Homogeneous and nonradioactive high-throughput screening platform for the characterization of kinase inhibitors in cell lysates

Journal of Biomolecular Screening

Volumn 11, Issue 8, 2006, Pages 1015-1026

  Guenat, Sylvie ^a   Rouleau, Nathalie ^b   Bielmann, Christelle ^a   Bedard, Julie ^b   Maurer, Fabienne ^a   Allaman Pillet, Nathalie ^a   Nicod, Pascal ^a   Bielefeld Sévigny, Martina ^b   Beckmann, Jacques S ^a   Bonny, Christophe ^a   Bossé, Roger ^b   Roduit, Raphaël ^a,c  

^a LAUSANNE UNIVERSITY HOSPITAL   (Switzerland)

^b INSTITUTE FOR RESEARCH IN IMMUNOLOGY AND CANCER   (Canada)

^c Institut de Recherche en Ophtalmologie   (Switzerland)

Author keywords

AlphaScreen; JNK inhibitors; Protein kinases

Indexed keywords

PEPTIDE; PROTEIN KINASE; PROTEIN KINASE INHIBITOR; RECOMBINANT ENZYME; STRESS ACTIVATED PROTEIN KINASE; STRESS ACTIVATED PROTEIN KINASE INHIBITOR;

ARTICLE; BINDING AFFINITY; BIOTECHNOLOGY; CELL LYSATE; CELL STRAIN HEPG2; CONTROLLED STUDY; ENZYME ACTIVITY; ENZYME ANALYSIS; ENZYME ASSAY; ENZYME INHIBITION; ENZYME PURIFICATION; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; LUMINESCENCE; PRIORITY JOURNAL; PROCESS DEVELOPMENT; REGULATORY MECHANISM;

BINDING SITES; BINDING, COMPETITIVE; CELL LINE; COMBINATORIAL CHEMISTRY TECHNIQUES; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; HUMANS; MAP KINASE KINASE 4; PROTEIN KINASES;

EID: 33751558665     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057106294697     Document Type: Article

References (25)

1. Manning G, Whyte DB, Martinez R, Hunter T, Sudarsanam S: The protein kinase complement of the human genome. Science 2002;298:1912-1934.
2. Futreal PA, Coin L, Marshall M, Down T, Hubbard T, Wooster R, et al: A census of human cancer genes. Nat Rev Cancer 2004;3:177-183.
3. Manning AM, Davis RJ: Targeting JNK for therapeutic benefit: from junk to gold? Nat Rev Drug Discov 2003;7:554-565.
4. Cohen P: Protein kinases - the major drug targets of the twenty-first century? Nat Rev Drug Discov 2002;4:309-315.
5. Dancey J, Sausville EA: Issues and progress with protein kinase inhibitors for cancer treatment. Nat Rev Drug Discov 2003;4:296-313.
6. Warner G, Illy C, Pedro L, Roby P, Bossé R: AlphaScreen kinase HTS platforms. Curr Med Chem 2004;11:719-728.
7. Li Y, Cummings RT, Cunningham BR, Chen Y, Zhou G: Homogeneous assays for adenosine 5′-monophosphate-activated protein kinase. Anal Biochem 2003;2:151-156.
8. Gray A, Olsson H, Batty IH, Priganica L, Peter DC: Nonradioactive methods for the assay of phosphoinositide 3-kinases and phosphoinositide phosphatases and selective detection of signaling lipids in cell and tissue extracts. Anal Biochem 2003;2:234-245.
9. Skelton NJ, Koehler MFT, Zobel K, Wong WL, Yeh S, Pisabarro MT, et al: Origins of PDZ domain ligand specificity: structure determination and mutagenesis of the Erbin PDZ domain. J Biol Chem 2003;9:7645-7654.
10. Xu HE, Stanley TB, Montana VG, Lambert MH, Shearer BG, Cobb JE, et al: Structural basis for antagonist-mediated recruitment of nuclear corepressors by PPAR[alpha]. Nature 2002;6873:813-817.
11. Bonny C, Oberson A, Negri S, Sauser C, Schorderet DF: Cell-permeable peptide inhibitors of JNK: novel blockers of beta-cell death. Diabetes 2001;1:77-82.
12. Barr RK, Kendrick TS, Bogoyevitch MA: Identification of the critical features of a small peptide inhibitor of JNK activity. J Biol Chem 2002;13:10987-10997.
13. Bogoyevitch MA: Therapeutic promise of JNK ATP-noncompetitive inhibitors. Trends Mol Med 2005;5:232-239.
14. Chorev M, Goodman M: Recent developments in retro peptides and proteins - an ongoing topochemical exploration. Trends Biotechnol 1995;10:438-445.
15. 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;2:67-73.
16. Bozyczko-Coyne D, Saporito MS, Hudkins RL: Targeting the JNK pathway for therapeutic benefit in CNS disease. Curr Drug Targets CNS Neurol Disord 2002;1:31-49.
17. Dickens M, Rogers JS, Cavanagh J, Raitano A, Xia Z, Halpern JR, et al: A cytoplasmic inhibitor of the JNK signal transduction pathway. Science 1997;5326:693-696.
18. Shults MD, Janes KA, Lauffenburger DA, Imperiali B: A multiplexed homogeneous fluorescence-based assay for protein kinase activity in cell lysates. Nat Methods 2005;4:277-284.
19. Deniz AA, Dahan M, Grunwell JR, Ha T, Faulhaber AE, Chemla DS, et al: Single-pair fluorescence resonance energy transfer on freely diffusing molecules: observation of Forster distance dependence and subpopulations. Proc Natl Acad Sci USA 1999;7:3670-3675.
20. Heo YS, Kim SK, Seo CI, Kim YK, Sung BJ, Lee HS, et al: Structural basis for the selective inhibition of JNK1 by the scaffolding protein JIP1 and SP600125. EMBO J 2004;23:2185-2195.
21. Liu B, Li S, Hu J: Technological advances in high-throughput screening. Am J Pharmacogenomics 2004;4:263-276.
22. Glickman JF, Wu X, Mercuri R, Illy C, Bowen BR, He Y et al: A comparison of ALPHAScreen, TR-FRET, and TRF as assay methods for FXR nuclear receptors. J Biomol Screen 2002;1:3-10.
23. Bosse R, Illy C, Elands J, Chelsky D: Miniaturizing screening: how low can we go today? Drug Discovery Today 2000;1(Suppl 1):42-47.
24. Von Leoprechting A, Kumpf R, Menzel S, Reulle D, Griebel R, Valler MJ, et al: Miniaturization and validation of a high-throughput serine kinase assay using the AlphaScreen platform. J Biomol Screen 2004;8:719-725.
25. Rininsland F, Xia W, Wittenburg S, Shi X, Stankewicz C, Achyuthan K, et al: Metal ion-mediated polymer superquenching for highly sensitive detection of kinase and phosphatase activities. Proc Natl Acad Sci USA 2004;43:15295-15300.