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

  • Chem Commun (Camb). 2019 Jan 2;55(3):369-372. doi: 10.1039/c8cc07813k.
Qiuye Zhao  1 ,  Tianlong Lan ,  Shang Su ,  Yu Rao
Affiliations
  • 1. MOE Key Laboratory of Protein Sciences, School of Pharmaceutical Sciences, MOE Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology, Tsinghua University, Beijing 100084, P. R. China. [email protected].
PMID: 30540295 DOI: 10.1039/c8cc07813k
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.

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