Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Liu, S.; Ji, S.; Yu, Z.J.; Wang, H.L.; Cheng, X.; Li, W.J.; Jing, L.; Yu, Y.; Chen, Q.; Yang, L.L.; Li, G.B.; Wu, Y.
    Structure-based discovery of new selective small-molecule sirtuin 5 inhibitors (2018), Chem. Biol. Drug Des., 91, 257-268 .
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.3.1.B43 gene SIRT5, recombinant expression of N-terminally His-tagged enzyme in Escherichia coli strain Transetta(DE3) Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.B43 2-cyano-3-[5-(4-cyanophenyl)furan-2-yl]-N-(3,4-dimethylphenyl)propanamide
-
 Homo sapiens
2.3.1.B43 2-cyano-N-(3,4-dimethylphenyl)-3-[5-(4-nitrophenyl)furan-2-yl]propanamide
-
 Homo sapiens
2.3.1.B43 3',5'-dimethyl-1'-phenyl-1H,1'H-[3,4'-bipyrazole]-5-carboxylic acid 21.54% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 3-chloro-5-(3,4-dimethoxyphenyl)-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine-2-carboxylic acid 30.85% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 3-hydroxy-5-(morpholine-4-sulfonyl)naphthalene-2-carboxylic acid 9.2% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 3-hydroxy-5-[(prop-2-en-1-yl)sulfamoyl]naphthalene-2-carboxylic acid 17.43% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 3-[3-[5-(4-carboxyphenyl)furan-2-yl]-2-cyanopropanamido]benzoic acid
-
 Homo sapiens
2.3.1.B43 3-[5-[2-cyano-3-(3,4-dimethylanilino)-3-oxopropyl]furan-2-yl]benzoic acid
-
 Homo sapiens
2.3.1.B43 4-(3,4-dimethyl-6-oxopyrano[2,3-c]pyrazol-1(6H)-yl)benzoic acid 18.70% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 4-(5-[(Z)-[1-(3-chloro-4-methylphenyl)-3-methyl-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene]methyl]furan-2-yl)benzoic acid 94.3% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 4-(5-[2-cyano-3-[(2,3-dihydro-1,4-benzodioxin-6-yl)amino]-3-oxopropyl]furan-2-yl)benzoic acid
-
 Homo sapiens
2.3.1.B43 4-(5-[2-cyano-3-[3-(methylcarbamoyl)anilino]-3-oxopropyl]furan-2-yl)benzoic acid
-
 Homo sapiens
2.3.1.B43 4-(5-[2-cyano-3-[4-cyano-3-(trifluoromethyl)anilino]-3-oxopropyl]furan-2-yl)benzoic acid
-
 Homo sapiens
2.3.1.B43 4-(5-[3-[(2H-1,3-benzodioxol-5-yl)amino]-2-cyano-3-oxopropyl]furan-2-yl)benzoic acid
-
 Homo sapiens
2.3.1.B43 4-(5-[3-[4-chloro-3-(trifluoromethyl)anilino]-2-cyano-3-oxopropyl]furan-2-yl)benzoic acid
-
 Homo sapiens
2.3.1.B43 4-(6-tert-butyl-2H-1,3-benzoxazin-3(4H)-yl)benzoic acid 24.54% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 4-([(Z)-[2-(2-bromophenyl)-5-oxo-1,3-oxazol-4(5H)-ylidene]methyl]amino)benzoic acid 34.24% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 4-[(4Z)-3-methyl-5-oxo-4-[(2E)-3-phenylprop-2-en-1-ylidene]-4,5-dihydro-1H-pyrazol-1-yl]benzoic acid 77.26% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 4-[(E)-(4-hydroxyphenyl)diazenyl]benzoic acid 51.3% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 4-[(E)-(6-hydroxyquinolin-5-yl)diazenyl]benzoic acid 61.3% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 4-[(E)-[(4-bromo-3-chloro-2-hydroxyphenyl)methylidene]amino]benzoic acid 33.66% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 4-[5-[(1E)-3-(4-chloro-3-nitroanilino)-2-cyano-3-oxoprop-1-en-1-yl]furan-2-yl]benzoic acid 97.14% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 4-[5-[2-cyano-3-(3,4-dimethoxyanilino)-3-oxopropyl]furan-2-yl]benzoic acid
