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poly (ADP-ribose) polymerase 3

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Target not currently curated in GtoImmuPdb

Target id: 2864

Nomenclature: poly (ADP-ribose) polymerase 3

Abbreviated Name: PARP3

Family: Mono-ADP-ribosylating PARPs

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 533 3p21.2 PARP3 poly(ADP-ribose) polymerase family member 3
Mouse - 528 9 F1 Parp3 poly (ADP-ribose) polymerase family, member 3
Rat - 526 8q32 Parp3 poly (ADP-ribose) polymerase family, member 3
Previous and Unofficial Names Click here for help
ADP-ribosyltransferase (NAD+; poly (ADP-ribose) polymerase)-like 3 | ADPRTL3 | IRT1 | pADPRT-3 | poly (ADP-ribose) polymerase family | poly (ADP-ribose) polymerase family, member 3 | poly(ADP-ribose) synthetase-3
Database Links Click here for help
Alphafold Q9Y6F1 (Hs)
BRENDA 2.4.2.30
CATH/Gene3D 1.20.142.10, 2.20.140.10
ChEMBL Target CHEMBL5083 (Hs)
Ensembl Gene ENSG00000041880 (Hs), ENSMUSG00000023249 (Mm), ENSRNOG00000012865 (Rn)
Entrez Gene 10039 (Hs), 235587 (Mm), 300985 (Rn)
Human Protein Atlas ENSG00000041880 (Hs)
KEGG Enzyme 2.4.2.30
KEGG Gene hsa:10039 (Hs), mmu:235587 (Mm), rno:300985 (Rn)
OMIM 607726 (Hs)
Pharos Q9Y6F1 (Hs)
RefSeq Nucleotide NM_005485 (Hs), NM_145619 (Mm), NM_001008328 (Rn)
RefSeq Protein NP_005476 (Hs), NP_663594 (Mm), NP_001008329 (Rn)
SynPHARM 82200 (in complex with ME0328)
UniProtKB Q9Y6F1 (Hs)
Wikipedia PARP3 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.4.2.30

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
olaparib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.2 pKd 1
⤷ pKd 8.2 (Kd 5.8x10-9 M) [1]
KU0058948 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pKd 2
⤷ pKd 7.2 (Kd 7x10-8 M) [2]
Description: Binding affinity for PARP3 catalytic domain (178−532) determined by isothermal titration calorimetry.
ME0328 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.1 pIC50 3
⤷ pIC50 6.1 (IC50 9x10-7 M) [3]
Immuno Process Associations
Immuno Process:  B cell (activation)
Immuno Process:  Cellular signalling
Immuno Process:  Immune regulation
Immuno Process:  Immune system development
Immuno Process:  Inflammation
Immuno Process:  T cell (activation)

References

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1. Johannes JW, Balazs A, Barratt D, Bista M, Chuba MD, Cosulich S, Critchlow SE, Degorce SL, Di Fruscia P, Edmondson SD et al.. (2021) Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs. J Med Chem, 64 (19): 14498-14512. [PMID:34570508]

2. Lehtiö L, Jemth AS, Collins R, Loseva O, Johansson A, Markova N, Hammarström M, Flores A, Holmberg-Schiavone L, Weigelt J et al.. (2009) Structural basis for inhibitor specificity in human poly(ADP-ribose) polymerase-3. J Med Chem, 52 (9): 3108-11. [PMID:19354255]

3. 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]

How to cite this page

Mono-ADP-ribosylating PARPs: poly (ADP-ribose) polymerase 3. Last modified on 24/01/2024. Accessed on 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2864.