Mechanisms of action and resistance in histone methylation-targeted therapy (IMAGE)
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Valemetostat reduces methylated histone levels by inhibiting EZH1/2 and induces expression of tumor suppressor genes, resulting in a sustained clinical benefit. In some patients receiving long-term therapy, mutations in target molecules or aberrant DNA methylation can cause chromatin structure reaggregation, leading to clinical relapse.
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2024 Makoto Yamagishi, The University of Tokyo
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