-
 Homo sapiens
2.3.1.B43 4-[5-[2-cyano-3-(3,4-dimethylanilino)-3-oxopropyl]furan-2-yl]-3-fluorobenzoic acid
-
 Homo sapiens
2.3.1.B43 4-[5-[2-cyano-3-(3,4-dimethylanilino)-3-oxopropyl]furan-2-yl]-3-methylbenzoic acid
-
 Homo sapiens
2.3.1.B43 4-[5-[2-cyano-3-(3,4-dimethylanilino)-3-oxopropyl]furan-2-yl]benzoic acid
-
 Homo sapiens
2.3.1.B43 4-[5-[2-cyano-3-(3,5-dichloroanilino)-3-oxopropyl]furan-2-yl]benzoic acid
-
 Homo sapiens
2.3.1.B43 4-[5-[2-cyano-3-(3,5-dimethylanilino)-3-oxopropyl]furan-2-yl]benzoic acid
-
 Homo sapiens
2.3.1.B43 4-[5-[2-cyano-3-(4-cyano-3-fluoroanilino)-3-oxopropyl]furan-2-yl]benzoic acid competitive inhibitor Homo sapiens
2.3.1.B43 4-[5-[3-(3-acetamidoanilino)-2-cyano-3-oxopropyl]furan-2-yl]benzoic acid
-
 Homo sapiens
2.3.1.B43 5-(4-hydroxy-2,2-dimethyloxan-4-yl)-1,2-oxazole-3-carboxylic acid 17.41% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 5-(4-methylphenyl)-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine-2-carboxylic acid 11.08% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 5-[(E)-(5-hydroxy-3-methyl-1-phenyl-1H-pyrazol-4-yl)diazenyl]-4H-pyrazole-3-carboxylic acid 70.03% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 6-carboxy-5-methyl-3-[2-(3-methylpiperidin-1-yl)-2-oxoethyl]-4-oxo-4,4a-dihydrothieno[2,3-d]pyrimidin-3-ium 15.43% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 7-(diethylamino)-2-oxo-2H-1-benzopyran-3-carboxylic acid 28.91% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 methyl 4-[5-[2-cyano-3-(3,4-dimethylanilino)-3-oxopropyl]furan-2-yl]benzoate
-
 Homo sapiens
2.3.1.B43 additional information no inhibition by (2E)-4,4-dihydroxy-N-[4-[(5-methyl-1,2-oxazol-3-yl)sulfamoyl]phenyl]but-2-enamide; structure-based discovery of selective small-molecul sirtuin 5 inhibitors. Synthesis of (E)-2-cyano-N-phenyl-3-(5-phenylfuran-2-yl)acrylamide derivatives/analogues, docking study, structure-activity relationship analyses, overview. No inhibition by 14 at 0.1 mM Homo sapiens
2.3.1.B43 nicotinamide NAM, 70.57% inhibition at 0.1 mM Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.B43 Homo sapiens Q9NXA8
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.3.1.B43 recombinant N-terminally His-tagged enzyme from Escherichia coli strain Transetta(DE3) by nickel affinity chromatography, tag cleavage by TEV protease, and ultrafiltration Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.B43 NAD+ + benzyl-(N6-succinyl)Lys-7-amido-4-methylcoumarin fluorogenic substrate Homo sapiens nicotinamide + benzyl-Lys-7-amido-4-methylcoumarin + 2'-O-succinyl-ADP-ribose
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.1.B43 SIRT5
-
 Homo sapiens
2.3.1.B43 sirtuin 5
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.3.1.B43 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.3.1.B43 8
-
 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.3.1.B43 NAD+
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.B43 0.0457
-
 pH 8.0, 37°C, recombinant enzyme Homo sapiens nicotinamide