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Literature summary for 3.5.3.15 extracted from

  • Bozdag, M.; Dreker, T.; Henry, C.; Tosco, P.; Vallaro, M.; Fruttero, R.; Scozzafava, A.; Carta, F.; Supuran, C.T.
    Novel small molecule protein arginine deiminase 4 (PAD4) inhibitors (2013), Bioorg. Med. Chem. Lett., 23, 715-719.
    View publication on PubMed
Search for more literature for 3.5.3.15

Inhibitors

Inhibitors Comment Organism Structure
1-(2-{4-[(aminooxy)sulfinyl]phenyl}ethyl)guanidine hydrochloride 5% inhibition at 0.01 mM Homo sapiens
1-[3-(1H-imidazol-4-yl)propyl]-3-{2-[(4-phenyl-1,2,5-oxadiazol-3-yl)oxy]ethyl}guanidine hydrochloride 34% inhibition at 0.01 mM Homo sapiens
2-cyano-1-methyl-3-(2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl)guanidine 1% inhibition at 0.01 mM Homo sapiens
2-cyano-1-{2-[({2-[(diaminomethylidene)amino]-1,3-thiazol-5-yl}methyl)sulfanyl]ethyl}-3-(2-hydroxyethyl)guanidine ethanedioate 3% inhibition at 0.01 mM Homo sapiens
chloroamidine 35% inhibition at 0.01 mM Homo sapiens
N-[3-(1H-imidazol-4-yl)propyl]-N'-{3-[(5-oxo-4-phenyl-1,2lambda~5~,5-oxadiazol-3-yl)oxy]propyl}guanidine hydrochloride 36% inhibition at 0.01 mM Homo sapiens
oxalic acid 3-(N''-cyano-N'-{2-[({2-[(diaminomethylidene)amino]-1,3-thiazol-5-yl}methyl)sulfanyl]ethyl}carbamimidamido)propane-1,2-diyl dinitrate 8% inhibition at 0.01 mM Homo sapiens
oxalic acid 3-(N''-cyano-N'-{2-[({2-[(diaminomethylidene)amino]-1,3-thiazol-5-yl}methyl)sulfanyl]ethyl}carbamimidamido)propyl nitrate 10% inhibition at 0.01 mM Homo sapiens
oxalic acid 3-({2-[({5-[(dimethylamino)methyl]furan-2-yl}methyl)sulfanyl]ethyl}amino)-4-(methylamino)-1H-1lambda~4~,2,5-thiadiazol-1-one 9% inhibition at 0.01 mM Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.25
-
 Nalpha-benzoyl-L-arginine amide at pH 7.5 and 37°C Homo sapiens
0.41
-
 Nalpha-benzoyl-L-arginine at pH 7.5 and 37°C Homo sapiens
1.36
-
 Nalpha-benzoyl-L-arginine ethyl ester at pH 7.5 and 37°C Homo sapiens
1.66
-
 Nalpha-benzoyl-L-arginine methyl ester at pH 7.5 and 37°C Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
protein L-arginine + H2O Homo sapiens
-
 protein L-citrulline + NH3
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9UM07
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Nalpha-benzoyl-L-arginine + H2O
-
 Homo sapiens Nalpha-benzoyl-L-citrulline + NH3
-
 ?
Nalpha-benzoyl-L-arginine amide + H2O
-
 Homo sapiens Nalpha-benzoyl-L-citrulline amide + NH3
-
 ?
Nalpha-benzoyl-L-arginine ethyl ester + H2O 100% activity Homo sapiens Nalpha-benzoyl-L-citrulline ethyl ester + NH3
-
 ?
Nalpha-benzoyl-L-arginine methyl ester + H2O
-
 Homo sapiens Nalpha-benzoyl-L-citrulline methyl ester + NH3
-
 ?
protein L-arginine + H2O
-
 Homo sapiens protein L-citrulline + NH3
-
 ?

Synonyms

Synonyms Comment Organism
PAD4
-
 Homo sapiens
protein arginine deiminase 4
-
 Homo sapiens