Data concordance from a comparison between filter binding and fluorescence polarization assay formats for identification of ROCK-II inhibitors

Journal of Biomolecular Screening

Volumn 8, Issue 4, 2003, Pages 399-409

  Hubert, Cassandra L ^a   Sherling, Stacy E ^a   Johnston, Patricia A ^a   Stancato, Louis F ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

Comparison; Filtration; Fluorescence polarization; Format; Kinase assays; Rho kinase; ROCK inhibitors

Indexed keywords

CYTOKINE; GROWTH FACTOR; GUANOSINE TRIPHOSPHATASE; PHOSPHORUS 33; PROTEIN KINASE INHIBITOR; PROTEIN SERINE THREONINE KINASE; RAC PROTEIN; RHO FACTOR; SERINE THREONINE KINASE ROCK I; SERINE THREONINE KINASE ROCK II; SERINE THREONINE KINASE ROCK II INHIBITOR; UNCLASSIFIED DRUG; ADENOSINE TRIPHOSPHATE; ENZYME INHIBITOR; RHO KINASE; RHO-ASSOCIATED KINASE; SIGNAL PEPTIDE;

ARTICLE; CANCER; CARDIOVASCULAR DISEASE; CYTOSKELETON; DRUG DETERMINATION; DRUG POTENCY; FLUORESCENCE POLARIZATION; HIGH THROUGHPUT SCREENING; KINETICS; METHODOLOGY; MOLECULAR DYNAMICS; PRIORITY JOURNAL; PROTEIN FAMILY; QUALITY CONTROL; COMPARATIVE STUDY; DRUG ANTAGONISM; DRUG SCREENING; EVALUATION; FILTRATION; METABOLISM;

ADENOSINE TRIPHOSPHATE; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; FILTRATION; FLUORESCENCE POLARIZATION; INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS; KINETICS; PROTEIN-SERINE-THREONINE KINASES;

EID: 2142830967     PISSN: 10870571     EISSN: None     Source Type: Journal    
DOI: 10.1177/1087057103255071     Document Type: Article

References (26)

1. Bishop AL, Hall A: Rho GTPases and their effector proteins. Biochem J 2000;348(Pt. 2):241-255.
2. Nakagawa O, Fujisawa K, Ishizaki T, Saito Y, Nakao K, Narumiya S: ROCK-I and ROCK-II, two isoforms of Rho-associated coiled-coil forming protein serine/threonine kinase in mice. FEBS Lett 1996;392(2):189-193.
3. Teo M, Manser E, Lim L: Identification and molecular cloning of a p21cdc42/rac1-activated serine/threonine kinase that is rapidly activated by thrombin in platelets. J Biol Chem 1995;270(44):26690-26697.
4. Di Cunto F, Calautti E, Hsiao J, Ong L, Topley G, Turco E, et al: Citron rho-interacting kinase, a novel tissue-specific ser/thr kinase encompassing the Rho-Rac-binding protein Citron. J Biol Chem 1998;273(45):29706-29711.
5. Yang N, Higuchi O, Ohashi K, Nagata K, Wada A, Kangawa K, et al: Cofilin phosphorylation by LIM-kinase 1 and its role in Rac-mediated actin reorganization. Nature 1998;393(6687):809-812.
6. Potier MC, Chelot E, Pekarsky Y, Gardiner K, Rossier J, Turnell WG: The human myosin light chain kinase (MLCK) from hippocampus: cloning, sequencing, expression, and localization to 3qcen-q21. Genomics 1995;29(3):562-570.
7. Itoh K, Yoshioka K, Akedo H, Uehata M, Ishizaki T, Narumiya S: An essential part for Rho-associated kinase in the transcellular invasion of tumor cells. Nat Med 1999;5(2):221-225.
8. Bourguignon LY, Zhu H, Shao L, Zhu D, Chen YW: Rho-kinase (ROK) promotes CD44v(3,8-10)-ankyrin interaction and tumor cell migration in metastatic breast cancer cells. Cell Motil Cytoskeleton 1999;43(4):269-287.
9. Uehata M, Ishizaki T, Satoh H, Ono T, Kawahara T, Morishita T, et al: Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension. Nature 1997;389(6654):990-994.
10. Myers MR, He W, Hulme C: Inhibitors of tyrosine kinases involved in inflammation and autoimmune disease. Current Phar Design 1997;3:473-502.
11. Warrior U, Chiou XG, Sheets MP, Sciotti RJ, Parry JM, Simmer RL, et al: Development of a p38 kinase binding assay for high throughput screening. J Biomol Screen 1999;4(3):129-135.
12. 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(2):318-329.
13. Checovich WJ, Bolger RE, Burke T: Fluorescence polarization-a new tool for cell and molecular biology. Nature 1995;375(6528):254-256.
14. Kenten JH, Casadei J, Link J, Lupold S, Willey J, Powell M, et al: Rapid electrochemiluminescence assays of polymerase chain reaction products. Clin Chem 1991;37(9):1626-1632.
15. Cohen CB, Chin-Dixon E, Jeong S, Nikiforov TT: A microchip-based enzyme assay for protein kinase A. Anal Biochem 1999;273(1):89-97.
16. Fox S, Wang H, Sopchak L, Farr-Jones S: High throughput screening 2002: moving toward increased success rates. J Biomol Screen 2002;7(4):313-316.
17. Seethala R, Menzel R: A homogeneous, fluorescence polarization assay for src-family tyrosine kinases. Anal Biochem 1997;253(2):210-218.
18. Park YW, 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(1):94-104.
19. Sorg G, Schubert HD, Buttner FH, Heilker R: Automated high throughput screening for serine kinase inhibitors using a LEADseeker scintillation proximity assay in the 1536-well format. J Biomol Screen 2002;7(1):11-19.
20. 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(3):191-214.
21. Trauger JW, Lin FF, Turner MS, Stephens J, LoGrasso PV: Kinetic mechanism for human Rho-Kinase II (ROCK-II). Biochemistry 2002;41(28):8948-8953.
22. Newton AC: Protein kinase C: structural and spatial regulation by phosphorylation, cofactors, and macromolecular interactions. Chem Rev 2001;101(8):2353-2364.
23. 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(2):77-88.
24. Chang PC, Rubin RT, Yu M: Optimal statistical design of radioimmunoassays and competitive protein-binding assays. Endocrinology 1975;96(4): 973-981.
25. 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(2):67-73.
26. Bland JM, Altman DG: Statistical methods for assessing agreement between two methods of clinical measurement. Lancet 1986;1(8476):307-310.