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Poly(ADP-ribose) polymerase inhibition: past, present and future

Lookup NU author(s): Professor Nicola CurtinORCiD


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© 2020, Springer Nature Limited. The process of poly(ADP-ribosyl)ation and the major enzyme that catalyses this reaction, poly(ADP-ribose) polymerase 1 (PARP1), were discovered more than 50 years ago. Since then, advances in our understanding of the roles of PARP1 in cellular processes such as DNA repair, gene transcription and cell death have allowed the investigation of therapeutic PARP inhibition for a variety of diseases — particularly cancers in which defects in DNA repair pathways make tumour cells highly sensitive to the inhibition of PARP activity. Efforts to identify and evaluate potent PARP inhibitors have so far led to the regulatory approval of four PARP inhibitors for the treatment of several types of cancer, and PARP inhibitors have also shown therapeutic potential in treating non-oncological diseases. This Review provides a timeline of PARP biology and medicinal chemistry, summarizes the pathophysiological processes in which PARP plays a role and highlights key opportunities and challenges in the field, such as counteracting PARP inhibitor resistance during cancer therapy and repurposing PARP inhibitors for the treatment of non-oncological diseases.

Publication metadata

Author(s): Curtin NJ, Szabo C

Publication type: Review

Publication status: Published

Journal: Nature Reviews Drug Discovery

Year: 2020

Volume: 19

Issue: 10

Pages: 711-736

Print publication date: 01/10/2020

Online publication date: 03/09/2020

Acceptance date: 30/06/2020

ISSN (print): 1474-1776

ISSN (electronic): 1474-1784

Publisher: Nature Research


DOI: 10.1038/s41573-020-0076-6

PubMed id: 32884152