora Kinases as Anticancer Drug Targets. Clin. Cancer Res. 2008, 14, 1639-1648. (Pubitemid 351471713)
2. Barr, A. R.; Gergely, F. Aurora-A: The Maker and Breaker of Spindle Poles. J. Cell Sci. 2007, 120, 2987-2996.
3. Manfredi, M. G.; Ecsedy, J. A.; Meetze, K. A.; Balani, S. K.; Burenkova, O.; Chen, W.; Galvin, K. M.; Hoar, K. M.; Huck, J. J.; Leroy, P. J.; et al. Antitumor Activity of MLN8054, an Orally Active Small-Molecule Inhibitor of Aurora A Kinase. Proc. Natl. Acad. Sci. U. S. A. 2007, 104, 4106-4111. (Pubitemid 47181586)
4. Ruchaud, S.; Carmena, M.; Earnshaw, W. C. Chromosomal Passengers: Conducting Cell Division. Nat. Rev. Mol. Cell Biol. 2007, 8, 798-812. (Pubitemid 47462135)
5. Ditchfield, C.; Johnson, V. L.; Tighe, A.; Ellston, R.; Haworth, C.; Johnson, T.; Mortlock, A.; Keen, N.; Taylor, S. S. Aurora B Couples Chromosome Alignment with Anaphase by Targeting BubR1, Mad2, and Cenp-E to Kinetochores. J. Cell Biol. 2003, 161, 267-280. (Pubitemid 36529846)
6. Hauf, S.; Cole, R. W.; Laterra, S.; Zimmer, C.; Schnapp, G.; Walter, R.; Heckel, A.; Van Meel, J.; Rieder, C. L.; Peters, J. M. The Small Molecule Hesperadin Reveals a Role for Aurora B in Correcting Kinetochore-Microtubule Attachment and in Maintaining the Spindle Assembly Checkpoint. J. Cell Biol. 2003, 161, 281-294. (Pubitemid 36529847)
7. Bushway, P. J.; Mercola, M.; Price, J. H. A. Comparative Analysis of Standard Microtiter Plate Reading versus Imaging in Cellular Assays. Assay Drug Dev. Technol. 2008, 6, 557-567.
8. Catalano, S. M.; Mclaughlin, J.; Hitoshi, Y.; Payan, D. Discovery and Development of an Aurora Kinase Inhibitor Clinical Candidate using an Image-Based Assay for Measuring Proliferation, Apoptosis, and DNA Content. Assay Drug Dev. Technol. 2009, 7, 180-190.
9. Gasparri, F.; Sola, F.; Bandiera, T.; Moll, J.; Galvani, A. High-Content Analysis of Kinase Activity in Cells. Comb. Chem. High Throughput Screen. 2008, 11, 523-536.
10. Leroy, P. J.; Hunter, J. J.; Hoar, K. M.; Burke, K. E.; Shinde, V.; Ruan, J.; Bowman, D.; Galvin, K.; Ecsedy, J. A. Localization of Human TACC3 to Mitotic Spindles Is Mediated by Phosphorylation on Ser558 by Aurora A: A Novel Pharmacodynamic Method for Measuring Aurora A Activity. Cancer Res. 2007, 67, 5362-5370. (Pubitemid 46997276)
11. Kinoshita, K.; Noetzel, T. L.; Pelletier, L.; Mechtler, K.; Drechsel, D. N.; Schwager, A.; Lee, M.; Raff, J. W.; Hyman, A. A. Aurora A Phosphorylation of TACC3/Maskin Is Required for Centrosome-Dependent Microtubule Assembly in Mitosis. J. Cell Biol. 2005, 170, 1047-1055. (Pubitemid 41362637)
12. Toji, S.; Yabuta, N.; Hosomi, T.; Nishihara, S.; Kobayashi, T.; Suzuki, S.; Tamai, K.; Nojima, H. The Centrosomal Protein Lats2 Is a Phosphorylation Target of Aurora-A Kinase. Genes Cells 2004, 9, 383-397. (Pubitemid 38771930)
13. Harrington, E. A.; Bebbington, D.; Moore, J.; Rasmussen, R. K.; Ajose-Adeogun, A. O.; Nakayama, T.; Graham, J. A.; Demur, C.; Hercend, T.; Diu-Hercend, A.; et al. VX-680, a Potent and Selective Small-Molecule Inhibitor of the Aurora Kinases, Suppresses Tumor Growth In Vivo. Nat. Med. 2004, 10, 262-267. (Pubitemid 38667616)
14. Zhang, J. H.; Chung, T. D.; Oldenburg, K. R. A Simple Statistical Parameter for use in Evaluation and Validation of High Throughput Screening Assays. J. Biomol. Screen. 1999, 4, 67-73. (Pubitemid 29278954)
15. Mortlock, A. A.; Foote, K. M.; Heron, N. M.; Jung, F. H.; Pasquet, G.; Lohmann, J. J.; Warin, N.; Renaud, F.; De Savi, C.; Roberts, N. J.; et al. Discovery, Synthesis, and In Vivo Activity of a New Class of Pyrazoloquinazolines as Selective Inhibitors of Aurora B Kinase. J. Med. Chem. 2007, 50, 2213-2224. (Pubitemid 46683074)