Induction of apoptosis in MDA-MB-231 breast cancer cells by a PARP1-targeting PROTAC small molecule

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 represe...

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Veröffentlicht in:Chemical communications (Cambridge, England) England), 2019, Vol.55 (3), p.369-372
Hauptverfasser: Zhao, Qiuye, Lan, Tianlong, Su, Shang, Rao, Yu
Format: Artikel
Sprache:eng
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Zusammenfassung: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.
ISSN:1359-7345
1364-548X
DOI:10.1039/c8cc07813k