Poly [ADP-ribose] polymerase 1
Also known as: ADPRT, PARP1, PPOL
Function
Poly-ADP-ribosyltransferase that mediates poly-ADP-ribosylation of proteins and plays a key role in DNA repair. Mediates glutamate, aspartate, serine, histidine or tyrosine ADP-ribosylation of proteins: the ADP-D-ribosyl group of NAD(+) is transferred to the acceptor carboxyl group of target residues and further ADP-ribosyl groups are transferred to the 2'-position of the terminal adenosine moiety, building up a polymer with an average chain length of 20-30 units. Serine ADP-ribosylation of proteins constitutes the primary form of ADP-ribosylation of proteins in response to DNA damage. Specificity for the different amino acids is conferred by interacting factors, such as HPF1 and NMNAT1. Following interaction with HPF1, catalyzes serine ADP-ribosylation of target proteins; HPF1 confers serine specificity by completing the PARP1 active site. Also catalyzes tyrosine ADP-ribosylation of target proteins following interaction with HPF1. Following interaction with NMNAT1, catalyzes glutamate and aspartate ADP-ribosylation of target proteins; NMNAT1 confers glutamate and aspartate specificity (By similarity). PARP1 initiates the repair of DNA breaks: recognizes and binds DNA breaks within chromatin and recruits HPF1, licensing serine ADP-ribosylation of target proteins, such as histones (H2BS6ADPr and H3S10ADPr), thereby promoting decompaction of chromatin and the recruitment of repair factors leading to the reparation of DNA strand breaks. HPF1 initiates serine ADP-ribosylation but restricts the polymerase activity of PARP1 in order to limit the length of poly-ADP-ribose chains. In addition to base excision repair (BER) pathway, also involved in double-strand breaks (DSBs) repair: together with TIMELESS, accumulates at DNA damage sites and promotes homologous recombination repair by mediating poly-ADP-ribosylation. Mediates the poly-ADP-ribosylation of a number of proteins, including itself, APLF, CHFR, RPA1 and NFAT5. In addition to proteins, also able to ADP-ribosylate DNA: catalyzes ADP-ribosylation of DNA strand break termini containing terminal phosphates and a 2'-OH group in single- and double-stranded DNA, respectively. Required for PARP9 and DTX3L recruitment to DNA damage sites. PARP1-dependent PARP9-DTX3L-mediated ubiquitination promotes the rapid and specific recruitment of 53BP1/TP53BP1, UIMC1/RAP80, and BRCA1 to DNA damage sites. PARP1-mediated DNA repair in neurons plays a role in sleep: senses DNA damage in neurons and promotes sleep, facilitating efficient DNA repair (By similarity). In addition to DNA repair, also involved in other processes, such as transcription regulation, programmed cell death, membrane repair, adipogenesis and innate immunity. Acts as a repressor of transcription: binds to nucleosomes and modulates chromatin structure in a manner similar to histone H1, thereby altering RNA polymerase II. Acts both as a positive and negative regulator of transcription elongation, depending on the context. Acts as a positive regulator of transcription elongation by mediating poly-ADP-ribosylation of NELFE, preventing RNA-binding activity of NELFE and relieving transcription pausing. Acts as a negative regulator of transcription elongation in response to DNA damage by catalyzing poly-ADP-ribosylation of CCNT1, disrupting the phase separation activity of CCNT1 and subsequent activation of CDK9. Involved in replication fork progression following interaction with CARM1: mediates poly-ADP-ribosylation at replication forks, slowing fork progression. Poly-ADP-ribose chains generated by PARP1 also play a role in poly-ADP-ribose-dependent cell death, a process named parthanatos (By similarity). Also acts as a negative regulator of the cGAS-STING pathway. Acts by mediating poly-ADP-ribosylation of CGAS: PARP1 translocates into the cytosol following phosphorylation by PRKDC and catalyzes poly-ADP-ribosylation and inactivation of CGAS. Acts as a negative regulator of adipogenesis: catalyzes poly-ADP-ribosylation of histone H2B on 'Glu-35' (H2BE35ADPr) following interaction with NMNAT1, inhibiting phosphorylation of H2B at 'Ser-36' (H2BS36ph), thereby blocking expression of pro-adipogenetic genes (By similarity). Involved in the synthesis of ATP in the nucleus, together with NMNAT1, PARG and NUDT5. Nuclear ATP generation is required for extensive chromatin remodeling events that are energy-consuming. Plays a role in sister chromatid cohesion by mediating ADP-ribosylation of RSMC during S phase which promotes the interaction between RSMC and CDCA5/sororin, leading to enhanced interaction of CDCA5/sororin with the cohesin complex and promotion of sister chromatid cohesion.
