The future therapeutic potential of histone demethylases: A critical analysis
- PMID: 19736620
The future therapeutic potential of histone demethylases: A critical analysis
Abstract
Once regarded as an irreversible modification, the methylation of histone protein tails has recently been highlighted following the identification of enzymes capable of histone demethylation in response to developmental or environmental cues. An awareness of the dynamic nature of histone modification has stimulated interest in the concept that drugs targeting histone methylation/demethylation might provide treatments for cancer, inflammation and metabolic disorders. However, epigenetic therapies that target histone demethylation are at the concept stage. Histone demethylases and their potential as therapeutic targets are discussed in this review.
Similar articles
-
The emerging therapeutic potential of histone methyltransferase and demethylase inhibitors.ChemMedChem. 2009 Oct;4(10):1568-82. doi: 10.1002/cmdc.200900301. ChemMedChem. 2009. PMID: 19739196 Review.
-
Targeting histone lysine demethylases by truncating the histone 3 tail to obtain selective substrate-based inhibitors.Angew Chem Int Ed Engl. 2011 Sep 19;50(39):9100-3. doi: 10.1002/anie.201101849. Epub 2011 Aug 25. Angew Chem Int Ed Engl. 2011. PMID: 21919140 No abstract available.
-
Epigenetic cancer therapy: Proof of concept and remaining challenges.Bioessays. 2010 Nov;32(11):949-57. doi: 10.1002/bies.201000061. Bioessays. 2010. PMID: 21154865 Review.
-
Structure and function of histone H3 lysine 9 methyltransferases and demethylases.Chembiochem. 2011 Jan 24;12(2):254-63. doi: 10.1002/cbic.201000545. Epub 2011 Jan 5. Chembiochem. 2011. PMID: 21243713 Review.
-
Development of homogeneous nonradioactive methyltransferase and demethylase assays targeting histone H3 lysine 4.J Biomol Screen. 2012 Jan;17(1):49-58. doi: 10.1177/1087057111416659. Epub 2011 Sep 21. J Biomol Screen. 2012. PMID: 21940714
Cited by
-
A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases.J Am Chem Soc. 2011 Jun 22;133(24):9451-6. doi: 10.1021/ja201597b. Epub 2011 May 31. J Am Chem Soc. 2011. PMID: 21585201 Free PMC article.
-
Is JmjC oxygenase catalysis limited to demethylation?Angew Chem Int Ed Engl. 2013 Jul 22;52(30):7709-13. doi: 10.1002/anie.201303282. Epub 2013 Jun 20. Angew Chem Int Ed Engl. 2013. PMID: 23788451 Free PMC article.
-
Computer-aided Molecular Design of Compounds Targeting Histone Modifying Enzymes.Comput Struct Biotechnol J. 2015 May 7;13:358-65. doi: 10.1016/j.csbj.2015.04.007. eCollection 2015. Comput Struct Biotechnol J. 2015. PMID: 26082827 Free PMC article. Review.
-
Pharmacological levels of Withaferin A (Withania somnifera) trigger clinically relevant anticancer effects specific to triple negative breast cancer cells.PLoS One. 2014 Feb 3;9(2):e87850. doi: 10.1371/journal.pone.0087850. eCollection 2014. PLoS One. 2014. PMID: 24498382 Free PMC article.
-
The pharmacological role of histone demethylase JMJD3 inhibitor GSK-J4 on glioma cells.Oncotarget. 2017 Aug 2;8(40):68591-68598. doi: 10.18632/oncotarget.19793. eCollection 2017 Sep 15. Oncotarget. 2017. PMID: 28978140 Free PMC article.
Publication types
MeSH terms
Substances
LinkOut - more resources
Medical