Issue 3, 2019

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

Abstract

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.

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

Supplementary files

Article information

Article type
Communication
Submitted
30 Sep 2018
Accepted
05 Dec 2018
First published
05 Dec 2018

Chem. Commun., 2019,55, 369-372

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

Q. Zhao, T. Lan, S. Su and Y. Rao, Chem. Commun., 2019, 55, 369 DOI: 10.1039/C8CC07813K

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