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Induction of apoptosis in MDA-MB-231 breast cancer cells by a PARP1-targeting PROTAC small molecule†
Chemical Communications ( IF 4.9 ) Pub Date : 2018-12-05 00:00:00 , DOI: 10.1039/c8cc07813k
Qiuye Zhao 1, 2, 3, 4, 5 , Tianlong Lan 1, 2, 3, 4, 5 , Shang Su 1, 4, 5, 6, 7 , Yu Rao 1, 2, 3, 4, 5
Affiliation  

Poly (ADP-ribose) polymerase-1 (PARP1) is a major member of the PARP superfamily that is involved in DNA damage signalling and other important cellular processes. Here we report the development of a small molecule targeting PARP1 based on the PROTAC strategy. In the MDA-MB-231 cell line, the representative compound 3 can induce significant PARP1 cleavage and programmed cell death.

中文翻译:

靶向PARP1的PROTAC小分子诱导MDA-MB-231乳腺癌细胞凋亡

聚(ADP-核糖)聚合酶-1(PARP1)是PARP超家族的主要成员,该家族参与DNA损伤信号传导和其他重要的细胞过程。在这里,我们报告了基于PROTAC策略的靶向PARP1的小分子的发展。在MDA-MB-231细胞系中,代表性化合物3可以诱导明显的PARP1裂解和程序性细胞死亡。
更新日期:2018-12-05
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