poly(ADP-ribose) polymerase 2

Target id: 2772

Nomenclature: poly(ADP-ribose) polymerase 2

Abbreviated Name: PARP2

Family: 2.4.2.30 poly(ADP-ribose)polymerases

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for poly(ADP-ribose) polymerase 2 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 583 14q11.2-q12 PARP2 poly(ADP-ribose) polymerase 2
Mouse - 559 14 C1 Parp2 poly (ADP-ribose) polymerase family, member 2
Rat - 558 15p14 Parp2 poly (ADP-ribose) polymerase 2
Previous and Unofficial Names
ADPRTL2 | poly (ADP-ribose) polymerase 2
Database Links
BRENDA
CATH/Gene3D
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Structure of PARP2 catalytic domain bound to inhibitor BMN 673 (talazoparib)
PDB Id:  4PJV
Ligand:  talazoparib
Resolution:  2.5Å
Species:  Human
References:  1
Image of receptor 3D structure from RCSB PDB
Description:  Structure of PARP2 catalytic domain bound to an isoindolinone inhibitor
PDB Id:  4ZZX
Ligand:  compound 10b [PMID: 26222319]
Resolution:  1.65Å
Species:  Human
References:  5
Enzyme Reaction
EC Number: 2.4.2.30

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
compound 10b [PMID: 26222319] Hs Inhibition 6.9 pKd 5
pKd 6.9 (Kd 1.25x10-7 M) [5]
olaparib Hs Inhibition 9.0 pIC50 2,4
pIC50 9.0 (IC50 1x10-9 M) [2,4]
Description: Assayed using PARP-2 isolated from HeLa cells, in a scintillation proximity ELISA.
niraparib Hs Binding 8.7 pIC50 3
pIC50 8.7 (IC50 2.1x10-9 M) [3]
talazoparib Hs Inhibition - - 1
[1]

References

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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 Commun70 (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 Screen8 (3): 347-52. [PMID:12857389]

3. 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]

4. 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]

5. 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.,  [Epub ahead of print]. [PMID:26222319]

How to cite this page

2.4.2.30 poly(ADP-ribose)polymerases: poly(ADP-ribose) polymerase 2. Last modified on 29/01/2016. Accessed on 17/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2772.