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Literature summary for 1.14.18.1 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
Search for more literature for 1.14.18.1

Application

Application Comment Organism
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

Inhibitors Comment Organism Structure
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
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
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
arbutin
-
 Danio rerio
arbutin
-
 Homo sapiens
hydroquinone
-
 Danio rerio
hydroquinone
-
 Homo sapiens
kojic acid
-
 Agaricus bisporus
kojic acid
-
 Danio rerio
kojic acid
-
 Homo sapiens

KM Value [mM]

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

Localization

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

Metals/Ions

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Agaricus bisporus
-
-
-
Danio rerio
-
-
-
Homo sapiens
-
-
-

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
mushroom tyrosinase
-
 Agaricus bisporus

Temperature Optimum [°C]

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

pH Optimum

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

Ki Value [mM]

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

General Information

General Information Comment Organism
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
malfunction enzyme inhibition reduces melanogenesis Homo sapiens
additional information molecular docking and molecular dynamic simulation Homo sapiens
additional information molecular docking and molecular dynamic simulation Danio rerio