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Updated: Jun 22, 2026

A 3D Organotypic Melanoma Spheroid Skin Model
Published on: May 18, 2018
Tyrosinase activated melanoma prodrugs
Samaila Jawaid1, Tariq H Khan, Helen M I Osborn
1School of Pharmacy, University of Reading, Whiteknights, Reading, UK. h.m.i.osborn@rdg.ac.uk
Abstract:
Metastatic malignant melanoma remains a highly aggressive form of skin cancer for which no reliable methods for treatment exist. Given the increasing incidence of this cancer, considerable attention has focused on the development of new and improved methods for tackling this disease. Within this article, methods for treating melanoma are reviewed and discussed with particular attention focusing on prodrugs that are activated by the tyrosinase enzyme. This enzyme is up-regulated and is of elevated activity within malignant melanomas compared with healthy melanocytes, providing an ideal in-situ tool for the activation of melanoma prodrugs. By way of background to the prodrug strategies discussed within this review, the causes of melanoma, the enzymology of tyrosinase, and the chemistry of the biosynthetic pathways associated with melanogenesis are presented. Aspects of the design, mode of action, and biological profiles of key prodrugs that are activated by tyrosinase, and that show potential for the treatment of melanoma, are then presented and compared.
Insights
Prodrugs activated by the tyrosinase enzyme offer a promising new strategy for treating metastatic malignant melanoma. This approach leverages the enzyme
Area of Science:
- Oncology
- Dermatology
- Biochemistry
Background:
- Metastatic malignant melanoma is an aggressive skin cancer with limited treatment options.
- Tyrosinase enzyme activity is elevated in malignant melanomas compared to healthy melanocytes.
- Melanogenesis involves complex biosynthetic pathways crucial for understanding melanoma biology.
Purpose of the Study:
- To review and discuss prodrug strategies for melanoma treatment.
- To focus on prodrugs activated by the tyrosinase enzyme for targeted therapy.
- To explore the potential of tyrosinase-activated prodrugs in combating melanoma.
Main Methods:
- Review of existing literature on melanoma treatment methods.
- Analysis of tyrosinase enzymology and melanogenesis pathways.
- Comparison of the design, mode of action, and biological profiles of key tyrosinase-activated prodrugs.
Main Results:
- Tyrosinase enzyme's up-regulation in melanoma provides a target for in-situ prodrug activation.
- Several prodrugs activated by tyrosinase show potential for melanoma treatment.
- Understanding of prodrug design and biological activity is crucial for therapeutic development.
Conclusions:
- Tyrosinase-activated prodrugs represent a promising therapeutic avenue for metastatic malignant melanoma.
- Targeted drug activation by tyrosinase offers a strategy to overcome current treatment limitations.
- Further research into these prodrugs could lead to improved clinical outcomes for melanoma patients.
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