Classification
- Family (Pfam)
- PF00533 BRCT, PF21728 PADR1_N, PF00644 PARP, PF02877 PARP_reg, PF05406 WGR, PF00645 zf-PARP, PF08063 Zn_ribbon_PADR1
- InterPro
- ARTD/PARP, BRCT_dom, BRCT_dom_sf, PADR1_C_dom_sf, PARP, PARP1-like_PADR1_N, PARP1-like_PADR1_Zn_ribbon, Poly(ADP-ribose)pol_cat_dom, Poly(ADP-ribose)pol_reg_dom, Poly(ADP-ribose)pol_reg_dom_sf, WGR_dom_sf, WGR_domain, Znf_PARP, Znf_PARP_sf
- Functional cluster
- Adenylate Kinases & Peroxiredoxins
Experimental structures · PDB · 102
- 1UK0 X-ray 3.00A
- 1UK1 X-ray 3.00A
- 1WOK X-ray 3.00A
- 2COK NMR
- 2CR9 NMR
- 2CS2 NMR
- 2DMJ NMR
- 2JVN NMR
- 2L30 NMR
- 2L31 NMR
- 2N8A NMR
- 2RCW X-ray 2.80A
- … and 90 more
A predicted model is available from AlphaFold.
Gene Ontology · 106
- GO:0000785 chromatin
- GO:0000781 chromosome, telomeric region
- GO:0005829 cytosol
- GO:0001650 fibrillar center
- GO:0016020 membrane
- GO:0005739 mitochondrion
- GO:0016604 nuclear body
- GO:0005635 nuclear envelope
- GO:0043596 nuclear replication fork
- GO:0005730 nucleolus
- GO:0005654 nucleoplasm
- GO:0005634 nucleus
- GO:0032991 protein-containing complex
- GO:0032993 protein-DNA complex
- GO:0090734 site of DNA damage
- GO:0035861 site of double-strand break
- GO:0005667 transcription regulator complex
- GO:0003682 chromatin binding
- GO:0003684 damaged DNA binding
- GO:0003677 DNA binding
- GO:0008047 enzyme activator activity
- GO:0019899 enzyme binding
- GO:0042826 histone deacetylase binding
- GO:0042802 identical protein binding
- GO:0051287 NAD binding
- GO:0140294 NAD DNA ADP-ribosyltransferase activity
- GO:0003950 NAD+ poly-ADP-ribosyltransferase activity
- GO:0140822 NAD+-histone H2BE35 glutamate ADP-ribosyltransferase activity
- GO:0140816 NAD+-histone H2BS6 serine ADP-ribosyltransferase activity
- GO:0140817 NAD+-histone H3S10 serine ADP-ribosyltransferase activity
- GO:1990404 NAD+-protein mono-ADP-ribosyltransferase activity
- GO:0140806 NAD+-protein-aspartate ADP-ribosyltransferase activity
- GO:0140807 NAD+-protein-glutamate ADP-ribosyltransferase activity
- GO:0140815 NAD+-protein-histidine ADP-ribosyltransferase activity
- GO:0140805 NAD+-protein-serine ADP-ribosyltransferase activity
- GO:0140808 NAD+-protein-tyrosine ADP-ribosyltransferase activity
- GO:0044378 non-sequence-specific DNA binding, bending
- GO:0030331 nuclear estrogen receptor binding
- GO:0031491 nucleosome binding
- GO:0016779 nucleotidyltransferase activity
- GO:0042803 protein homodimerization activity
- GO:0019901 protein kinase binding
- GO:0070412 R-SMAD binding
- GO:0003723 RNA binding
- GO:0061629 RNA polymerase II-specific DNA-binding transcription factor binding
- GO:1990165 single-strand break-containing DNA binding
- GO:0140537 transcription regulator activator activity
- GO:0031625 ubiquitin protein ligase binding
- GO:0008270 zinc ion binding
- GO:0006915 apoptotic process
- GO:1990966 ATP generation from poly-ADP-D-ribose
- GO:0016051 carbohydrate biosynthetic process
