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前景光明：BET和EZH2抑制剂治疗淋巴瘤

2018-03-06 MedSci MedSci原创

BETEzh2表观遗传学淋巴瘤
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近日，在巴黎召开的2018年TAT（靶向抗癌治疗）国际大会上，研究人员公布了新的表观遗传化合物，它们已在淋巴瘤的早期活动中显示出了抗肿瘤效果。

近日，在巴黎召开的2018年TAT（靶向抗癌治疗）国际大会上，研究人员公布了新的表观遗传化合物，它们已在淋巴瘤的早期活动中显示出了抗肿瘤效果。

表观遗传学靶向化合物包括BET抑制剂和EZH2抑制剂，研究人员发现BET抑制剂在白血病，淋巴瘤以及NUT肿瘤中均能表现出抗癌活性。NUT肿瘤是一种由涉及BET基因的易位驱动的罕见和侵袭性肿瘤。I型BET抑制剂birabresib（OTX015 / MK-8628）的研究显示其在弥漫性B细胞淋巴瘤和NUT肿瘤具有抗癌效果。

截至目前，临床试验已经研究了几种其他的BET抑制剂，初步结果证实它们可能对弥漫性B细胞淋巴瘤和NUT肿瘤患者有效。尽管一般耐受性水平良好，但观察到了一些可能限制治疗依从性的副作用，这些副作用包括血小板减少症（血小板数量减少，这可能是剂量限制性的，可逆的并且不伴有大出血），疲劳和胃肠道症状。临床数据的另一个领域涉及EZH2抑制剂，EZH2是一种在淋巴瘤中表现出相对频繁的突变的蛋白质。对B细胞淋巴瘤患者的研究结果显示，EZH2抑制剂具有抗肿瘤活性，耐受性良好且具有可控的毒性。 

原始出处：

https://www.europeanpharmaceuticalreview.com/news/73359/promising-results-bet-inhibitor-lymphoma/

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    2018-12-09 ms5439512287675881

    #BET#

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    2018-11-06 fusion

    #Ezh2#

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    2019-02-08 liuquan

    #2抑制剂#

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    2019-01-16 119337470

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    2018-11-04 jklm09

    #抑制剂#

    0

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