IMR Press / FBL / Volume 23 / Issue 1 / DOI: 10.2741/4578

Frontiers in Bioscience-Landmark (FBL) is published by IMR Press from Volume 26 Issue 5 (2021). Previous articles were published by another publisher on a subscription basis, and they are hosted by IMR Press on as a courtesy and upon agreement with Frontiers in Bioscience.


Regulation of poly(ADP-Ribose) polymerase 1 functions by post-translational modifications

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1 Institute of Bioinformatics and Medical Engineering, Jiangsu University of Technology, Changzhou 213001, China
2 Division of Molecular Modification and Cancer Biology, National Cancer Center Research Institute, 5-1-1 Tsukiji, Chuo-ku, Tokyo 104-0045, Japan
3 Department of Bioengineering, School of Engineering, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-8656, Japan
Front. Biosci. (Landmark Ed) 2018, 23(1), 13–26;
Published: 1 January 2018

The poly(ADP-ribose) polymerases (PARPs) catalyze poly(ADP-ribosyl)ation, a post-translational modification of proteins. This consists of the attachment of mono- or poly-adenosine diphosphate (ADP)-ribose units from nicotinamide adenine dinucleotide (NAD+) to specific polar residues of target proteins. PARP1 is the most abundant and best-characterized member of the family of PARP enzymes. PARP1 plays key roles in DNA repair, as well as a wide variety of cellular processes, including transcriptional regulation, chromatin modulation, cellular signaling pathway, inflammation, cellular stress responses and so on. Hence, PARP1 inhibitors have become a promising therapeutic approach for human diseases including cancer. Recent studies indicate that post-translational modifications (PTMs) such as phosphorylation, acetylation, and methylation are crucial for the regulation of PARP1 activity, and dysregulation of modifications on PARP1 is observed in human cancer. In this review, we describe the importance of PTMs to regulate the activity of PARP1, and the involvement of dysregulation of PTMs in human cancer.

Post-translational modification
Targeted cancer therapy
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