TABLE 1.
Summary of H3 methylation master regulators considered as potential therapeutic targets in PCa.
| Enzyme type | Enzyme name | PTMs | Function in PCa | References |
|---|---|---|---|---|
| HMTs | SMYD3 | H3K4me2/3 | Promotes cell proliferation and migration | Vieira et al. (2015) |
| SUV39H1 | H3K9me3 | Enhance prostate cancer cell and migration | Baratchian et al. (2022) | |
| G9a | H3K9me2 | Contributes to the development of PCa | Chen et al. (2012) | |
| Jones et al. (2021) | ||||
| EZH2 | H3K27me2/3 | Crucial key driver of prostate cancer development | Yang and Yu (2013) | |
| Abida et al. (2019) | ||||
| NSD2 | H3K36me2 | Promotes prostate cancer tumorigenesis and progression. | Ezponda et al. (2013) | |
| DOT1L | H3K79me2/3 | Is necessary for the viability of AR+ PCa | Vatapalli et al. (2020) | |
| PRMT4 (CARM1) | H3R17me2a | Overexpressed in prostate cancer. Associated with tumorigenesis and cancer progression | Hong et al. (2004) | |
| PRMT5 | H3R8me2a | Promotes development of CRPC | Beketova et al. (2022) | |
| PRMT6 | H3R2/17/42me2a | Overexpressed in prostate cancer | Vieira et al. (2014) | |
| HDMs | KDM5B (JARID1B) | H3K4me1/2/3 | AR coactivator. Upregulated in PCa | Khan et al. (2019) |
| KDM5C (JARID1C) | H3K4me2/3 | Controls the proliferation of prostate cancer cells; might represent a novel therapeutic target. | Stein et al. (2014) | |
| JMJD2A (KDM2A) | H3K9me3 | Promotes prostate cancer initiation. Associate with PCa aggressiveness. | Kim et al. (2016) | |
| H3K36me3 | ||||
| JMJD3 (KDM6B) | H3K27me3 | Overexpressed in metastatic prostate cancer | Xiang et al. (2007) | |
| JMJD6 | H3R2me2 | Promotes castration resistant disease | Paschalis et al. (2021) | |
| PADI2 | H3R26me | Promotes AR signaling activation and progression of CRPC | Wang et al. (2017) |