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Target not currently curated in GtoImmuPdb
Target id: 2771
Nomenclature: poly(ADP-ribose) polymerase 1
Abbreviated Name: PARP1
Family: Poly ADP-ribose polymerases
Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 1014 | 1q42.12 | PARP1 | poly(ADP-ribose) polymerase 1 | |
Mouse | - | 1013 | 1 84.44 cM | Parp1 | poly (ADP-ribose) polymerase family, member 1 | |
Rat | - | 1014 | 13q26 | Parp1 | poly (ADP-ribose) polymerase 1 |
Previous and Unofficial Names ![]() |
poly (ADP-ribose) polymerase family, member 1 | poly (ADP-ribose) polymerase family | ADP-ribosyltransferase | ADPRT | poly (ADP-ribose) polymerase 1 | PPOL |
Database Links ![]() |
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BRENDA | 2.4.2.30 |
CATH/Gene3D | 2.20.140.10, 3.30.1740.10, 3.40.50.10190, 1.20.142.10 |
ChEMBL Target | CHEMBL3105 (Hs), CHEMBL3740 (Mm), CHEMBL4664 (Rn) |
Ensembl Gene | ENSG00000143799 (Hs), ENSMUSG00000026496 (Mm), ENSRNOG00000003084 (Rn) |
Entrez Gene | 142 (Hs), 11545 (Mm), 25591 (Rn) |
Human Protein Atlas | ENSG00000143799 (Hs) |
KEGG Enzyme | 2.4.2.30 |
KEGG Gene | hsa:142 (Hs), mmu:11545 (Mm), rno:25591 (Rn) |
OMIM | 173870 (Hs) |
Pharos | P09874 (Hs) |
RefSeq Nucleotide | NM_001618 (Hs), NM_007415 (Mm), NM_013063 (Rn) |
RefSeq Protein | NP_001609 (Hs), NP_031441 (Mm), NP_037195 (Rn) |
SynPHARM |
82673 (in complex with compound 10b [PMID: 26222319]) 81911 (in complex with niraparib) 79917 (in complex with olaparib) 80263 (in complex with rucaparib) 81953 (in complex with talazoparib) |
UniProtKB | P09874 (Hs), P11103 (Mm), P27008 (Rn) |
Wikipedia | PARP1 (Hs) |
Selected 3D Structures ![]() |
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Enzyme Reaction ![]() |
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Download all structure-activity data for this target as a CSV file
Inhibitors | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Immuno Process Associations | |||||||||
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1. Aoyagi-Scharber M, Gardberg AS, Yip BK, Wang B, Shen Y, Fitzpatrick PA. (2014) Structural basis for the inhibition of poly(ADP-ribose) polymerases 1 and 2 by BMN 673, a potent inhibitor derived from dihydropyridophthalazinone. Acta Crystallogr F Struct Biol Commun, 70 (Pt 9): 1143-9. [PMID:25195882]
2. Dillon KJ, Smith GC, Martin NM. (2003) A FlashPlate assay for the identification of PARP-1 inhibitors. J Biomol Screen, 8 (3): 347-52. [PMID:12857389]
3. Johannes JW, Almeida L, Barlaam B, Boriack-Sjodin PA, Casella R, Croft RA, Dishington AP, Gingipalli L, Gu C, Hawkins JL et al.. (2015) Pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathway inhibitors suitable for in vivo pharmacology. ACS Med Chem Lett, 6 (3): 254-9. [PMID:25815142]
4. Jones P, Altamura S, Boueres J, Ferrigno F, Fonsi M, Giomini C, Lamartina S, Monteagudo E, Ontoria JM, Orsale MV et al.. (2009) Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J. Med. Chem., 52 (22): 7170-85. [PMID:19873981]
5. Kang J-H, Lee H-S, Lee Y-S, Park J-T, An K-M, Jeong J-A, Kim K-S, Kim J-G, Hong C-H, Park S-Y et al.. (2015) A novel phtalazinone derivatives and manufacturing process thereof. Patent number: WO2015037939A1. Assignee: Ildong Pharm Co., Ltd.. Priority date: 13/09/2013. Publication date: 19/03/2015.
6. Lindgren AE, Karlberg T, Ekblad T, Spjut S, Thorsell AG, Andersson CD, Nhan TT, Hellsten V, Weigelt J, Linusson A et al.. (2013) Chemical probes to study ADP-ribosylation: synthesis and biochemical evaluation of inhibitors of the human ADP-ribosyltransferase ARTD3/PARP3. J. Med. Chem., 56 (23): 9556-68. [PMID:24188023]
7. Menear KA, Adcock C, Boulter R, Cockcroft XL, Copsey L, Cranston A, Dillon KJ, Drzewiecki J, Garman S, Gomez S et al.. (2008) 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1. J. Med. Chem., 51 (20): 6581-91. [PMID:18800822]
8. Mosca L, Rotili D, Tempera I, Masci A, Fontana M, Chiaraluce R, Mastromarino P, d'Erme M, Mai A. (2011) Biological effects of MC2050, a quinazoline-based PARP-1 inhibitor, in human neuroblastoma and EBV-positive Burkitt's lymphoma cells. ChemMedChem, 6 (4): 606-11. [PMID:21365766]
9. Papeo G, Posteri H, Borghi D, Busel AA, Caprera F, Casale E, Ciomei M, Cirla A, Corti E, D'Anello M et al.. (2015) Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy. J. Med. Chem., 58 (17): 6875-98. [PMID:26222319]
10. Skalitzky DJ, Marakovits JT, Maegley KA, Ekker A, Yu XH, Hostomsky Z, Webber SE, Eastman BW, Almassy R, Li J et al.. (2003) Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors. J. Med. Chem., 46 (2): 210-3. [PMID:12519059]
11. Thomas HD, Calabrese CR, Batey MA, Canan S, Hostomsky Z, Kyle S, Maegley KA, Newell DR, Skalitzky D, Wang LZ et al.. (2007) Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol. Cancer Ther., 6 (3): 945-56. [PMID:17363489]
12. Tomassi S, Pfahler J, Mautone N, Rovere A, Esposito C, Passeri D, Pellicciari R, Novellino E, Pannek M, Steegborn C et al.. (2020) From PARP1 to TNKS2 Inhibition: A Structure-Based Approach. ACS Med Chem Lett, [Articles ASAP]. DOI: 10.1021/acsmedchemlett.9b00654
Poly ADP-ribose polymerases: poly(ADP-ribose) polymerase 1. Last modified on 17/08/2020. Accessed on 20/01/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2771.