- GO:1904646 cellular response to amyloid-beta
- GO:0032869 cellular response to insulin stimulus
- GO:1990090 cellular response to nerve growth factor stimulus
- GO:0034599 cellular response to oxidative stress
- GO:0034644 cellular response to UV
- GO:0071294 cellular response to zinc ion
- GO:0046697 decidualization
- GO:0030592 DNA ADP-ribosylation
- GO:0006974 DNA damage response
- GO:0006281 DNA repair
- GO:0006302 double-strand break repair
- GO:0071169 establishment of protein localization to chromatin
- GO:0045087 innate immune response
- GO:0030225 macrophage differentiation
- GO:0032042 mitochondrial DNA metabolic process
- GO:0043504 mitochondrial DNA repair
- GO:0007005 mitochondrion organization
- GO:1904178 negative regulation of adipose tissue development
- GO:2001170 negative regulation of ATP biosynthetic process
- GO:0160049 negative regulation of cGAS/STING signaling pathway
- GO:0045892 negative regulation of DNA-templated transcription
- GO:0045824 negative regulation of innate immune response
- GO:1904357 negative regulation of telomere maintenance via telomere lengthening
- GO:0000122 negative regulation of transcription by RNA polymerase II
- GO:0034244 negative regulation of transcription elongation by RNA polymerase II
- GO:0043123 positive regulation of canonical NF-kappaB signal transduction
- GO:0010613 positive regulation of cardiac muscle hypertrophy
- GO:0032786 positive regulation of DNA-templated transcription, elongation
- GO:1905168 positive regulation of double-strand break repair via homologous recombination
- GO:0033148 positive regulation of intracellular estrogen receptor signaling pathway
- GO:0051901 positive regulation of mitochondrial depolarization
- GO:1904762 positive regulation of myofibroblast differentiation
- GO:0060545 positive regulation of necroptotic process
- GO:1900182 positive regulation of protein localization to nucleus
- GO:0060391 positive regulation of SMAD protein signal transduction
- GO:0045944 positive regulation of transcription by RNA polymerase II
- GO:0070213 protein auto-ADP-ribosylation
- GO:0016540 protein autoprocessing
- GO:0071168 protein localization to chromatin
- GO:0036211 protein modification process
- GO:0070212 protein poly-ADP-ribosylation
- GO:1905051 regulation of base-excision repair
- GO:0045188 regulation of circadian sleep/wake cycle, non-REM sleep
- GO:1903376 regulation of oxidative stress-induced neuron intrinsic apoptotic signaling pathway
- GO:0032880 regulation of protein localization
- GO:0071932 replication fork reversal
- GO:1904044 response to aldosterone
- GO:0045471 response to ethanol
- GO:0010332 response to gamma radiation
- GO:0023019 signal transduction involved in regulation of gene expression
- GO:0000012 single strand break repair
- GO:0000723 telomere maintenance
- GO:0006366 transcription by RNA polymerase II
- GO:0007179 transforming growth factor beta receptor signaling pathway
Drugs targeting this protein · 13
- NIRAPARIB inhibitor
