A Generic Platform for Cellular Screening Against Ubiquitin Ligases

Scientific Reports

Volumn 6, Issue , 2016, Pages

  Maculins, Timurs ^a,d,e   Carter, Nikki ^a   Dorval, Thierry ^a   Hudson, Kevin ^a   Nissink, J Willem M ^b   Hay, Ronald T ^c   Alwan, Husam ^a  

^a ASTRAZENECA   (United Kingdom)

^b Oncology iMED   (United Kingdom)

^c UNIVERSITY OF DUNDEE   (United Kingdom)

^d GOETHE UNIVERSITY   (Germany)

^e FRAUNHOFER INSTITUTE FOR MOLECULAR BIOLOGY AND APPLIED ECOLOGY IME   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

2-((4-METHYLPHENYL)SULFONYL)-5-NITROFURAN; DNA BINDING PROTEIN; ENZYME INHIBITOR; GAL4 PROTEIN, S CEREVISIAE; LUCIFERASE; NITROFURAN DERIVATIVE; SACCHAROMYCES CEREVISIAE PROTEIN; SULFONE; TRANSCRIPTION FACTOR; UBIQUITIN; UBIQUITIN PROTEIN LIGASE;

ANTAGONISTS AND INHIBITORS; CHEMISTRY; CYTOLOGY; DRUG DEVELOPMENT; DRUG EFFECTS; GENE EXPRESSION REGULATION; GENE VECTOR; GENETIC TRANSFECTION; GENETICS; HEK293 CELL LINE; HIGH THROUGHPUT SCREENING; HUMAN; METABOLISM; OSTEOBLAST; PROCEDURES; PROMOTER REGION; REPORTER GENE; TUMOR CELL LINE; UBIQUITINATION;

CELL LINE, TUMOR; DNA-BINDING PROTEINS; DRUG DISCOVERY; ENZYME INHIBITORS; GENE EXPRESSION REGULATION; GENES, REPORTER; GENETIC VECTORS; HEK293 CELLS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; LUCIFERASES; NITROFURANS; OSTEOBLASTS; PROMOTER REGIONS, GENETIC; SACCHAROMYCES CEREVISIAE PROTEINS; SULFONES; TRANSCRIPTION FACTORS; TRANSFECTION; UBIQUITIN; UBIQUITIN-PROTEIN LIGASES; UBIQUITINATION;

EID: 84953896882     PISSN: None     EISSN: 20452322     Source Type: Journal    
DOI: 10.1038/srep18940     Document Type: Article

References (33)

