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Role of Histone Methyltransferase in Breast Cancer
Published in Meenu Gupta, Rachna Jain, Arun Solanki, Fadi Al-Turjman, Cancer Prediction for Industrial IoT 4.0: A Machine Learning Perspective, 2021
Surekha Manhas, Zaved Ahmed Khan
Methylation at H3K36 histone protein residue is recognized as an abundant mark of histone that is highly conserved in eukaryotes. In addition, mono/di/trimethylation of H3K36 residue of H3 histone exists in yeast, and all these states of H3K36 are catalyzed through SET2. In the other cases, mammals have all other H3K36 methylation multiple writers, which include SETD2, NSD (1–3) family, SMYD2, ASH1L, and SETMAR, but SETD2 is recognized as the main sole enzyme that is responsible for proceeding the process of trimethylation at H3K36 in vivo [55]). Captivatingly, uncoupling of the activity H3K36me3 from H3K36me (1–2) over evolutionary alludes towards the biologically specified variable roles associated with each state of methylation. In addition, H3K36me3 is mostly associated with the active transcribed specific regions of specific genes and H3K36me3 level increase in the direction of the 30th end of active genes [10].
Small molecule KDM4s inhibitors as anti-cancer agents
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
Hongzhi Lin, Qihang Li, Qi Li, Jie Zhu, Kai Gu, Xueyang Jiang, Qianqian Hu, Feng Feng, Wei Qu, Yao Chen, Haopeng Sun
All the four members of KDM4s subfamily can catalyze the demethylation H3K9me3/2, furthermore, the KDM4A ∼ C can also demonstrated to demethylate H3K36me330. KDM4s have also been demonstrated to H1.4K26me3/231. The positions and states of the methylated marks on histone mostly decide the roles of enzymes in the transcriptional regulation. H3K9me3/2 is a transcriptional suppressive mark that is associated with heterochromatin assembly32,33. The roles of H3K36me3 are indistinct at some level, but it is generally believed that this histone mark inhibits transcription at start but facilitates transcriptional elongation16,34,35. Thus, KDM4s are thought as transcriptional activators. In fact, overexpression of KDM4A indeed promotes genetic transcription in some types of cancers21,22,36. But the relationship between the activity roles of KDM4s and genetic transcription is not very solid: KDM4A directs the repression of E2F responsive promoters37. Additionally, some studies show that KDM4s catalysis is not only limited to demethylation but also to act on N-alkyl groups other than methyl38. Beyond the roles of catalysis, the antagonism between KDM4A and heterochromatin protein 1 gamma (HP1γ) during cell cycle also controls the chromatin accessibility and facilitates transcription39.