PARP1 in carcinomas and PARP1 inhibitors as antineoplastic drugs

Luyao Wang, Chao LIANG, Fangfei LI, Daogang GUAN, Xiaoqiu Wu, Xuekun Fu, Aiping LYU, Ge ZHANG*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

26 Citations (Scopus)

Abstract

Poly (ADP-ribose) polymerase 1 (PARP1), the best-studied isoform of the nuclear enzyme PARP family, plays a pivotal role in cellular biological processes, such as DNA repair, gene transcription, and so on. PARP1 has been found to be overexpressed in various carcinomas. These all indicate the clinical potential of PARP1 as a therapeutic target of human malignancies. Additionally, multiple preclinical research studies and clinical trials demonstrate that inhibition of PARP1 can repress tumor growth and metastasis. Up until now, PARP1 inhibitors are clinically used not only for monotherapy to suppress various tumors, but also for adjuvant therapy, to maintain or enhance therapeutic effects of mature antineoplastic drugs, as well as protect patients from chemotherapy and surgery-induced injury. To supply a framework for understanding recent research progress of PARP1 in carcinomas, we review the structure, expression, functions, and mechanisms of PARP1, and summarize the clinically mature PARP1-related anticancer agents, to provide some ideas for the development of other promising PARP1 inhibitors in antineoplastic therapy.

Original languageEnglish
Article number2111
JournalInternational Journal of Molecular Sciences
Volume18
Issue number10
DOIs
Publication statusPublished - Oct 2017

Scopus Subject Areas

  • Catalysis
  • Molecular Biology
  • Spectroscopy
  • Computer Science Applications
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry

User-Defined Keywords

  • Carcinomas
  • PARP1
  • PARP1 inhibitors

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