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Literature summary for 3.2.1.143 extracted from

  • Islam, R.; Koizumi, F.; Kodera, Y.; Inoue, K.; Okawara, T.; Masutani, M.
    Design and synthesis of phenolic hydrazide hydrazones as potent poly(ADP-ribose) glycohydrolase (PARG) inhibitors (2014), Bioorg. Med. Chem. Lett., 24, 3802-3806.
    View publication on PubMed
Search for more literature for 3.2.1.143

Inhibitors

Inhibitors Comment Organism Structure
adenosine diphosphate (hydroxymethyl) pyrrolidinediol ADP-HPD Rattus norvegicus
additional information design and synthesis of phenolic hydrazide hydrazones as potent poly(ADP-ribose) glycohydrolase inhibitors, molecular docking analyses, overview Rattus norvegicus
N'',N'''-bis[(E)-(2,3,4-trihydroxyphenyl)methylidene]carbonohydrazide
-
 Rattus norvegicus
N'',N'''-bis[(E)-(3,4,5-trihydroxyphenyl)methylidene]carbonohydrazide
-
 Rattus norvegicus
N'1,N'3-bis[(E)-(2,3,4-trihydroxyphenyl)methylidene]propanedihydrazide
-
 Rattus norvegicus
N'1,N'3-bis[(E)-(3,4,5-trihydroxyphenyl)methylidene]propanedihydrazide
-
 Rattus norvegicus
N'1,N'4-bis[(E)-(2,3,4-trihydroxyphenyl)methylidene]butanedihydrazide
-
 Rattus norvegicus
N'1,N'4-bis[(E)-(3,4,5-trihydroxyphenyl)methylidene]butanedihydrazide
-
 Rattus norvegicus
N'1,N'4-bis[(E)-(3,4-dihydroxyphenyl)methylidene]benzene-1,4-dicarbohydrazide slight inhibition Rattus norvegicus
N'1,N'5-bis[(E)-(2,3,4-trihydroxyphenyl)methylidene]pentanedihydrazide
-
 Rattus norvegicus
N'1,N'5-bis[(E)-(3,4,5-trihydroxyphenyl)methylidene]pentanedihydrazide
-
 Rattus norvegicus
N'1-[(E)-(2,3,4-trihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3,4-trihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
 Rattus norvegicus
N'1-[(E)-(2,3,4-trihydroxyphenyl)methylidene]-N'4-[(Z)-(2,3,4-trihydroxyphenyl)methylidene]benzene-1,4-dicarbohydrazide
-
 Rattus norvegicus
N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
 Rattus norvegicus
N'1-[(E)-(2,4,6-trihydroxyphenyl)methylidene]-N'3-[(Z)-(2,4,6-trihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
 Rattus norvegicus
N'1-[(E)-(2,4,6-trihydroxyphenyl)methylidene]-N'4-[(Z)-(2,4,6-trihydroxyphenyl)methylidene]benzene-1,4-dicarbohydrazide
-
 Rattus norvegicus
N'1-[(E)-(2,4-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,4-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
 Rattus norvegicus
N'1-[(E)-(3,4,5-trihydroxyphenyl)methylidene]-N'3-[(Z)-(3,4,5-trihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
 Rattus norvegicus
N'1-[(E)-(3,4,5-trihydroxyphenyl)methylidene]-N'4-[(Z)-(3,4,5-trihydroxyphenyl)methylidene]benzene-1,4-dicarbohydrazide
-
 Rattus norvegicus
N'1-[(E)-(3,4-dihydroxyphenyl)methylidene]-N'3-[(Z)-(3,4-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
 Rattus norvegicus
N'1-[(E)-(4,6-dihydroxycyclohexa-1,3-dien-1-yl)methylidene]-N'4-[(E)-(2,4-dihydroxyphenyl)methylidene]benzene-1,4-dicarbohydrazide slight inhibition Rattus norvegicus
N'1-[(E)-(5,6-dihydroxycyclohexa-1,3-dien-1-yl)methylidene]-N'4-[(E)-(2,3-dihydroxyphenyl)methylidene]benzene-1,4-dicarbohydrazide slight inhibition Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Synonyms

