Literature summary for 1.14.18.1 extracted from

Lima, C.R.; Silva, J.R.; de Tassia Carvalho Cardoso, E.; Silva, E.O.; Lameira, J.; do Nascimento, J.L.; do Socorro Barros Brasil, D.; Alves, C.N.
Combined kinetic studies and computational analysis on kojic acid analogous as tyrosinase inhibitors (2014), Molecules, 19, 9591-9605 .

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Inhibitors

Inhibitors	Comment	Organism	Structure
2-ethyl-3-hydroxy-4H-pyran-4-one	-	Agaricus bisporus
3-hydroxy-1,2-dimethyl-4(1H)-pyridone	-	Agaricus bisporus
5-hydroxy-4-oxo-4H-pyran-2-carboxylic acid	-	Agaricus bisporus
kojic acid	-	Agaricus bisporus
additional information	the inhibition of tyrosinase by analogues of kojic acid, main interactions occurring between inhibitors-tyrosinase complexes and influence of divalent cation (Cu2+) in enzymatic inhibition are analysed using molecular docking, molecular dynamic simulations and linear interaction energy (LIE) method, using the three-dimensional structure of enzyme AbTYR in complex with inhibitor tropolone, PDB 2Y9X, overview. No inhibition by 3-hydroxy-2-methyl-4-pyrone. Tyrosinase displays various inhibition patterns	Agaricus bisporus
tropolone	-	Agaricus bisporus

Metals/Ions

Metals/Ions	Comment	Organism	Structure
Cu2+	the enzyme's catalytic site contains two divalent copper cations chelated by His61, His85, His94, His259, His263 and His294 catalytic amino acid residue	Agaricus bisporus

Natural Substrates/ Products (Substrates)

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

Organism

Organism	UniProt	Comment	Textmining
Agaricus bisporus	-	-	-

Substrates and Products (Substrate)

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

Synonyms

Synonyms	Comment	Organism
AbTYR	-	Agaricus bisporus

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
7.2	-	assay at	Agaricus bisporus

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
additional information	-	additional information	inhibition kinetic analysis	Agaricus bisporus
0.0008	-	tropolone	pH 7.2, temperature not specified in the publication	Agaricus bisporus
0.005	-	kojic acid	pH 7.2, temperature not specified in the publication	Agaricus bisporus
0.064	-	3-hydroxy-1,2-dimethyl-4(1H)-pyridone	pH 7.2, temperature not specified in the publication	Agaricus bisporus
0.145	-	5-hydroxy-4-oxo-4H-pyran-2-carboxylic acid	pH 7.2, temperature not specified in the publication	Agaricus bisporus
1	-	2-ethyl-3-hydroxy-4H-pyran-4-one	pH 7.2, temperature not specified in the publication	Agaricus bisporus

General Information

General Information	Comment	Organism
malfunction	excessive accumulation of melanin, due to the overexpression of the enzyme, leads to skin disorders such as age spots, freckles and malignant melanoma	Agaricus bisporus
physiological function	tyrosinase is a key enzyme in melanin synthesis	Agaricus bisporus

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Release 2023.1 (January 2023)