- RUCAPARIB inhibitor
- TALAZOPARIB TOSYLATE inhibitor
- TALAZOPARIB inhibitor
- E-7016 inhibitor
- 2X-121 inhibitor
- RUCAPARIB CAMSYLATE inhibitor
- NIRAPARIB TOSYLATE MONOHYDRATE inhibitor
- PAMIPARIB inhibitor
- SENAPARIB inhibitor
- VELIPARIB inhibitor
- OLAPARIB inhibitor
- AMELPARIB DIHYDROCHLORIDE DIHYDRATE inhibitor
Related proteins · sequence + function similarity
- Poly [ADP-ribose] polymerase 1 0.99
- Poly [ADP-ribose] polymerase 1 0.98
- Poly [ADP-ribose] polymerase 1 0.98
- Poly [ADP-ribose] polymerase 1 0.98
- Poly [ADP-ribose] polymerase 1 0.98
- Poly [ADP-ribose] polymerase 1 0.97
- Poly [ADP-ribose] polymerase 1 0.96
- Poly [ADP-ribose] polymerase 1 0.86
- Poly [ADP-ribose] polymerase 1 0.80
- Poly [ADP-ribose] polymerase 1 0.80
- Poly [ADP-ribose] polymerase 1 0.78
- Poly [ADP-ribose] polymerase 1 0.76
Co-cited proteins · studied together in the literature
- Histone PARylation factor 1 13 shared papers
- Poly [ADP-ribose] polymerase 2 11 shared papers
- ATP-dependent chromatin remodeler CHD1L 4 shared papers
- Pumilio homolog 3 1 shared papers
- DNA repair protein XRCC1 3 shared papers
- Histone PARylation factor 1 1 shared papers
- ATP-dependent DNA helicase Q1 1 shared papers
- Tyrosine--tRNA ligase, cytoplasmic 1 shared papers
- Replication and transcription activator 1 shared papers
- Caspase-3 3 shared papers
- DNA polymerase alpha catalytic subunit 1 shared papers
- Nuclear factor of activated T-cells 5 1 shared papers
Literature · 122 cited papers
- S-phase PARylation of microprotein RSMC enhances the function of Sororin in sister chromatid cohesion. EMBO J. · 2026
- ZNF432 stimulates PARylation and inhibits DNA resection to balance PARPi sensitivity and resistance. Nucleic Acids Res. · 2023
- Cytoplasmic PARP1 links the genome instability to the inhibition of antiviral immunity through PARylating cGAS. Mol. Cell · 2022
- Poly(ADP-ribosylation) of P-TEFb by PARP1 disrupts phase separation to inhibit global transcription after DNA damage. Nat. Cell Biol. · 2022
- Micropeptide PACMP inhibition elicits synthetic lethal effects by decreasing CtIP and poly(ADP-ribosyl)ation. Mol. Cell · 2022
- PARP1 is activated by membrane damage and is involved in membrane repair through poly(ADP-ribosyl)ation. Genes Cells · 2022
- SPARCLE, a p53-induced lncRNA, controls apoptosis after genotoxic stress by promoting PARP-1 cleavage. Mol. Cell · 2022
- RECON syndrome is a genome instability disorder caused by mutations in the DNA helicase RECQL1. J. Clin. Invest. · 2022
- The ubiquitin-dependent ATPase p97 removes cytotoxic trapped PARP1 from chromatin. Nat. Cell Biol. · 2022
- The BRCT domain of PARP1 binds intact DNA and mediates intrastrand transfer. Mol. Cell · 2021
- Serine ADP-ribosylation marks nucleosomes for ALC1-dependent chromatin remodeling. Elife · 2021
- XRCC1 protects transcription from toxic PARP1 activity during DNA base excision repair. Nat. Cell Biol. · 2021
- … and 110 more in the literature graph