Journal article
Polyamine-based small molecule epigenetic modulators
MedChemComm, Vol.3(1), pp.14-21
01/01/2012
DOI: 10.1039/c1md00220a
PMCID: PMC3535317
PMID: 23293738
Abstract
Chromatin remodelling enzymes such as the histone deacetylases (HDACs) and histone demethylases such as lysine-specific demethylase 1 (LSD1) have been validated as targets for cancer drug discovery. Although a number of HDAC inhibitors have been marketed or are in human clinical trials, the search for isoform-specific HDAC inhibitors is an ongoing effort. In addition, the discovery and development of compounds targeting histone demethylases are in their early stages. Epigenetic modulators used in combination with traditional antitumor agents such as 5-azacytidine represent an exciting new approach to cancer chemotherapy. We have developed multiple series of HDAC inhibitors and LSD1 inhibitors that promote the re-expression of aberrantly silenced genes that are important in human cancer. The design, synthesis and biological activity of these analogues is described herein.
Details
- Title: Subtitle
- Polyamine-based small molecule epigenetic modulators
- Creators
- Shiv K. Sharma - Wayne State UniversityStuart Hazeldine - Wayne State UniversityMichael L. Crowley - Wayne State UniversityAllison Hanson - Wayne State UniversityRoss Beattie - Wayne State UniversitySheeba Varghese - Wayne State UniversityThulani M. D. Senanayake - Wayne State UniversityAiko Hirata - Wayne State UniversityFusao Hirata - Wayne State UniversityYi Huang - Sidney Kimmel Comprehensive Cancer CenterYu Wu - Johns Hopkins UniversityNora Steinbergs - Sidney Kimmel Comprehensive Cancer CenterTracey Murray-Stewart - Sidney Kimmel Comprehensive Cancer CenterIan Bytheway - Ligand Pharmaceuticals (United Kingdom)Robert A. Casero - Sidney Kimmel Comprehensive Cancer CenterPatrick M. Woster - Medical University of South Carolina
- Resource Type
- Journal article
- Publication Details
- MedChemComm, Vol.3(1), pp.14-21
- DOI
- 10.1039/c1md00220a
- PMID
- 23293738
- PMCID
- PMC3535317
- NLM abbreviation
- Medchemcomm
- ISSN
- 2040-2503
- eISSN
- 2040-2511
- Publisher
- Royal Soc Chemistry
- Number of pages
- 8
- Grant note
- R01CA149095 / NATIONAL CANCER INSTITUTE; United States Department of Health & Human Services; National Institutes of Health (NIH) - USA; NIH National Cancer Institute (NCI) 5RO1 CA149095 / NIH; United States Department of Health & Human Services; National Institutes of Health (NIH) - USA
- Language
- English
- Date published
- 01/01/2012
- Academic Unit
- Internal Medicine
- Record Identifier
- 9984383924102771
Metrics
10 Record Views