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Fig. 1 | Clinical Epigenetics

Fig. 1

From: Finding an easy way to harmonize: a review of advances in clinical research and combination strategies of EZH2 inhibitors

Fig. 1

Two types EZH2i through suppressed key steps of Methionine cycle. (1) SAH hydrolase inhibitor inhibits SAH degradation into adenosine and homocysteine to cause methyl accumulation, which suppresses methionine cycling production of methyl and inhibits EZH2 enzyme activity indirectly. (2) SAM-competitive inhibitor partially occupies the site for the co‐substrate SAM in the binding pocket of EZH2 to deprive EZH2 the use of methyl, such as tazemetostat, GSK126, CPI-1205, PF-06821497 and SHR2554. These inhibitors have more direct characteristic compared to the SAH hydrolase.

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Clinical Epigenetics

ISSN: 1868-7083

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