Synonyms Comment Organism
PARG
-
 Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 assay at Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0001
-
 pH 7.5, 37°C Rattus norvegicus adenosine diphosphate (hydroxymethyl) pyrrolidinediol
0.001
-
 pH 7.5, 37°C Rattus norvegicus N'1-[(E)-(2,3,4-trihydroxyphenyl)methylidene]-N'4-[(Z)-(2,3,4-trihydroxyphenyl)methylidene]benzene-1,4-dicarbohydrazide
0.0016
-
 pH 7.5, 37°C Rattus norvegicus N'1,N'3-bis[(E)-(2,3,4-trihydroxyphenyl)methylidene]propanedihydrazide
0.0021
-
 pH 7.5, 37°C Rattus norvegicus N'1-[(E)-(3,4,5-trihydroxyphenyl)methylidene]-N'4-[(Z)-(3,4,5-trihydroxyphenyl)methylidene]benzene-1,4-dicarbohydrazide
0.0028
-
 pH 7.5, 37°C Rattus norvegicus N'',N'''-bis[(E)-(3,4,5-trihydroxyphenyl)methylidene]carbonohydrazide
0.0031
-
 pH 7.5, 37°C Rattus norvegicus N'1-[(E)-(2,3,4-trihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3,4-trihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
0.0031
-
 pH 7.5, 37°C Rattus norvegicus N'',N'''-bis[(E)-(2,3,4-trihydroxyphenyl)methylidene]carbonohydrazide
0.0032
-
 pH 7.5, 37°C Rattus norvegicus N'1-[(E)-(3,4,5-trihydroxyphenyl)methylidene]-N'3-[(Z)-(3,4,5-trihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
0.0082
-
 pH 7.5, 37°C Rattus norvegicus N'1,N'4-bis[(E)-(3,4,5-trihydroxyphenyl)methylidene]butanedihydrazide
0.0098
-
 pH 7.5, 37°C Rattus norvegicus N'1,N'4-bis[(E)-(2,3,4-trihydroxyphenyl)methylidene]butanedihydrazide
0.0099
-
 pH 7.5, 37°C Rattus norvegicus N'1-[(E)-(2,4,6-trihydroxyphenyl)methylidene]-N'4-[(Z)-(2,4,6-trihydroxyphenyl)methylidene]benzene-1,4-dicarbohydrazide
0.0139
-
 pH 7.5, 37°C Rattus norvegicus N'1,N'5-bis[(E)-(2,3,4-trihydroxyphenyl)methylidene]pentanedihydrazide
0.0148
-
 pH 7.5, 37°C Rattus norvegicus N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
0.0154
-
 pH 7.5, 37°C Rattus norvegicus N'1,N'3-bis[(E)-(3,4,5-trihydroxyphenyl)methylidene]propanedihydrazide
0.0188
-
 pH 7.5, 37°C Rattus norvegicus N'1-[(E)-(2,4,6-trihydroxyphenyl)methylidene]-N'3-[(Z)-(2,4,6-trihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
0.0192
-
 pH 7.5, 37°C Rattus norvegicus N'1-[(E)-(3,4-dihydroxyphenyl)methylidene]-N'3-[(Z)-(3,4-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
0.0274
-
 pH 7.5, 37°C Rattus norvegicus N'1,N'5-bis[(E)-(3,4,5-trihydroxyphenyl)methylidene]pentanedihydrazide
0.0401
-
 pH 7.5, 37°C Rattus norvegicus N'1-[(E)-(2,4-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,4-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide

General Information

General Information Comment Organism
malfunction genetic disruption of the enzyme leads to increased level of cell death by accumulation of poly(ADP-ribose) Rattus norvegicus
additional information the Glu752 residue plays an important role in the enzyme's catalytic activity by functioning as a general acid or base to protonate the 2'-OH of the ribose of the leaving group, and subsequently activating a water molecule for nucleophilic attack Rattus norvegicus
physiological function the enzyme is responsible for the degradation of poly(ADP-ribose) (PAR) polymers Rattus norvegicus