Identification of HDAC Inhibitors Using a Cell-Based HDAC I/II Assay

Journal of Biomolecular Screening

Volumn 21, Issue 6, 2016, Pages 643-652

  Hsu, Chia Wen ^a   Shou, David ^a   Huang, Ruili ^a   Khuc, Thai ^a   Dai, Sheng ^a   Zheng, Wei ^a   Klumpp Thomas, Carleen ^a   Xia, Menghang ^a  

^a NATIONAL INSTITUTES OF HEALTH   (United States)

Author keywords

cancer; epigenetics; histone deacetylase; neurodegenerative disease; qHTS

Indexed keywords

6 (1,3 DIOXO 1H,3H BENZO[DE]ISOQUINOLIN 2 YL) N HYDROXYHEXANAMIDE; AMLEXANOX; AR 42; ATALUREN; AXITINIB; DIPHENYL ISOPHTHALATE; ENSULIZOLE; FEBUXOSTAT; HISTONE DEACETYLASE 1; HISTONE DEACETYLASE 10; HISTONE DEACETYLASE 11; HISTONE DEACETYLASE 2; HISTONE DEACETYLASE 3; HISTONE DEACETYLASE 4; HISTONE DEACETYLASE 5; HISTONE DEACETYLASE 6; HISTONE DEACETYLASE 8; HISTONE DEACETYLASE 9; HISTONE DEACETYLASE INHIBITOR; ISOLIQUIRITIGENIN; ISOX; LEFLUNOMIDE; NAFAMSTAT; NICLOSAMIDE; NITAZOXANIDE; PICEATANNOL; PRACINOSTAT; RESVERATROL; TRICHOSTATIN A; UNCLASSIFIED DRUG; VORINOSTAT; HISTONE DEACETYLASE;

ARTICLE; CANCER CELL LINE; CELL ASSAY; CELL BASED HISTONE DEACETYLASE I/II ASSAY; CONTROLLED STUDY; DRUG EFFICACY; DRUG IDENTIFICATION; DRUG POTENCY; EMBRYO; ENZYME ACTIVITY; ENZYME ASSAY; EPIGENETICS; HCT116 CELL LINE; HEK293 CELL LINE; HUMAN; HUMAN CELL; IC50; NEURAL STEM CELL; PRIORITY JOURNAL; ACETYLATION; DRUG EFFECTS; GENE EXPRESSION REGULATION; GENETIC EPIGENESIS; HCT 116 CELL LINE; HIGH THROUGHPUT SCREENING; ISOLATION AND PURIFICATION; METABOLISM; PROCEDURES;

ACETYLATION; EPIGENESIS, GENETIC; GENE EXPRESSION REGULATION; HCT116 CELLS; HIGH-THROUGHPUT SCREENING ASSAYS; HISTONE DEACETYLASE INHIBITORS; HISTONE DEACETYLASES; HUMANS; NEURAL STEM CELLS;

EID: 84975818532     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057116629381     Document Type: Article

References (16)

1. Berdasco M., Esteller M., Genetic Syndromes Caused by Mutations in Epigenetic Genes. Hum. Genet. 2013, 132, 359-383.
2. Chuang D. M., Leng Y., Marinova Z., et al. Multiple Roles of HDAC Inhibition in Neurodegenerative Conditions. Trends Neurosci. 2009, 32, 591-601.
3. Marmorstein R., Structure of Histone Deacetylases: Insights into Substrate Recognition and Catalysis. Structure 2001, 9, 1127-1133.
4. Falkenberg K. J., Johnstone R. W., Histone Deacetylases and Their Inhibitors in Cancer, Neurological Diseases and Immune Disorders. Nat. Rev. Drug Discov. 2014, 13, 673-691.
5. West A. C., Johnstone R. W., New and Emerging HDAC Inhibitors for Cancer Treatment. J. Clin. Invest. 2014, 124, 30-39.
6. Halley F., Reinshagen J., Ellinger B., et al. A Bioluminogenic HDAC Activity Assay: Validation and Screening. J. Biomol. Screen. 2011, 16, 1227-1235.
7. Riester D., Hildmann C., Haus P., et al. Non-Isotopic Dual Parameter Competition Assay Suitable for High-Throughput Screening of Histone Deacetylases. Bioorg. Med. Chem. Lett. 2009, 19, 3651-3656.
8. Mazitschek R., Patel V., Wirth D. F., et al. Development of a Fluorescence Polarization Based Assay for Histone Deacetylase Ligand Discovery. Bioorg. Med. Chem. Lett. 2008, 18, 2809-2812.
9. Riester D., Hildmann C., Schwienhorst A., et al. Histone Deacetylase Inhibitor Assay Based on Fluorescence Resonance Energy Transfer. Anal. Biochem. 2007, 362, 136-141.
10. Wegener D., Hildmann C., Riester D., et al. Improved Fluorogenic Histone Deacetylase Assay for High-Throughput-Screening Applications. Anal. Biochem. 2003, 321, 202-208.
11. Padige G., Negmeldin A. T., Pflum M. K. H., Development of an ELISA-Based HDAC Activity Assay for Characterization of Isoform-Selective Inhibitors. J. Biomol. Screen. 2015, 20, 1277-1285.
12. Ito A., Lai C. H., Zhao X., et al. p300/CBP-Mediated p53 Acetylation Is Commonly Induced by p53-Activating Agents and Inhibited by MDM2. Embo J. 2001, 20, 1331-1340.
13. Ito A., Kawaguchi Y., Lai C. H., et al. MDM2-HDAC1-Mediated Deacetylation of p53 Is Required for Its Degradation. Embo J. 2002, 21, 6236-6245.
14. Barlev N. A., Liu L., Chehab N. H., et al. Acetylation of p53 Activates Transcription through Recruitment of Coactivators/Histone Acetyltransferases. Mol. Cell. 2001, 8, 1243-1254.
15. Mottamal M., Zheng S., Huang T. L., et al. Histone Deacetylase Inhibitors in Clinical Studies as Templates for New Anticancer Agents. Molecules 2015, 20, 3898-3941.
16. Venturelli S., Berger A., Böcker A., et al. Resveratrol as a Pan-HDAC Inhibitor Alters the Acetylation Status of Histone [Corrected] Proteins in Human-Derived Hepatoblastoma Cells. PLoS One 2013, 8, e73097.