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Literature summary extracted from

  • Venkannagari, H.; Fallarero, A.; Feijs, K.L.; Luescher, B.; Lehtioe, L.
    Activity-based assay for human mono-ADP-ribosyltransferases ARTD7/PARP15 and ARTD10/PARP10 aimed at screening and profiling inhibitors (2013), Eur. J. Pharm. Sci., 49, 148-156.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.2.30 expressed in Escherichia coli Rosetta2 (DE3) cells Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
2.4.2.30 G888W inactive Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.2.30 (beta,beta-dimethylacryl)shikonin 64% inhibition at 0.01 mM; 64% inhibition at 0.01 mM Homo sapiens
2.4.2.30 bergapten 69% inhibition at 0.01 mM; 69% inhibition at 0.01 mM Homo sapiens
2.4.2.30 deoxyshikonin 67% inhibition at 0.01 mM; 67% inhibition at 0.01 mM Homo sapiens
2.4.2.30 DMSO at 2% (v/v) DMSO isoform ARTD10 loses more than half of its activity; at 2% (v/v) DMSO isoform ARTD7 loses its activity completely Homo sapiens
2.4.2.30 EB-47 i.e. 5'-deoxy-5'-[4-[2-[(2,3-dihydro-1-oxo-1H-isoindol-4-yl)amino]-2-oxoethyl]-1-piperazinyl]-5'-oxoadenosine dihydrochloride; i.e. 5'-deoxy-5'-[4-[2-[(2,3-dihydro-1-oxo-1H-isoindol-4-yl)amino]-2-oxoethyl]-1-piperazinyl]-5'-oxoadenosine dihydrochloride Homo sapiens
2.4.2.30 embelin 57% inhibition at 0.01 mM; 57% inhibition at 0.01 mM Homo sapiens
2.4.2.30 gambogic acid 75% inhibition at 0.01 mM; 75% inhibition at 0.01 mM Homo sapiens
2.4.2.30 gossypol 75% inhibition at 0.01 mM; 75% inhibition at 0.01 mM Homo sapiens
2.4.2.30 menadione 55% inhibition at 0.01 mM; 55% inhibition at 0.01 mM Homo sapiens
2.4.2.30 myricetin 78% inhibition at 0.01 mM; 78% inhibition at 0.01 mM Homo sapiens
2.4.2.30 olaparib i.e. 4-[(3-[(4-cyclopropylcarbonyl)piperazin-4-yl]carbonyl)-4-fluorophenyl]methyl(2H)phthalazin-1-one; i.e. 4-[(3-[(4-cyclopropylcarbonyl)piperazin-4-yl]carbonyl)-4-fluorophenyl]methyl(2H)phthalazin-1-one Homo sapiens
2.4.2.30 phenantridinone i.e. 6(5H)-phenantridinone; i.e. 6(5H)-phenantridinone Homo sapiens
2.4.2.30 Plumbagin 67% inhibition at 0.01 mM; 67% inhibition at 0.01 mM Homo sapiens
2.4.2.30 TIQ-A i.e. 4H-thieno[2,3-c]isoquinolin-5-one; i.e. 4H-thieno[2,3-c]isoquinolin-5-one Homo sapiens
2.4.2.30 trimethylpsoralen 61% inhibition at 0.01 mM; 61% inhibition at 0.01 mM Homo sapiens

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.4.2.30 25000
-
 x * 25000, SDS-PAGE Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.4.2.30 Homo sapiens Q460N3
-
-
2.4.2.30 Homo sapiens Q53GL7
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.4.2.30 HisTrap column chromatography Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.2.30 NAD+ + (ADP-D-ribosyl)n-serine/arginine-rich protein-specific kinase 2
-
 Homo sapiens nicotinamide + (ADP-D-ribosyl)n+1-serine/arginine-rich protein-specific kinase 2 + H+
-
 ?

Subunits

EC Number Subunits Comment Organism
2.4.2.30 ? x * 25000, SDS-PAGE Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
2.4.2.30 ARTD10/PARP10 isoform Homo sapiens
2.4.2.30 ARTD7/PARP15 isoform Homo sapiens
2.4.2.30 mono-ADP-ribosyltransferase
-
 Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.4.2.30 6.5
-
 ARDT7 Homo sapiens
2.4.2.30 8
-
 ARDT10 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.2.30 0.000232
-
 isoform ARDT7, pH and temperature not specified in the publication Homo sapiens TIQ-A
2.4.2.30 0.000745
-
 isoform ARDT10, pH and temperature not specified in the publication Homo sapiens phenantridinone
2.4.2.30 0.000925
-
 isoform ARDT7, pH and temperature not specified in the publication Homo sapiens olaparib
2.4.2.30 0.00114
-
 isoform ARDT7, pH and temperature not specified in the publication Homo sapiens phenantridinone
2.4.2.30 0.00118
-
 isoform ARDT10, pH and temperature not specified in the publication Homo sapiens EB-47
2.4.2.30 0.00204
-
 isoform ARDT10, pH and temperature not specified in the publication Homo sapiens olaparib