溴尿嘧啶
癌症研究
BRD4
生物
BET抑制剂
靶向治疗
转录因子
小细胞肺癌
癌症
化疗
表观遗传学
小细胞癌
基因
遗传学
作者
Gerhard Hamilton,Sandra Stickler,Barbara H. Rath
标识
DOI:10.2174/0115680096272757231211113206
摘要
the bromodomain (BET) protein BRD4, which activates MYC transcription, by specific BET inhibitors that reduce the expression of this oncogenic driver. Here, novel BET-directed Proteolysis Targeting Chimeras (PROTACs) are discussed that show high antiproliferative activity in SCLC. Particularly, ARV-825, targeting specifically BRD4, exhibits superior cytotoxic effects on SCLC cell lines and may become a valuable adjunct to SCLC combination chemotherapy.
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