- About this Journal ·
- Abstracting and Indexing ·
- Aims and Scope ·
- Annual Issues ·
- Article Processing Charges ·
- Articles in Press ·
- Author Guidelines ·
- Bibliographic Information ·
- Citations to this Journal ·
- Contact Information ·
- Editorial Board ·
- Editorial Workflow ·
- Free eTOC Alerts ·
- Publication Ethics ·
- Reviewers Acknowledgment ·
- Submit a Manuscript ·
- Subscription Information ·
- Table of Contents
Journal of Biomedicine and Biotechnology
Volume 2011 (2011), Article ID 868095, 11 pages
Identification of Four Potential Epigenetic Modulators from the NCI Structural Diversity Library Using a Cell-Based Assay
1Department of Pharmacology and Hamon Center for Therapeutic Oncology Research, UT Southwestern Medical Center, 6000 Harry Hines Boulevard, Dallas, TX 75390, USA
2Molecular Targets Laboratory, Center for SAIC-Frederick, National Cancer Institute, Frederick, MD 21702, USA
3Molecular Targets Laboratory, Center for Cancer Research, National Cancer Institute, Boulevard, Dallas, TX 75390, USA
Received 29 July 2010; Accepted 7 October 2010
Academic Editor: Minoru Yoshida
Copyright © 2011 Anne M. Best et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
- P. A. Jones and S. B. Baylin, “The epigenomics of cancer,” Cell, vol. 128, no. 4, pp. 683–692, 2007.
- A. Fucito, C. Lucchetti, A. Giordano, and G. Romano, “Genetic and epigenetic alterations in breast cancer: what are the perspectives for clinical practice?” International Journal of Biochemistry and Cell Biology, vol. 40, no. 4, pp. 565–575, 2008.
- Y. Huang, E. Greene, T. M. Stewart et al., “Inhibition of lysine-specific demethylase 1 by polyamine analogues results in reexpression of aberrantly silenced genes,” Proceedings of the National Academy of Sciences of the United States of America, vol. 104, no. 19, pp. 8023–8028, 2007.
- H. Santos-Rosa and C. Caldas, “Chromatin modifier enzymes, the histone code and cancer,” European Journal of Cancer, vol. 41, no. 16, pp. 2381–2402, 2005.
- M. Candelaria, D. Gallardo-Rincón, C. Arce et al., “A phase II study of epigenetic therapy with hydralazine and magnesium valproate to overcome chemotherapy resistance in refractory solid tumors,” Annals of Oncology, vol. 18, no. 9, pp. 1529–1538, 2007.
- S. Grant, C. Easley, and P. Kirkpatrick, “Vorinostat,” Nature Reviews Drug Discovery, vol. 6, no. 1, pp. 21–22, 2007.
- Q. C. Ryan, D. Headlee, M. Acharya et al., “Phase I and pharmacokinetic study of MS-275, a histone deacetylase inhibitor, in patients with advanced and refractory solid tumors or lymphoma,” Journal of Clinical Oncology, vol. 23, no. 17, pp. 3912–3922, 2005.
- O. Khan and N. B. La Thangue, “Drug Insight: histone deacetylase inhibitor-based therapies for cutaneous T-cell lymphomas,” Nature Clinical Practice Oncology, vol. 5, no. 12, pp. 714–726, 2008.
- D. M. Vigushin and R. C. Coombes, “Histone deacetylase inhibitors in cancer treatment,” Anti-Cancer Drugs, vol. 13, no. 1, pp. 1–13, 2002.
- H. Nakajima, Y. B. Kim, H. Terano, M. Yoshida, and S. Horinouchi, “FR901228, a potent antitumor antibiotic, is a novel histone deacetylase inhibitor,” Experimental Cell Research, vol. 241, no. 1, pp. 126–133, 1998.
- V. M. Richon, Y. Webb, R. Merger et al., “Second generation hybrid polar compounds are potent inducers of transformed cell differentiation,” Proceedings of the National Academy of Sciences of the United States of America, vol. 93, no. 12, pp. 5705–5708, 1996.
- O. D. Lau, T. K. Kundu, R. E. Soccio et al., “HATs off: selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF,” Molecular Cell, vol. 5, no. 3, pp. 589–595, 2000.
- A. Bedalov, T. Gatbonton, W. P. Irvine, D. E. Gottschling, and J. A. Simon, “Identification of a small molecule inhibitor of Sir2p,” Proceedings of the National Academy of Sciences of the United States of America, vol. 98, no. 26, pp. 15113–15118, 2001.
- C. M. Grozinger, E. D. Chao, H. E. Blackwell, D. Moazed, and S. L. Schreiber, “Identification of a class of small molecule inhibitors of the sirtuin family of NAD-dependent deacetylases by phenotypic screening,” Journal of Biological Chemistry, vol. 276, no. 42, pp. 38837–38843, 2001.
- S. Kubicek, R. J. O'Sullivan, E. M. August et al., “Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase,” Molecular Cell, vol. 25, no. 3, pp. 473–481, 2007.
- A. M. Quinn, A. Allali-Hassani, M. Vedadi, and A. Simeonov, “A chemiluminescence-based method for identification of histone lysine methyltransferase inhibitors,” Molecular BioSystems, vol. 6, no. 5, pp. 782–788, 2010.
