Potential Therapeutics Targeting Upstream Regulators and Interactors of EHMT1/2
Euchromatin histone lysine methyltransferases (EHMTs) are epigenetic regulators responsible for silencing gene transcription by catalyzing H3K9 dimethylation. Dysregulation of EHMT1/2 has been reported in multiple cancers and is associated with poor clinical outcomes. Although substantial insights h...
| Main Authors: | , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2022-06-01
|
| Series: | Cancers |
| Subjects: | |
| Online Access: | https://www.mdpi.com/2072-6694/14/12/2855 |
| _version_ | 1797489167546974208 |
|---|---|
| author | Gareth Chin Khye Ang Amogh Gupta Shirlyn Xue Ling Yap Uttam Surana Reshma Taneja |
| author_facet | Gareth Chin Khye Ang Amogh Gupta Shirlyn Xue Ling Yap Uttam Surana Reshma Taneja |
| author_sort | Gareth Chin Khye Ang |
| collection | DOAJ |
| description | Euchromatin histone lysine methyltransferases (EHMTs) are epigenetic regulators responsible for silencing gene transcription by catalyzing H3K9 dimethylation. Dysregulation of EHMT1/2 has been reported in multiple cancers and is associated with poor clinical outcomes. Although substantial insights have been gleaned into the downstream targets and pathways regulated by EHMT1/2, few studies have uncovered mechanisms responsible for their dysregulated expression. Moreover, EHMT1/2 interacting partners, which can influence their function and, therefore, the expression of target genes, have not been extensively explored. As none of the currently available EHMT inhibitors have made it past clinical trials, understanding upstream regulators and EHMT protein complexes may provide unique insights into novel therapeutic avenues in EHMT-overexpressing cancers. Here, we review our current understanding of the regulators and interacting partners of EHMTs. We also discuss available therapeutic drugs that target the upstream regulators and binding partners of EHMTs and could potentially modulate EHMT function in cancer progression. |
| first_indexed | 2024-03-10T00:13:38Z |
| format | Article |
| id | doaj.art-0291aba029a3400da4140c240dc20c98 |
| institution | Directory Open Access Journal |
| issn | 2072-6694 |
| language | English |
| last_indexed | 2024-03-10T00:13:38Z |
| publishDate | 2022-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Cancers |
| spelling | doaj.art-0291aba029a3400da4140c240dc20c982023-11-23T15:55:21ZengMDPI AGCancers2072-66942022-06-011412285510.3390/cancers14122855Potential Therapeutics Targeting Upstream Regulators and Interactors of EHMT1/2Gareth Chin Khye Ang0Amogh Gupta1Shirlyn Xue Ling Yap2Uttam Surana3Reshma Taneja4Healthy Longevity Translational Research Program, Department of Physiology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore 117593, SingaporeHealthy Longevity Translational Research Program, Department of Physiology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore 117593, SingaporeDepartment of Medicine, Yong Loo Lin School of Medicine, National University of Singapore, Singapore 119228, SingaporeDepartment of Pharmacology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore 117593, SingaporeHealthy Longevity Translational Research Program, Department of Physiology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore 117593, SingaporeEuchromatin histone lysine methyltransferases (EHMTs) are epigenetic regulators responsible for silencing gene transcription by catalyzing H3K9 dimethylation. Dysregulation of EHMT1/2 has been reported in multiple cancers and is associated with poor clinical outcomes. Although substantial insights have been gleaned into the downstream targets and pathways regulated by EHMT1/2, few studies have uncovered mechanisms responsible for their dysregulated expression. Moreover, EHMT1/2 interacting partners, which can influence their function and, therefore, the expression of target genes, have not been extensively explored. As none of the currently available EHMT inhibitors have made it past clinical trials, understanding upstream regulators and EHMT protein complexes may provide unique insights into novel therapeutic avenues in EHMT-overexpressing cancers. Here, we review our current understanding of the regulators and interacting partners of EHMTs. We also discuss available therapeutic drugs that target the upstream regulators and binding partners of EHMTs and could potentially modulate EHMT function in cancer progression.https://www.mdpi.com/2072-6694/14/12/2855lysine methyltransferasesupstream regulatorsinteractomepost-translational modificationstherapeutics |
| spellingShingle | Gareth Chin Khye Ang Amogh Gupta Shirlyn Xue Ling Yap Uttam Surana Reshma Taneja Potential Therapeutics Targeting Upstream Regulators and Interactors of EHMT1/2 Cancers lysine methyltransferases upstream regulators interactome post-translational modifications therapeutics |
| title | Potential Therapeutics Targeting Upstream Regulators and Interactors of EHMT1/2 |
| title_full | Potential Therapeutics Targeting Upstream Regulators and Interactors of EHMT1/2 |
| title_fullStr | Potential Therapeutics Targeting Upstream Regulators and Interactors of EHMT1/2 |
| title_full_unstemmed | Potential Therapeutics Targeting Upstream Regulators and Interactors of EHMT1/2 |
| title_short | Potential Therapeutics Targeting Upstream Regulators and Interactors of EHMT1/2 |
| title_sort | potential therapeutics targeting upstream regulators and interactors of ehmt1 2 |
| topic | lysine methyltransferases upstream regulators interactome post-translational modifications therapeutics |
| url | https://www.mdpi.com/2072-6694/14/12/2855 |
| work_keys_str_mv | AT garethchinkhyeang potentialtherapeuticstargetingupstreamregulatorsandinteractorsofehmt12 AT amoghgupta potentialtherapeuticstargetingupstreamregulatorsandinteractorsofehmt12 AT shirlynxuelingyap potentialtherapeuticstargetingupstreamregulatorsandinteractorsofehmt12 AT uttamsurana potentialtherapeuticstargetingupstreamregulatorsandinteractorsofehmt12 AT reshmataneja potentialtherapeuticstargetingupstreamregulatorsandinteractorsofehmt12 |