A bioluminogenic HDAC activity assay: Validation and screening

Journal of Biomolecular Screening

Volumn 16, Issue 10, 2011, Pages 1227-1235

  Halley, Francoise ^a   Reinshagen, Jeanette ^a   Ellinger, Bernhard ^a   Wolf, Markus ^a   Niles, Andrew L ^b   Evans, Nathan J ^b   Kirkland, Thomas A ^c   Wagner, Julia M ^d   Jung, Manfred ^d   Gribbon, Philip ^a   Gul, Sheraz ^a  

^a European ScreeningPort GmbH   (Germany)

^b PROMEGA CORPORATION   (United States)

^c Promega Biosciences LLC   (United States)

^d UNIVERSITY OF FREIBURG   (Germany)

Author keywords

assay development; drug discovery; high throughput screening; histone deacetylase; sirtuin

Indexed keywords

B 5887; BUTYRIC ACID; DIMETHYL SULFOXIDE; HISTONE DEACETYLASE 1; HISTONE DEACETYLASE 3; HISTONE DEACETYLASE 6; P 4543; RECOMBINANT ENZYME; S 2671; SIRTUIN 1; SURAMIN; T 8552; TRICHOSTATIN A; UNCLASSIFIED DRUG; VALPROIC ACID;

ARTICLE; ENZYME ACTIVITY; ENZYME ASSAY; FERMENTATION; FOOD AND DRUG ADMINISTRATION; FUNGUS; HUMAN; MOLECULAR WEIGHT; PRIORITY JOURNAL; REPRODUCIBILITY; SCREENING; SENSITIVITY ANALYSIS; VALIDATION STUDY;

AUTOMATION, LABORATORY; DRUG DISCOVERY; ENZYME ACTIVATION; ENZYME ASSAYS; HIGH-THROUGHPUT SCREENING ASSAYS; HISTONE DEACETYLASE INHIBITORS; HISTONE DEACETYLASES; HUMANS; KINETICS; LUMINESCENT MEASUREMENTS; REPRODUCIBILITY OF RESULTS; SIRTUINS; SMALL MOLECULE LIBRARIES; SUBSTRATE SPECIFICITY;

EID: 83455218642     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057111416004     Document Type: Article

References (34)

