An electrophoretic mobility shift assay for the identification and kinetic analysis of acetyl transferase inhibitors

Analytical Biochemistry

Volumn 402, Issue 1, 2010, Pages 65-68

  Fanslau, Caroline ^a   Pedicord, Donna ^a   Nagulapalli, Sujatha ^a   Gray, Hillary ^a   Pang, Suhong ^a   Jayaraman, Lata ^a   Lippy, Jonathan ^a   Blat, Yuval ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

Acetyl transferase; Electrophoretic mobility shift assay; GCN5

Indexed keywords

BIOCHEMISTRY; CHEMISTRY;

ACETYL COENZYME; ACETYL TRANSFERASE; CELLULAR HOMEOSTASIS; ELECTROPHORETIC MOBILITY SHIFT ASSAY; GCN5; HIGH THROUGHPUT TESTING; KINETIC ANALYSIS; REACTIVE INHIBITORS;

ELECTROPHORETIC MOBILITY;

ACETYL COENZYME A; ACYLTRANSFERASE INHIBITOR; HISTONE ACETYLTRANSFERASE; PROTEIN GCN5L2; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; ENZYME INHIBITION; GEL MOBILITY SHIFT ASSAY; HUMAN; KINETICS; PRIORITY JOURNAL;

EID: 77952743473     PISSN: 00032697     EISSN: 10960309     Source Type: Journal    
DOI: 10.1016/j.ab.2010.03.025     Document Type: Article

References (15)

1. Selvi R.B., Kundu T.K. Reversible acetylation of chromatin: implication in regulation of gene expression, disease, and therapeutics. Biotechnol. J. 2009, 4:375-390.
2. Yang X.J., Seto E. HATs and HDACs: from structure, function, and regulation to novel strategies for therapy and prevention. Oncogene 2007, 26:5310-5318.
3. Tanner K.G., Trievel R.C., Kuo M.H., Howard R.M., Berger S.L., Allis C.D., Marmorstein R., Denu J.M. Catalytic mechanism and function of invariant glutamic acid 173 from the histone acetyltransferase GCN5 transcriptional coactivator. J. Biol. Chem. 1999, 274:18157-18160.
4. Trievel R.C., Rojas J.R., Sterner D.E., Venkataramani R.N., Wang L., Zhou J., Allis C.D., Berger S.L., Marmorstein R. Crystal structure and mechanism of histone acetylation of the yeast GCN5 transcriptional coactivator. Proc. Natl. Acad. Sci. USA 1999, 96:8931-8936.
5. Tanner K.G., Langer M.R., Denu J.M. Kinetic mechanism of human histone acetyltransferase P/CAF. Biochemistry 2000, 39:15652.
6. Yan Y., Harper S., Speicher D.W., Marmorstein R. The catalytic mechanism of the ESA1 histone acetyltransferase involves a self-acetylated intermediate. Nat. Struct. Biol. 2002, 9:862-869.
7. Manzo F., Tambaro F.P., Mai A., Altucci L. Histone acetyltransferase inhibitors and preclinical studies. Expert Opin. Ther. Pat. 2009, 19:761-774.
8. Stimson L., Rowlands M.G., Newbatt Y.M., Smith N.F., Raynaud F.I., Rogers P., Bavetsias V., Gorsuch S., Jarman M., Bannister A., Kouzarides T., McDonald E., Workman P., Aherne G.W. Isothiazolones as inhibitors of PCAF and p300 histone acetyltransferase activity. Mol. Cancer Ther. 2005, 4:1521-1532.
9. Biel M., Kretsovali A., Karatzali E., Papamatheakis J., Giannis A. Design, synthesis, and biological evaluation of a small-molecule inhibitor of the histone acetyltransferase Gcn5. Angew. Chem. Intl. Ed. Engl. 2004, 43:3974-3976.
10. Lau O.D., Kundu T.K., Soccio R.E., Ait-Si-Ali S., Khalil E.M., Vassilev A., Wolffe A.P., Nakatani Y., Roeder R.G., Cole P.A. HATs off: selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF. Mol. Cell 2000, 5:589-595.
11. Berndsen C.E., Denu J.M. Assays for mechanistic investigations of protein/histone acetyltransferases. Methods 2005, 36:321-331.
12. Kim Y., Tanner K.G., Denu J.M. A continuous, nonradioactive assay for histone acetyltransferases. Anal. Biochem. 2000, 280:308-314.
13. Trievel R.C., Li F.Y., Marmorstein R. Application of a fluorescent histone acetyltransferase assay to probe the substrate specificity of the human p300/CBP-associated factor. Anal. Biochem. 2000, 287:319-328.
14. Perrin D., Fremaux C., Scheer A. Assay development and screening of a serine/threonine kinase in an on-chip mode using Caliper nanofluidics technology. J. Biomol. Screen. 2006, 11:359-368.
15. Lau O.D., Courtney A.D., Vassilev A., Marzilli L.A., Cotter R.J., Nakatani Y., Cole P.A. P300/CBP-associated factor histone acetyltransferase processing of a peptide substrate: kinetic analysis of the catalytic mechanism. J. Biol. Chem. 2000, 275:21953-21959.