High-throughput screening for identification of small molecule inhibitors of histone acetyltransferases using scintillating microplates (FlashPlate)

Analytical Biochemistry

Volumn 298, Issue 1, 2001, Pages 62-68

  Turlais, F ^a   Hardcastle, Anthea ^a   Rowlands, M ^a   Newbatt, Yvette ^a   Bannister, A ^b   Kouzarides, T ^b   Workman, P ^a   Aherne, G Wynne ^a  

^a INSTITUTE OF CANCER RESEARCH   (United Kingdom)

^b WELLCOME CRC INSTITUTE   (United Kingdom)

Author keywords

Acetyltransferase; Drug discovery; Histone; HTS screen

Indexed keywords

ENZYMES; MOLECULES; RECOMBINANT PROTEINS; SCINTILLATION; SIGNAL TO NOISE RATIO; TRANSCRIPTION;

ACETYL TRANSFERASE; DRUG DISCOVERY; GLUTATHIONE S-TRANSFERASES; HIGH THROUGHPUT SCREENING; HISTONE; HISTONE ACETYLTRANSFERASES; SCINTILLATION SIGNALS; SMALL MOLECULE INHIBITOR;

DRUG PRODUCTS;

ACETYL COENZYME A; BINDING PROTEIN; CYCLIC AMP RESPONSIVE ELEMENT BINDING PROTEIN; ENZYME INHIBITOR; GLUTATHIONE TRANSFERASE; HISTONE ACETYLTRANSFERASE; HISTONE ANTIBODY; HISTONE H3; HYBRID PROTEIN; PROTEIN P300; RECOMBINANT ENZYME; TRITIUM;

ARTICLE; AUTOMATION; DEVICE; ENZYME ACTIVITY; ENZYME ASSAY; ENZYME INHIBITION; ISOTOPE LABELING; PRIORITY JOURNAL; REPRODUCIBILITY; SCINTILLATION; SCREENING TEST; SIGNAL DETECTION; SIGNAL NOISE RATIO; VALIDATION PROCESS;

EID: 0035499141     PISSN: 00032697     EISSN: None     Source Type: Journal    
DOI: 10.1006/abio.2001.5340     Document Type: Article

References (31)

1. Histone acetylases and deacetylases in cell proliferation
2. Acetylation: A regulatory modification to rival phosphorylation?
3. Acetylation of general transcription factors by histone acetyltransferase
4. Differential roles of p300 and PCAF acetyltransferases in muscle differentiation
5. P300 is required for MyoD-dependent cell cycle arrest and muscle specific gene transcription
6. E1A directly binds and regulates the PCAF acetyltransferase
7. Regulation of E2F1 activity by acetylation
8. Activation of p53 sequence specific DNA binding by acetylation of p53 C-terminal domain
9. p53 sites acetylated in vitro by PCAF and p300 are acetylated in vivo in response to DNA damage
10. The language of covalent histone modifications
11. Gene dosage-dependent embryonic development and proliferation defects in mice lacking the transcriptional integrator p300
12. Function for p300 and not CBP in the apoptotic response to DNA damage
13. The translocation of acute myeloid leukaemia fuses a putative acetyltransferase to the CREB-binding protein
14. Adenovirus E1A-associated protein p300 is involved in acute myeloid leukaemia with t(11:22)
15. MLL is fused to CBP, a histone acetyl transferase in therapy-related acute myeloid leukemia with a t(11.,16)(q23:p13.3)
16. Mutations truncating the EP300 acetylase in human cancers
17. p300 gene alterations in colorectal and gastric carcinomas
18. ALB1, a steriod receptor co-activator amplified in breast and ovarian cancer
19. DNA tumour virus transforming proteins and the cell cycle
20. Potent and specific inhibition of mammalian histone deacetylase both in vivo and in vitro by Trichostatin A
21. A synthetic inhibitor of histone deacteylase, MS-27-275, with marked in vivo antitumour activity against human tumours
22. Trichostatin A and Trapoxin: Novel chemical probes for role of histone acetylation in chromatin structure and function
23. Selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF
24. Development of a scintillation proximity assay for histone deacetylase using a biotinylated peptide derived from histone-H4
25. A non-isotopic assay for histone deacetylase activity
26. A rapid and sensitive assay for acetyl-transferase activity
27. A continuous, non-radioactive assay for histone acetyltransferases
28. The CBP co-activator is a histone acetyltransferase
29. A simple statistical parameter for use in evaluation and validation of HTS assays
30. Binding of protein to polystyrene in solid-phase immunoassays
31. Homogeneous purification of human recombinant GST Akt/PKB from Sf9 cells