1. Gallinari P., Di Marco S., Jones P., Pallaoro M., Steinkühler C.. HDACs, Histone Deacetylation and Gene Transcription: From Molecular Biology to Cancer Therapeutics. Cell Res. 2007 ; 17: 195-211 (Pubitemid 46438722)
2. Kim H. J., Bae S. C.. Histone Deacetylase Inhibitors: Molecular Mechanisms of Action and Clinical Trials as Anti-cancer Drugs. Am. J. Transl. Res. 2011 ; 3: 166-179
3. Bhavsar P., Ahmad T., Adcock I. M.. The Role of Histone Deacetylases in Asthma and Allergic Diseases. J. Allergy Clin. Immunol. 2008 ; 121: 580-584
4. Chavan A. V., Somani R. R.. HDAC Inhibitors-New Generation of Target Specific Treatment. Mini. Rev. Med. Chem. 2010 ; 10: 1263-1276
5. Wang H., Dymock B. W.. New Patented Histone Deacetylase Inhibitors. Expert Opin. Ther. Pat. 2009 ; 19: 1727-1757
6. de Ruijter A. J., van Gennip A. H., Caron H. N., Kemp S., van Kuilenburg A. B.. Histone Deacetylases (HDACs): Characterization of the Classical HDAC Family. Biochem. J. 2003 ; 15: 737-749 (Pubitemid 36399066)
7. Ficner R.. Novel Structural Insights into Class I and II Histone Deacetylases. Curr. Top. Med. Chem. 2009 ; 9: 235-240
8. Haigis M. C., Sinclair D. A.. Mammalian Sirtuins: Biological Insights and Disease Relevance. Annu. Rev. Pathol. 2010 ; 5: 253-295
9. Duvic M., Vu J.. Vorinostat: A New Oral Histone Deacetylase Inhibitor Approved for Cutaneous T-Cell Lymphoma. Expert Opin. Investig. Drugs. 2007 ; 16: 1111-1120 (Pubitemid 47074165)
10. Lemoine M., Younes A.. Histone Deacetylase Inhibitors in the Treatment of Lymphoma. Discov. Med. 2010 ; 10: 462-470
11. Schemies J., Uciechowska U., Sippl W., Jung M.. NAD+-Dependent Histone Deacetylases (Sirtuins) as Novel Therapeutic Targets. Med. Res. Rev. 2010 ; 30: 861-889
12. Aljada A., Dong L., Mousa S. A.. Sirtuin-Targeting Drugs: Mechanisms of Action and Potential Therapeutic Applications. Curr. Opin. Investig. Drugs. 2010 ; 11: 1158-1168
13. Sauve A. A.. Pharmaceutical Strategies for Activating Sirtuins. Curr. Pharm. Des. 2009 ; 15: 45-56
14. Kölle D., Brosch G., Lechner T., Lusser A., Loidl P.. Biochemical Methods for Analysis of Histone Deacetylases. Methods. 1998 ; 15: 323-331
15. Wegener D., Hildmann C., Riester D., Schober A., Meyer-Almes F. J., Deubzer H. E., Oehme I., Witt O., Lang S., Jaensch M., Makarov V., Lange C., Busse B., Schwienhorst A.. Identification of Novel Small-Molecule Histone Deacetylase Inhibitors by Medium-Throughput Screening Using a Fluorigenic Assay. Biochem. J. 2008 ; 413: 143-150 (Pubitemid 351946870)
16. Gribbon P., Sewing A.. Fluorescence Readouts in HTS: No Gain without Pain?. Drug Discov. Today. 2003 ; 8: 1035-1043 (Pubitemid 38018810)
17. Gul S., Gribbon P.. Exemplification of the Challenges Associated with Utilising Fluorescence Intensity Based Assays in Discovery. Expert Opin. Drug Discov. 2010 ; 5: 681-690
18. O'Brien M. A., Daily W. J., Hesselberth P. E., Moravec R. A., Scurria M. A., Klaubert D. H., Bulleit R. F., Wood K. V.. Homogeneous, Bioluminescent Protease Assays: Caspase-3 as a Model. J. Biomol. Screen. 2005 ; 10: 137-148
19. 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)
20. Hauser A. T., Jung M., Jung M.. Assays for Histone Deacetylases. Curr. Top. Med. Chem. 2009 ; 9: 227-234
21. Wegener D., Wirsching F., Riester D., Schwienhorst A.. A Fluorogenic Histone Deacetylase Assay Well Suited for High-Throughput Activity Screening. Chem. Biol. 2003 ; 10: 61-68 (Pubitemid 36154475)
22. Jadhav A., Ferreira R. S., Klumpp C., Mott B. T., Austin C. P., Inglese J., Thomas C. J., Maloney D. J., Shoichet B. K., Simeonov A.. Quantitative Analyses of Aggregation, Autofluorescence, and Reactivity Artifacts in a Screen for Inhibitors of a Thiol Protease. J. Med. Chem. 2010 ; 53: 37-51
23. Howitz K. T., Bitterman K. J., Cohen H. Y., Lamming D. W., Lavu S., Wood J. G., Zipkin R. E., Chung P., Kisielewski A., Zhang L. L., Scherer B., Sinclair D. A.. Small Molecule Activators of Sirtuins Extend Saccharomyces cerevisiae Lifespan. Nature. 2003 ; 425: 191-196 (Pubitemid 37150899)
24. Pacholec M., Bleasdale J. E., Chrunyk B., Cunningham D., Flynn D., Garofalo R. S., Griffith D., Griffor M., Loulakis P., Pabst B., Qiu X., Stockman B., Thanabal V., Varghese A., Ward J., Withka J., Ahn K.. SRT1720, SRT2183, SRT1460, and Resveratrol Are Not Direct Activators of SIRT1. J. Biol. Chem. 2010 ; 285: 8340-8351
25. Beher D., Wu J., Cumine S., Kim K. W., Lu S. C., Atangan L., Wang M.. Resveratrol Is Not a Direct Activator of SIRT1 Enzyme Activity. Chem. Biol. Drug Des. 2009 ; 74: 619-624
26. Ashburn T. T., Thor K. B.. Drug Repositioning: Identifying and Developing New Uses for Existing Drugs. Nat. Rev. Drug Discov. 2004 ; 3: 673-683 (Pubitemid 39173508)
27. Mack G. S.. To Selectivity and Beyond. Nat. Biotech. 2010 ; 28: 1259-1266
28. Gurvich N., Tsygankova O. M., Meinkoth J. L., Klein P. S.. Histone Deacetylase Is a Target of Valproic Acid-Mediated Cellular Differentiation. Cancer Res. 2004 ; 64: 1079-1086 (Pubitemid 38176913)
29. Olsen C. A., Ghadiri M. R.. Discovery of Potent and Selective Histone Deacetylase Inhibitors via Focused Combinatorial Libraries of Cyclic αβ-tetrapeptides. J. Med. Chem. 2009 ; 52: 7836-7846
30. Khan N., Jeffers M., Kumar S., Hackett C., Boldog F., Khramtsov N., Qian X., Mills E., Berghs S. C., Carey N., Finn P. W., Collins L. S., Tumber A., Ritchie J. W., Jensen P. B., Lichenstein H. S., Sehested M.. Determination of the Class and Isoform Selectivity of Small-Molecule Histone Deacetylase Inhibitors. Biochem. J. 2008 ; 409: 581-589 (Pubitemid 351184977)
31. Buggy J. J., Sideris M. L., Mak P., Lorimer D. D., McIntosh B., Clark J. M.. Cloning and Characterization of a Novel Human Histone Deacetylase, HDAC8. Biochem. J. 2000 ; 350: 199-205
32. Vannini A., Volpari C., Filocamo G., Casavola E. C., Brunetti M., Renzoni D., Chakravarty P., Paolini C., De Francesco R., Gallinari P., Steinkühler C., Di Marco S.. Crystal Structure of a Eukaryotic Zinc-Dependent Histone Deacetylase, Human HDAC8, Complexed with a Hydroxamic Acid Inhibitor. Proc. Natl. Acad. Sci. U. S. A. 2004 ; 101: 15064-15069 (Pubitemid 39391719)
33. Phiel C. J., Zhang F., Huang E. Y., Guenther M. G., Lazar M. A., Klein P. S.. Histone Deacetylase Is a Direct Target of Valproic Acid, a Potent Anticonvulsant, Mood Stabilizer, and Teratogen. J. Biol. Chem. 2001 ; 276: 36734-36741
34. Trapp J., Meier R., Hongwiset D., Kassack M. U., Sippl W., Jung M.. Structure-Activity Studies on Suramin Analogues as Inhibitors of NAD+-Dependent Histone Deacetylases (Sirtuins). Chem. Med. Chem. 2007 ; 2: 1419-1431