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BRD4 PROTAC降解剂MZ1通过向CCND3表现出抗B细胞急性淋巴细胞白血病的影响

Li Ma^1,2, Jianwei Wang³, Yang Yang³

¹Department of Hematology, Children's Hospital of Soochow University, Suzhou, People's Republic of China.

Hematology (Amsterdam, Netherlands)

|August 18, 2023

概括

MZ1是一种新型的Bromodomains和外终端 (BET) 抑制剂,有效地降低B细胞急性淋巴细胞白血病 (B-ALL) 细胞生长,并促进细胞亡. 这项研究突出了MZ1的特点.

科学领域:

血液学血液学血液学
在瘤学瘤学.
分子生物学分子生物学

背景情况:

B细胞急性淋巴细胞白血病 (B-ALL) 是一种常见的儿童癌症,在复发病例中死亡率高.
体蛋白和额外终端 (BET) 蛋白与血液性恶性瘤有关.
MZ1是一种新型BET抑制剂,具有已证明的抗瘤活性.

研究的目的:

研究MZ1在B-ALL治疗中的治疗潜力和机制.
为了评估MZ1对B-ALL细胞系的疗效.

主要方法:

在体外测定包括CCK8,酸 (PI) 染色和Annexin V/PI染色在B-ALL细胞系上进行.
西方涂抹和qRT-PCR用于分析蛋白质和mRNA表达.
RNA测序 (RNA-seq) 确定了MZ1的基因,而lentiviral转移确立了稳定的细胞系.

主要成果:

在B-ALL细胞中,MZ1诱导了BRD4,BRD3和BRD2的降解,抑制了生长,诱导了细胞亡和细胞循环停止.
MZ1对TCF3/PBX1和MLL-AF4 B-ALL亚型表现出细胞毒性作用.
RNA-seq显示MZ1降低了CCND3表达的调节,促进了细胞亡和抑制细胞增殖.

结论:

MZ1在体外表现出显著的抗B-ALL作用.
MZ1代表了B-ALL治疗的潜在新型治疗标.

关键词:

B细胞急性淋巴细胞白血病.这是一种BET抑制剂.这就是BRD4D.CCND3 在线阅读 MZ1MZ1MZ1MZ1MZ1MZ1MZ1MZ1MZ1MZ1MZ1MZ1MZ1MZ1MZ1MZ1MZ1MZ1MZ1MZ1MZ1MZ1

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