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Literature summary for 3.2.1.143 extracted from

  • Formentini, L.; Arapistas, P.; Pittelli, M.; Jacomelli, M.; Pitozzi, V.; Menichetti, S.; Romani, A.; Giovannelli, L.; Moroni, F.; Chiarugi, A.
    Mono-galloyl glucose derivatives are potent poly(ADP-ribose) glycohydrolase (PARG) inhibitors and partially reduce PARP-1-dependent cell death (2008), Br. J. Pharmacol., 155, 1235-1249.
    View publication on PubMedView publication on EuropePMC
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Activating Compound

Activating Compound Comment Organism Structure
1-methyl-3-nitro-1-nitrosoguanidine
-
 Bos taurus

Inhibitors

Inhibitors Comment Organism Structure
1,2,3,4,6-pentakis-O-galloyl-beta-D-glucoside about 25% inhibition at 10 microM in vitro Bos taurus
1,3,6-tris-O-galloyl-beta-D-glucoside about 25% inhibition at 10 microM in vitro Bos taurus
3-galloyl-D-glucose about 50% inhibition at 1 microM, 65% inhibition at 10 microM, about 85% at 100 microM in vitro, no inhibitory effect in HeLa cell death at 10 microM, induced by methylating agent 1-methyl-3-nitro-1-nitrosoguanidine (100 microM), because cell-permeability is probably hindered Bos taurus
ADP-HPD about 40% inhibition at 1 microM, about 70% inhibition at 10 microM, about 85% inhibition at 100 microM in vitro Bos taurus
gallotannin 25% inhibition at 10 micorM in vitro, reduced cell death in HeLa cells at 3 and 6 h exposure Bos taurus
methyl 2-O-galloyl-beta-D-glucoside about 25% inhibition at 1 microM, 65% inhibition at 10 microM, about 85% inhibition at 100 microM in vitro Bos taurus
methyl 3-O-galloyl-beta-D-glucoside about 25% inhibition at 1 microM, 65% inhibition at 10 microM, about 85% inhibition at 100 microM in vitro Bos taurus
additional information gallotannin is a complex mixture of hydrolysable tannins, gallic acid and various galloyl glucose derivatives with up to 12 galloyl residues, from oak gall, that inhibits PARG; no inhibitory effect of 100 microM gallic acid, of 10 microM methyl gallate, of 10 microM 2,3-digalloyl-D-glucose, of 10 microM 2,3-digalloyl-O-methyl-D-glucose, of 10 microM 2,3-hexahydroxydiphenoyl-D-glucose, of 10 microM 2,3-di(3-galloyl,4,5-dihydroxy-benzoyl)-D-glucose, of 10 microM epigallocatechin gallate, and of 10 and 100 microM 3-galloyl-1,2-O-isopropylidene-alpha-D-glucose in vitro, the latter can act in vivo as cell-permeable precursor of 3-D-galloyl-D-glucose preventing poly(ADP-ribose) degradation, reduced cell death in HeLa cells at 3 and 6 h exposure (10 or 100 microM), cell death induction by methylating agent 1-methyl-3-nitro-1-nitrosoguanidine (100 microM), increased intracellular NAD content without 1-methyl-3-nitro-1-nitrosoguanidine, no effect in the presence of this agent Bos taurus
sanguinin H-6 about 50% inhibition at 10 microM in vitro Bos taurus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Bos taurus several isoforms, functions in embryonic development, genotixicity, cell cycle regulation, mitotic spindle assembly, development, differentiation, and cell death ?
-
 ?

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information several isoforms, functions in embryonic development, genotixicity, cell cycle regulation, mitotic spindle assembly, development, differentiation, and cell death Bos taurus ?
-
 ?
poly(ADP-ribose) + H2O tritium-labelled poly(ADP-ribose) produced by PARP-1 (poly(ADP-ribose) polymerase) with tritium-labelled NAD + sonicated DNA containing histones, and bovine albumin Bos taurus ADP-ribose + ADP-ribose oligomer
-
 ?

Synonyms

Synonyms Comment Organism
PARG
-
 Bos taurus
poly(ADP-ribose) glycohydrolase
-
 Bos taurus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.95
-
 enzyme for 240 min at 37°C Bos taurus 3-galloyl-D-glucose
3.2
-
 enzyme for 240 min at 37°C Bos taurus ADP-HPD
7.1
-
 enzyme for 240 min at 37°C Bos taurus methyl 3-O-galloyl-beta-D-glucoside
7.2
-
 enzyme for 240 min at 37°C Bos taurus methyl 2-O-galloyl-beta-D-glucoside