Targeting histone methylation for cancer therapy: enzymes, inhibitors, biological activity and perspectives
Abstract Post-translational methylation of histone lysine or arginine residues plays important roles in gene regulation and other physiological processes. Aberrant histone methylation caused by a gene mutation, translocation, or overexpression can often lead to initiation of a disease such as cancer...
| Main Authors: | , , |
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| Format: | Article |
| Language: | English |
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BMC
2016-06-01
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| Series: | Journal of Hematology & Oncology |
| Subjects: | |
| Online Access: | http://link.springer.com/article/10.1186/s13045-016-0279-9 |
| _version_ | 1818131786708811776 |
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| author | Yongcheng Song Fangrui Wu Jingyu Wu |
| author_facet | Yongcheng Song Fangrui Wu Jingyu Wu |
| author_sort | Yongcheng Song |
| collection | DOAJ |
| description | Abstract Post-translational methylation of histone lysine or arginine residues plays important roles in gene regulation and other physiological processes. Aberrant histone methylation caused by a gene mutation, translocation, or overexpression can often lead to initiation of a disease such as cancer. Small molecule inhibitors of such histone modifying enzymes that correct the abnormal methylation could be used as novel therapeutics for these diseases, or as chemical probes for investigation of epigenetics. Discovery and development of histone methylation modulators are in an early stage and undergo a rapid expansion in the past few years. A number of highly potent and selective compounds have been reported, together with extensive preclinical studies of their biological activity. Several compounds have been in clinical trials for safety, pharmacokinetics, and efficacy, targeting several types of cancer. This review summarizes the biochemistry, structures, and biology of cancer-relevant histone methylation modifying enzymes, small molecule inhibitors and their preclinical and clinical antitumor activities. Perspectives for targeting histone methylation for cancer therapy are also discussed. |
| first_indexed | 2024-12-11T08:26:28Z |
| format | Article |
| id | doaj.art-577c11de8b5b4f9faf0c2a6d6b814bf8 |
| institution | Directory Open Access Journal |
| issn | 1756-8722 |
| language | English |
| last_indexed | 2024-12-11T08:26:28Z |
| publishDate | 2016-06-01 |
| publisher | BMC |
| record_format | Article |
| series | Journal of Hematology & Oncology |
| spelling | doaj.art-577c11de8b5b4f9faf0c2a6d6b814bf82022-12-22T01:14:32ZengBMCJournal of Hematology & Oncology1756-87222016-06-019112110.1186/s13045-016-0279-9Targeting histone methylation for cancer therapy: enzymes, inhibitors, biological activity and perspectivesYongcheng Song0Fangrui Wu1Jingyu Wu2Department of Pharmacology, Baylor College of MedicineDepartment of Pharmacology, Baylor College of MedicineDepartment of Pharmacology, Baylor College of MedicineAbstract Post-translational methylation of histone lysine or arginine residues plays important roles in gene regulation and other physiological processes. Aberrant histone methylation caused by a gene mutation, translocation, or overexpression can often lead to initiation of a disease such as cancer. Small molecule inhibitors of such histone modifying enzymes that correct the abnormal methylation could be used as novel therapeutics for these diseases, or as chemical probes for investigation of epigenetics. Discovery and development of histone methylation modulators are in an early stage and undergo a rapid expansion in the past few years. A number of highly potent and selective compounds have been reported, together with extensive preclinical studies of their biological activity. Several compounds have been in clinical trials for safety, pharmacokinetics, and efficacy, targeting several types of cancer. This review summarizes the biochemistry, structures, and biology of cancer-relevant histone methylation modifying enzymes, small molecule inhibitors and their preclinical and clinical antitumor activities. Perspectives for targeting histone methylation for cancer therapy are also discussed.http://link.springer.com/article/10.1186/s13045-016-0279-9Histone methylationEnzyme inhibitorHistone lysine methyltransferaseProtein arginine methyltransferaseHistone demethylaseCancer therapeutics |
| spellingShingle | Yongcheng Song Fangrui Wu Jingyu Wu Targeting histone methylation for cancer therapy: enzymes, inhibitors, biological activity and perspectives Journal of Hematology & Oncology Histone methylation Enzyme inhibitor Histone lysine methyltransferase Protein arginine methyltransferase Histone demethylase Cancer therapeutics |
| title | Targeting histone methylation for cancer therapy: enzymes, inhibitors, biological activity and perspectives |
| title_full | Targeting histone methylation for cancer therapy: enzymes, inhibitors, biological activity and perspectives |
| title_fullStr | Targeting histone methylation for cancer therapy: enzymes, inhibitors, biological activity and perspectives |
| title_full_unstemmed | Targeting histone methylation for cancer therapy: enzymes, inhibitors, biological activity and perspectives |
| title_short | Targeting histone methylation for cancer therapy: enzymes, inhibitors, biological activity and perspectives |
| title_sort | targeting histone methylation for cancer therapy enzymes inhibitors biological activity and perspectives |
| topic | Histone methylation Enzyme inhibitor Histone lysine methyltransferase Protein arginine methyltransferase Histone demethylase Cancer therapeutics |
| url | http://link.springer.com/article/10.1186/s13045-016-0279-9 |
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