This Article Full Text Full Text (PDF) Alert me when this article is cited Alert me if a correction is posted Services Similar articles in this journal Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Citing Articles Citing Articles via HighWire Citing Articles via Google Scholar Google Scholar Articles by Gilbert, J. Articles by Carducci, M. A. Search for Related Content PubMed PubMed Citation Articles by Gilbert, J. Articles by Carducci, M. A. Related Collections Therapeutics and Targets Therapeutics and Targets: Identification, Validation, and Markers

The Clinical Application of Targeting Cancer through Histone Acetylation and Hypomethylation

¹ Division of Oncology and Hematology, Stanley S. Scott Cancer Center, Louisiana State University, New Orleans, Louisiana, and Divisions of ² Hematologic Malignancies, ³ Cancer Biology, and ⁴ Medical Oncology, Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, Baltimore, Maryland

Methods of gene inactivation include genetic events such as mutations or deletions. Epigenetic changes, heritable traits that are mediated by changes in DNA other than nucleotide sequences, play an important role in gene expression. Two epigenetic events that have been associated with transcriptional silencing include methylation of CpG islands located in gene promoter regions of cancer cells and changes in chromatin conformation involving histone acetylation. Recent evidence demonstrates that these processes form layers of epigenetic silencing. Reversal of these epigenetic processes and up-regulation of genes important to prevent or reverse the malignant phenotype has therefore become a new therapeutic target in cancer treatment.

This article has been cited by other articles:

				E. De Bruyne, T. J. Bos, K. Asosingh, I. Vande Broek, E. Menu, E. Van Valckenborgh, P. Atadja, V. Coiteux, X. Leleu, K. Thielemans, et al. Epigenetic Silencing of the Tetraspanin CD9 during Disease Progression in Multiple Myeloma Cells and Correlation with Survival Clin. Cancer Res., May 15, 2008; 14(10): 2918 - 2926. [Abstract] [Full Text] [PDF]

				A. Hadnagy, R. Beaulieu, and D. Balicki Histone tail modifications and noncanonical functions of histones: perspectives in cancer epigenetics Mol. Cancer Ther., April 1, 2008; 7(4): 740 - 748. [Abstract] [Full Text] [PDF]

				F. Barlesi, G. Giaccone, M. I. Gallegos-Ruiz, A. Loundou, S. W. Span, P. Lefesvre, F. A.E. Kruyt, and J. A. Rodriguez Global Histone Modifications Predict Prognosis of Resected Non Small-Cell Lung Cancer J. Clin. Oncol., October 1, 2007; 25(28): 4358 - 4364. [Abstract] [Full Text] [PDF]

				I. Gojo, A. Jiemjit, J. B. Trepel, A. Sparreboom, W. D. Figg, S. Rollins, M. L. Tidwell, J. Greer, E. J. Chung, M.-J. Lee, et al. Phase 1 and pharmacologic study of MS-275, a histone deacetylase inhibitor, in adults with refractory and relapsed acute leukemias Blood, April 1, 2007; 109(7): 2781 - 2790. [Abstract] [Full Text] [PDF]

				L. C. Hsi, X. Xi, Y. Wu, and S. M. Lippman The methyltransferase inhibitor 5-aza-2-deoxycytidine induces apoptosis via induction of 15-lipoxygenase-1 in colorectal cancer cells Mol. Cancer Ther., November 1, 2005; 4(11): 1740 - 1746. [Abstract] [Full Text] [PDF]

				E. J. Chung, S. Lee, E. A. Sausville, Q. Ryan, J. E. Karp, I. Gojo, W. G. Telford, M.-J. Lee, H. S. Kong, and J. B. Trepel Histone Deacetylase Inhibitor Pharmacodynamic Analysis by Multiparameter Flow Cytometry Ann. Clin. Lab. Sci., October 1, 2005; 35(4): 397 - 406. [Abstract] [Full Text] [PDF]

				D. Sharma, J. Blum, X. Yang, N. Beaulieu, A. R. Macleod, and N. E. Davidson Release of Methyl CpG Binding Proteins and Histone Deacetylase 1 from the Estrogen Receptor {alpha} (ER) Promoter upon Reactivation in ER-Negative Human Breast Cancer Cells Mol. Endocrinol., July 1, 2005; 19(7): 1740 - 1751. [Abstract] [Full Text] [PDF]

				M. A. Rudek, M. Zhao, P. He, C. Hartke, J. Gilbert, S. D. Gore, M. A. Carducci, and S. D. Baker Pharmacokinetics of 5-Azacitidine Administered With Phenylbutyrate in Patients With Refractory Solid Tumors or Hematologic Malignancies J. Clin. Oncol., June 10, 2005; 23(17): 3906 - 3911. [Abstract] [Full Text] [PDF]

				K. N. Bhalla Epigenetic and Chromatin Modifiers As Targeted Therapy of Hematologic Malignancies J. Clin. Oncol., June 10, 2005; 23(17): 3971 - 3993. [Abstract] [Full Text] [PDF]

				J. L. Holleran, R. A. Parise, E. Joseph, J. L. Eiseman, J. M. Covey, E. R. Glaze, A. V. Lyubimov, Y.-F. Chen, D. Z. D'Argenio, and M. J. Egorin Plasma Pharmacokinetics, Oral Bioavailability, and Interspecies Scaling of the DNA Methyltransferase Inhibitor, Zebularine Clin. Cancer Res., May 15, 2005; 11(10): 3862 - 3868. [Abstract] [Full Text] [PDF]

				C. J. Fabian and B. F. Kimler Selective Estrogen-Receptor Modulators for Primary Prevention of Breast Cancer J. Clin. Oncol., March 10, 2005; 23(8): 1644 - 1655. [Full Text] [PDF]

				N. P. Mongan and L. J. Gudas Valproic acid, in combination with all-trans retinoic acid and 5-aza-2'-deoxycytidine, restores expression of silenced RAR{beta}2 in breast cancer cells Mol. Cancer Ther., March 1, 2005; 4(3): 477 - 486. [Abstract] [Full Text] [PDF]