Pharmacologic inhibition of histone demethylation as a therapy for pediatric brainstem glioma.
Pharmacologic inhibition of histone demethylation as a therapy for pediatric brainstem glioma.
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儿童脑干神经胶质瘤通常具有组蛋白H3.3的致癌K27M突变。我们发现GSKJ4对K27去甲基化酶JMJD3的药理学抑制作用增加了K27 M肿瘤细胞中H3K27的甲基化，并在体外和体内对K27 M异种移植物显示了有效的抗肿瘤活性。我们的研究结果表明，通过抑制K27去甲基化酶来增加H3K27甲基化是治疗表达K27 M的脑干胶质瘤的有效治疗策略。
Pediatric brainstem gliomas often harbor oncogenic K27M mutation of histone H3.3. Here we show that GSKJ4 pharmacologic inhibition of K27 demethylase JMJD3 increases cellular H3K27 methylation in K27M tumor cells and demonstrate potent antitumor activity bothin vitroagainst K27M cells andin vivoagainst K27M xenografts. Our results demonstrate that increasing H3K27 methylation by inhibiting K27 demethylase is a valid therapeutic strategy for treating K27M-expressing brainstem glioma.
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