1. Capili, A. D. & Lima, C. D. Taking it step by step: mechanistic insights from structural studies of ubiquitin/ubiquitin-like protein modification pathways. Curr Opin Struct Biol 17, 726-735 (2007).
2. Dikic, I., Wakatsuki, S. & Walters, K. J. Ubiquitin-binding domains - from structures to functions. Nat Rev Mol Cell Biol 10, 659-671 (2009).
3. Bedford, L., Lowe, J., Dick, L. R., Mayer, R. J. & Brownell, J. E. Ubiquitin-like protein conjugation and the ubiquitin-proteasome system as drug targets. 1-18 (2010). doi: 10.1038/nrd3321.
4. Varfolomeev, E. et al. IAP Antagonists Induce Autoubiquitination of c-IAPs, NF-κB Activation, and TNFα-Dependent Apoptosis. Cell 131, 669-681 (2007).
5. Ceccarelli, D. F. et al. An Allosteric Inhibitor of the Human Cdc34 Ubiquitin-Conjugating Enzyme. Cell 145, 1075-1087 (2011).
6. Verma, R. et al. Ubistatins inhibit proteasome-dependent degradation by binding the ubiquitin chain. Science (New York, NY) 306, 117-120 (2004).
7. Cohen, P. & Tcherpakov, M. Will the Ubiquitin System Furnish as Many Drug Targets as Protein Kinases? Cell 143, 686-693 (2010).
8. de Bie, P. & Ciechanover, A. Ubiquitination of E3 ligases: self-regulation of the ubiquitin system via proteolytic and non-proteolytic mechanisms. Cell Death and Differentiation 18, 1393-1402 (2011).
9. Fields, S. & Song, O. A novel genetic system to detect protein-protein interactions. Nature 340, 245-246 (1989).
10. Hjerpe, R. et al. Efficient protection and isolation of ubiquitylated proteins using tandem ubiquitin-binding entities. EMBO Rep 10, 1250-1258 (2009).
11. Sims, J. J. et al. Polyubiquitin-sensor proteins reveal localization and linkage-type dependence of cellular ubiquitin signaling. Nature Methods 9, 303-309 (2012).
12. van Wijk, S. J. L. et al. Fluorescence-based sensors to monitor localization and functions of linear and K63-linked ubiquitin chains in cells. Mol Cell 47, 797-809 (2012).
13. Emmerich, C. H. et al. Activation of the canonical IKK complex by K63/M1-linked hybrid ubiquitin chains. Proc. Natl. Acad. Sci 110, 15247-15252 (2013).
14. Plans, V. et al. The RING finger protein RNF8 recruits UBC13 for lysine 63-based self polyubiquitylation. J Cell Biochem 97, 572-582 (2006).
15. Yin, Q. et al. E2 interaction and dimerization in the crystal structure of TRAF6. Nat Struct Mol Biol 16, 658-666 (2009).
16. Kang, D., Chen, J., Wong, J. & Fang, G. The checkpoint protein Chfr is a ligase that ubiquitinates Plk1 and inhibits Cdc2 at the G2 to M transition. J Cell Biol 156, 249-259 (2002).
17. Bothos, J., Summers, M. K., Venere, M., Scolnick, D. M. & Halazonetis, T. D. The Chfr mitotic checkpoint protein functions with Ubc13-Mms2 to form Lys63-linked polyubiquitin chains. Oncogene 22, 7101-7107 (2003).
18. Petroski, M. D. et al. Substrate Modification with Lysine 63-linked Ubiquitin Chains through the UBC13-UEV1A Ubiquitin-conjugating Enzyme. Journal of Biological Chemistry 282, 29936-29945 (2007).
19. Pulvino, M. et al. Inhibition of proliferation and survival of diffuse large B-cell lymphoma cells by a small-molecule inhibitor of the ubiquitin-conjugating enzyme Ubc13-Uev1A. Blood 120, 1668-1677 (2012).
20. Sui, Y. & Wu, Z. Alternative Statistical Parameter for High-Throughput Screening Assay Quality Assessment. Journal of Biomolecular Screening 12, 229-234 (2007).
21. Luijsterburg, M. S. & van Attikum, H. Close encounters of the RNF8th kind: when chromatin meets DNA repair. Curr Opin Cell Biol 24, 439-447 (2012).
22. Mattiroli, F. et al. RNF168 Ubiquitinates K13-15 on H2A/H2AX to Drive DNA Damage Signaling. Cell 150, 1182-1195 (2012).
23. Acs, K. et al. The AAA-ATPase VCP/p97 promotes 53BP1 recruitment by removing L3MBTL1 from DNA double-strand breaks. Nat Struct Mol Biol 18, 1345-1350 (2011).
24. Nissink, J. W. M. & Blackburn, S. Quantification of frequent-hitter behavior based on historical high-throughput screening data. Future Medicinal Chemistry 6, 1113-1126 (2014).
25. Hunter, T. The Age of Crosstalk: Phosphorylation, Ubiquitination, and Beyond. Mol Cell 28, 730-738 (2007).
26. Huen, M. S. Y. et al. RNF8 Transduces the DNA-Damage Signal via Histone Ubiquitylation and Checkpoint Protein Assembly. Cell 131, 901-914 (2007).
27. Mailand, N. et al. RNF8 Ubiquitylates Histones at DNA Double-Strand Breaks and Promotes Assembly of Repair Proteins. Cell 131, 887-900 (2007).
28. Murray, M. F. et al. A High-Throughput Screen Measuring Ubiquitination of p53 by Human mdm2. Journal of Biomolecular Screening 12, 1050-1058 (2007).
29. Hong, C. A. et al. Development of a high throughput time-resolved fluorescence resonance energy transfer assay for TRAF6 ubiquitin polymerization. Assay Drug Dev Technol 1, 175-180 (2003).
30. Orlicky, S. et al. An allosteric inhibitor of substrate recognition by the SCFCdc4 ubiquitin ligase. Nat Biotechnol 28, 733-737 (2010).
31. Skaar, J. R., Pagan, J. K. & Pagano, M. SCF and drug discovery. Nat Rev Drug Discov 13, 889-903 (2014).
32. Vassilev, L. T. et al. In vivo activation of the p53 pathway by small-molecule antagonists of MDM2. Science (New York, NY) 303, 844-848 (2004).
33. Davies, S. P., Reddy, H., Caivano, M. & Cohen, P. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J 351, 95-105 (2000).