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Literature summary for 2.4.2.30 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
Search for more literature for 2.4.2.30

Cloned(Commentary)

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

Protein Variants

Protein Variants Comment Organism
G888W inactive Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(beta,beta-dimethylacryl)shikonin 64% inhibition at 0.01 mM; 64% inhibition at 0.01 mM Homo sapiens
bergapten 69% inhibition at 0.01 mM; 69% inhibition at 0.01 mM Homo sapiens
deoxyshikonin 67% inhibition at 0.01 mM; 67% inhibition at 0.01 mM Homo sapiens
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
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
embelin 57% inhibition at 0.01 mM; 57% inhibition at 0.01 mM Homo sapiens
gambogic acid 75% inhibition at 0.01 mM; 75% inhibition at 0.01 mM Homo sapiens
gossypol 75% inhibition at 0.01 mM; 75% inhibition at 0.01 mM Homo sapiens
menadione 55% inhibition at 0.01 mM; 55% inhibition at 0.01 mM Homo sapiens
myricetin 78% inhibition at 0.01 mM; 78% inhibition at 0.01 mM Homo sapiens
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
phenantridinone i.e. 6(5H)-phenantridinone; i.e. 6(5H)-phenantridinone Homo sapiens
Plumbagin 67% inhibition at 0.01 mM; 67% inhibition at 0.01 mM Homo sapiens
TIQ-A i.e. 4H-thieno[2,3-c]isoquinolin-5-one; i.e. 4H-thieno[2,3-c]isoquinolin-5-one Homo sapiens
trimethylpsoralen 61% inhibition at 0.01 mM; 61% inhibition at 0.01 mM Homo sapiens

Molecular Weight [Da]

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

Organism

Organism UniProt Comment Textmining
Homo sapiens Q460N3
-
-
Homo sapiens Q53GL7
-
-

Purification (Commentary)

Purification (Comment) Organism
HisTrap column chromatography Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
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

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

Synonyms

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

pH Optimum

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

IC50 Value

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