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Poly ADP-ribosylating PARPs and poly(ADP-ribose) glycohydrolase C

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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This subfamily includes four of the he best characterised enzymes (the PARylating PARPs) that catalyse the addition of poly-ADP-ribose chains as post-translational protein modifications: the nuclear enzymes PARP1, PARP2 and the tankyrases (TNKSs). PARPs 1 and 2 appear to function by binding to single strand breaks in DNA, allowing the recruitment of repair enzymes by the synthesis of NAD-derived ADP-ribose polymers, that are subsequently degraded by the glycohydrolase PARG. The most well defined function of the tankyrases (TNKSs) is their regulatory action on Wnt/β-catenin signalling [9]. PARPs 1 and 2 are targets of PARP inhibitor class anti-cancer drugs which are designed to disrupt the DNA damage response pathways to induce cancer cell death.
The catabolic enzyme poly(ADP-ribose) glycohydrolase (PARG) is also included in this section, as an important regulator of PARylation, and oncology drug target.

Enzymes

3347
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PARP1 (poly(ADP-ribose) polymerase 1) C Show summary » More detailed page go icon to follow link

PARP2 (poly(ADP-ribose) polymerase 2) C Show summary » More detailed page go icon to follow link

tankyrase Show summary » More detailed page go icon to follow link

tankyrase 2 Show summary » More detailed page go icon to follow link

poly(ADP-ribose) glycohydrolase Show summary »


Target Id 3347
Nomenclature poly(ADP-ribose) glycohydrolase
Genes PARG (Hs), Parg (Mm), Parg (Rn)
Ensembl ID ENSG00000227345 (Hs), ENSMUSG00000021911 (Mm), ENSRNOG00000019978 (Rn)
UniProtKB AC Q86W56 (Hs), O88622 (Mm), Q9QYM2 (Rn)
Inhibitors
FORX-428 pIC50 14.5 [8]
Comment PARG reverses PARylation (dePARylation) that is catalysed by PARP and tankyrase enzymes [1]. This enzyme is involved in DNA-damage repair, chromatin dynamics, transcriptional regulation, and apoptosis [4]. PARG has evolved as an oncology drug target [2-3,7,10-11,16].

Further reading

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References

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How to cite this family page

Database page citation:

Poly ADP-ribosylating PARPs and poly(ADP-ribose) glycohydrolase. Accessed on 16/06/2026. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=883.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Gibb AJ, Kelly E, Mathie AA, Peach CJ, Veale EL, Armstrong JF, Faccenda E, Harding SD, Southan C, Davies JA et al. (2025) The Concise Guide to PHARMACOLOGY 2025/26: Enzymes. Br J Pharmacol. 182: S307-S403.