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Cancer epigenetics drug discovery and development: the challenge of hitting the mark.
- Source :
-
The Journal of clinical investigation [J Clin Invest] 2014 Jan; Vol. 124 (1), pp. 64-9. Date of Electronic Publication: 2014 Jan 02. - Publication Year :
- 2014
-
Abstract
- Over the past several years, there has been rapidly expanding evidence of epigenetic dysregulation in cancer, in which histone and DNA modification play a critical role in tumor growth and survival. These findings have gained the attention of the drug discovery and development community, and offer the potential for a second generation of cancer epigenetic agents for patients following the approved "first generation" of DNA methylation (e.g., Dacogen, Vidaza) and broad-spectrum HDAC inhibitors (e.g., Vorinostat, Romidepsin). This Review provides an analysis of prospects for discovery and development of novel cancer agents that target epigenetic proteins. We will examine key examples of epigenetic dysregulation in tumors as well as challenges to epigenetic drug discovery with emerging biology and novel classes of drug targets. We will also highlight recent successes in cancer epigenetics drug discovery and consider important factors for clinical success in this burgeoning area.
- Subjects :
- Animals
Antineoplastic Agents therapeutic use
Clinical Trials as Topic
Drug Discovery
Drug Screening Assays, Antitumor
Enhancer of Zeste Homolog 2 Protein
Gene Expression Regulation, Neoplastic drug effects
Histone-Lysine N-Methyltransferase
Humans
Methyltransferases antagonists & inhibitors
Molecular Targeted Therapy
Neoplasms genetics
Point Mutation
Polycomb Repressive Complex 2 antagonists & inhibitors
Antineoplastic Agents pharmacology
Epigenesis, Genetic
Neoplasms drug therapy
Subjects
Details
- Language :
- English
- ISSN :
- 1558-8238
- Volume :
- 124
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- The Journal of clinical investigation
- Publication Type :
- Academic Journal
- Accession number :
- 24382391
- Full Text :
- https://doi.org/10.1172/JCI71605