- A. Dhayalan, E. Dimitrova, P. Rathert, and A. Jeltsch, “A continuous protein methyltransferase (G9a) assay for enzyme activity measurement and inhibitor screening,” Journal of Biomolecular Screening, vol. 14, no. 9, pp. 1129–1133, 2009.
- M. Yoshida, M. Kijima, M. Akita, and T. Beppu, “Potent and specific inhibition of mammalian histone deacetylase both in vivo and in vitro by trichostatin A,” Journal of Biological Chemistry, vol. 265, no. 28, pp. 17174–17179, 1990.
- S. J. Haggarty, K. M. Koeller, J. C. Wong, R. A. Butcher, and S. L. Schreiber, “Multidimensional chemical genetic analysis of diversity-oriented synthesis-derived deacetylase inhibitors using cell-based assays,” Chemistry and Biology, vol. 10, no. 5, pp. 383–396, 2003.
- S. J. Haggarty, K. M. Koeller, J. C. Wong, C. M. Grozinger, and S. L. Schreiber, “Domain-selective small-molecule inhibitor of histone deacetylase 6 (HDAC6)-mediated tubulin deacetylation,” Proceedings of the National Academy of Sciences of the United States of America, vol. 100, no. 8, pp. 4389–4394, 2003.
- S. W. Remiszewski, L. C. Sambucetti, K. W. Bair et al., “N-Hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activitydiscovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl] amino]methyl]-phenyl]-2-propenamide (NVP-LAQ824),” Journal of Medicinal Chemistry, vol. 46, no. 21, pp. 4609–4624, 2003.
- J. Tan, S. Cang, Y. Ma, R. L. Petrillo, and D. Liu, “Novel histone deacetylase inhibitors in clinical trials as anti-cancer agents,” Journal of Hematology and Oncology, vol. 3, article 5, 2010.
- E. Kaminskas, A. T. Farrell, Y.-C. Wang, R. Sridhara, and R. Pazdur, “FDA drug approval summary: azacitidine (5-azacytidine, Vidaza) for injectable suspension,” Oncologist, vol. 10, no. 3, pp. 176–182, 2005.
- B. S. Mann, J. R. Johnson, M. H. Cohen, R. Justice, and R. Pazdur, “FDA approval summary: vorinostat for treatment of advanced primary cutaneous T-cell lymphoma,” Oncologist, vol. 12, no. 10, pp. 1247–1252, 2007.
- S. D. Gore, C. Jones, and P. Kirkpatrick, “Decitabine,” Nature Reviews Drug Discovery, vol. 5, no. 11, pp. 891–892, 2006.
- C. Grant, F. Rahman, R. Piekarz et al., “Romidepsin: a new therapy for cutaneous T-cell lymphoma and a potential therapy for solid tumors,” Expert Review of Anticancer Therapy, vol. 10, no. 7, pp. 997–1008, 2010.
- E. D. Martinez, A. B. Dull, J. A. Beutler, and G. L. Hager, “High-content fluorescence-based screening for epigenetic modulators,” Methods in Enzymology, vol. 414, pp. 21–36, 2006.
- E. D. Martinez and G. L. Hager, “Development of assays for nuclear receptor modulators using fluorescently tagged proteins,” Methods in Enzymology, vol. 414, pp. 37–50, 2006.
- R. L. Johnson, W. Huang, A. Jadhav, C. P. Austin, J. Inglese, and E. D. Martinez, “A quantitative high-throughput screen identifies potential epigenetic modulators of gene expression,” Analytical Biochemistry, vol. 375, no. 2, pp. 237–248, 2008.
- U. M. Hanumegowda, V. C. Dhulipala, and C. S. Reddy, “Mechanism of secalonic acid D-induced inhibition of transcription factor binding to cyclic AMP response element in the developing murine palate,” Toxicological Sciences, vol. 70, no. 1, pp. 55–62, 2002.
- D. Mottet and V. Castronovo, “Histone deacetylases: target enzymes for cancer therapy,” Clinical and Experimental Metastasis, vol. 25, no. 2, pp. 183–189, 2008.
- M. Szyf, “Epigenetics, DNA methylation, and chromatin modifying drugs,” Annual Review of Pharmacology and Toxicology, vol. 49, pp. 243–263, 2009.
- A. F. Gazdar, B. Gao, and J. D. Minna, “Lung cancer cell lines: useless artifacts or invaluable tools for medical science?” Lung Cancer, vol. 68, no. 3, pp. 309–318, 2010.
- Y.-G. He, E. Mayhew, J. Mellon, and J. Y. Niederkorn, “Expression and possible function of IL-2 and IL-15 receptors on human uveal melanoma cells,” Investigative Ophthalmology and Visual Science, vol. 45, no. 12, pp. 4240–4246, 2004.
- S. B. Hake and C. D. Allis, “Histone H3 variants and their potential role in indexing mammalian genomes: the “H3 barcode hypothesis”,” Proceedings of the National Academy of Sciences of the United States of America, vol. 103, no. 17, pp. 6428–6435, 2006.