Target intelligence / Profile preview

Tyrosinase (TYR) (TYR)

Target
TYR
Molecular classification
Enzyme, Oxidoreductase, Copper-containing enzyme, Type I membrane glycoprotein
01

Overview

Tyrosinase is a copper-containing oxidase that serves as the rate-limiting enzyme in the biosynthesis of melanin, the pigment responsible for the color of skin, hair, and eyes [2, 8]. It catalyzes the hydroxylation of L-tyrosine to L-DOPA and the subsequent oxidation of L-DOPA to dopaquinone, which then polymerizes into eumelanin or pheomelanin [12, 15]. In mice, the tyrosinase gene (Tyr) is located at the albino locus, and mutations in this gene result in various forms of oculocutaneous albinism, such as the classic albino phenotype [4, 10]. Murine tyrosinase is a critical target in dermatological research for developing skin-lightening agents and in oncology as a tumor-associated antigen for melanoma immunotherapy [11, 14]. Because it is highly expressed in melanocytes and melanoma cells, it is used as a biomarker for disease progression and a target for enzyme-activated prodrugs [13, 16]. Therapeutic interventions include competitive inhibitors like hydroquinone and kojic acid to treat hyperpigmentation, as well as experimental vaccines designed to elicit an immune response against tyrosinase-expressing cancer cells [1, 6].

Other names
Monophenol monooxygenaseL-dopa oxidaseAlbino locus proteinSK29-L antigenEC 1.14.18.1
02

Mechanism of action

Competitive inhibition of the active site, suicide inactivation, or copper chelation to prevent the conversion of L-tyrosine and L-DOPA into melanin precursors [1, 3, 5].

03

Biological functions

Melanin biosynthesisPigmentationL-tyrosine hydroxylationL-DOPA oxidation
04

Disease associations

Oculocutaneous albinism type 1MelanomaHyperpigmentationVitiligo
05

Safety considerations

Skin irritationContact dermatitisExogenous ochronosisPotential for permanent depigmentation
06

Interacting drugs

Hydroquinone

6 more in the full profile.

07

Biomarkers

Melanin contentTyrosinase activityTYR mRNA expressionTYR protein levels

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