An update on poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors: Opportunities and challenges in cancer therapy

Ying Qing Wang, Pingyuan Wang, Yu Ting Wang, Guang Fu Yang, Ao Zhang, Ze Hong Miao

Research output: Contribution to journalReview article

65 Scopus citations


Poly(ADP-ribose)polymerase-1 (PARP-1) is a critical DNA repair enzyme in the base excision repair pathway. Inhibitors of this enzyme comprise a new type of anticancer drug that selectively kills cancer cells by targeting homologous recombination repair defects. Since 2010, important advances have been achieved in PARP-1 inhibitors. Specifically, the approval of olaparib in 2014 for the treatment of ovarian cancer with BRCA mutations validated PARP-1 as an anticancer target and established its clinical importance in cancer therapy. Here, we provide an update on PARP-1 inhibitors, focusing on breakthroughs in their clinical applications and investigations into relevant mechanisms of action, biomarkers, and drug resistance. We also provide an update on the design strategies and the structural types of PARP-1 inhibitors. Opportunities and challenges in PARP-1 inhibitors for cancer therapy will be discussed based on the above advances.

Original languageEnglish (US)
Pages (from-to)9575-9598
Number of pages24
JournalJournal of Medicinal Chemistry
Issue number21
StatePublished - Nov 10 2016
Externally publishedYes


ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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