AI Article Synopsis
- Histone methylation is a key part of epigenetics, involving enzymes like G9a that modify histones and regulate DNA processes such as replication and gene expression.
- Overexpression of G9a is linked to cancer development and progression, making it an appealing target for new cancer therapies.
- Research is also uncovering the role of G9a in diseases like Alzheimer's, leading to the development of G9a inhibitors that could treat various conditions by disrupting harmful signaling pathways.
Article Abstract
Histone methylation, a crucial aspect of epigenetics, intricately involves specialized enzymes such as G9a, a histone methyltransferase (HMT) catalyzing the methylation of histone H3 lysine 9 (H3K9) and H3K27. Apart from histone modification, G9a regulates essential cellular processes such as deoxyribonucleic acid (DNA) replication, damage repair, and gene expression via modulating DNA methylation patterns. The dysregulation and overexpression of G9a are intricately linked to cancer initiation, progression, and metastasis, making it a compelling target for anticancer therapy. Moreover, aberrant levels of H3K9 dimethylation were identified in Alzheimer's disease (AD), broadening the scope of epigenetic implications across various pathologies. The quest for potent therapy has resulted in the identification of numerous G9a inhibitors/degraders, each demonstrating the potential to disrupt aberrant signaling pathways. This perspective provides valuable insights into the evolving potential and advancement of G9a modulators as promising candidates for treating a spectrum of diseases.
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| http://dx.doi.org/10.1021/acs.jmedchem.4c02474 | DOI Listing |
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