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Literature summary extracted from

  • Abbas, Q.; Raza, H.; Hassan, M.; Phull, A.R.; Kim, S.J.; Seo, S.Y.
    Acetazolamide inhibits the level of tyrosinase and melanin an enzyme kinetic, in vitro, in vivo, and in silico studies (2017), Chem. Biodivers., 14, e1700117 .
    View publication on PubMed

Application

EC Number Application Comment Organism
1.14.18.1 drug development acetazolamide is a good candidate for the inhibition of melanin biosynthesis. and might be used as a lead for developing the drugs for treatment of hyperpigmentary disorders and skin whitening Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.14.18.1 2-acetylamino-1,3,4-thiadiazole-5-sulfonamide acetazolamide or ACZ, in vitro, in vivo studies, and in silico docking studies. Inhibition kinetics, noncompetitive inhibition. Molecular dynamics simulations, overview Agaricus bisporus
1.14.18.1 2-acetylamino-1,3,4-thiadiazole-5-sulfonamide acetazolamide or ACZ, in vitro, in vivo studies, and in silico docking studies, His244, Asn260 and His85 are the major interacting residues in the binding site of the protein. Inhibition kinetics, acetazolamide is a noncompetitive inhibitor without cytotoxic effect. Molecular dynamics simulations, overview Danio rerio
1.14.18.1 2-acetylamino-1,3,4-thiadiazole-5-sulfonamide acetazolamideor ACZ, in vitro, in vivo, and in silico studies, inhibition kinetics. Acetazolamide is a a noncompetitive inhibitor without cytotoxic effect showing inhibition of tyrosinase expression in L-DOPA-induced melanoma. Molecular dynamics simulations, overview Homo sapiens
1.14.18.1 arbutin
-
 Danio rerio
1.14.18.1 arbutin
-
 Homo sapiens
1.14.18.1 hydroquinone
-
 Danio rerio
1.14.18.1 hydroquinone
-
 Homo sapiens
1.14.18.1 kojic acid
-
 Agaricus bisporus
1.14.18.1 kojic acid
-
 Danio rerio
1.14.18.1 kojic acid
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.14.18.1 0.172
-
 L-Dopa pH 6.8, 25°C Agaricus bisporus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.14.18.1 membrane membrane-bound Homo sapiens 16020
-
1.14.18.1 membrane membrane-bound Agaricus bisporus 16020
-
1.14.18.1 membrane membrane-bound Danio rerio 16020
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
1.14.18.1 Cu2+ a copper-containing enzyme Homo sapiens
1.14.18.1 Cu2+ a copper-containing enzyme Agaricus bisporus
1.14.18.1 Cu2+ a copper-containing enzyme Danio rerio

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.14.18.1 2 L-dopa + O2 Homo sapiens
-
 2 dopaquinone + 2 H2O
-
 ?
1.14.18.1 2 L-dopa + O2 Agaricus bisporus
-
 2 dopaquinone + 2 H2O
-
 ?
1.14.18.1 2 L-dopa + O2 Danio rerio
-
 2 dopaquinone + 2 H2O
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.14.18.1 Agaricus bisporus
-
-
-
1.14.18.1 Danio rerio
-
-
-
1.14.18.1 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.14.18.1 A-375 cell
-
 Homo sapiens
-
1.14.18.1 commercial preparation
-
 Agaricus bisporus
-
1.14.18.1 melanoma cell
-
 Homo sapiens
-
1.14.18.1 skin
-
 Homo sapiens
-
1.14.18.1 skin
-
 Danio rerio
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.14.18.1 2 L-dopa + O2
-
 Homo sapiens 2 dopaquinone + 2 H2O
-
 ?
1.14.18.1 2 L-dopa + O2
-
 Agaricus bisporus 2 dopaquinone + 2 H2O
-
 ?
1.14.18.1 2 L-dopa + O2
-
 Danio rerio 2 dopaquinone + 2 H2O
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.14.18.1 mushroom tyrosinase
-
 Agaricus bisporus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.14.18.1 25
-
 assay at Agaricus bisporus
1.14.18.1 25
-
 in vitro assay at Homo sapiens
1.14.18.1 37
-
 in vivo assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.14.18.1 6.8
-
 assay at Homo sapiens
1.14.18.1 6.8
-
 assay at Agaricus bisporus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.14.18.1 0.007895
-
 2-acetylamino-1,3,4-thiadiazole-5-sulfonamide pH 6.8, 25°C Homo sapiens
1.14.18.1 0.01261
-
 2-acetylamino-1,3,4-thiadiazole-5-sulfonamide pH 6.8, 25°C Agaricus bisporus
1.14.18.1 0.01684
-
 kojic acid pH 6.8, 25°C Homo sapiens

General Information

EC Number General Information Comment Organism
1.14.18.1 malfunction after 72 h of treatment with inhibitors acetazolamide and kojic acid, acetazolamide at 0.04 mM significantly decreases the embryos pigmentation to 40.8% of untreated embryos, while kojic acid at 0.04 mM decreases only 25.0% of pigmentation. Phenotype, overview Danio rerio
1.14.18.1 malfunction enzyme inhibition reduces melanogenesis Homo sapiens
1.14.18.1 additional information molecular docking and molecular dynamic simulation Homo sapiens
1.14.18.1 additional information molecular docking and molecular dynamic simulation Danio rerio