Downregulation of melanogenesis: drug discovery and therapeutic options

Drug Discov Today. 2017 Feb;22(2):282-298. doi: 10.1016/j.drudis.2016.09.016. Epub 2016 Sep 28.

Abstract

Melanin, primarily responsible in humans for hair, eye and skin pigmentation, is produced by melanocytes through a process called melanogenesis. However, the abnormal accumulation of melanin causes dermatological problems such as café-au-lait macules ephelides (freckles), solar lentigo (age spots) and melasma, as well as cancer and vitiligo. Hence the regulation of melanogenesis is very important for treating hyperpigmentary disorders. Numerous antimelanogenic agents that target tyrosinase activity and/or stability, melanosome maturation, transfer and trafficking, or melanogenesis-related signaling pathways have been developed. This article reviews recent advances in research and development of human tyrosinase and melanogenesis-related signaling pathway inhibitors. Attempts have been made to provide a complete description of the mechanism of action of inhibitors on various melanogenesis signaling pathways.

Publication types

  • Review

MeSH terms

  • Animals
  • Autophagy
  • Copper-Transporting ATPases / metabolism
  • Down-Regulation
  • Drug Discovery
  • Humans
  • Melanins / antagonists & inhibitors*
  • Melanins / metabolism*
  • Microphthalmia-Associated Transcription Factor / metabolism
  • Mitogen-Activated Protein Kinases / metabolism
  • Monophenol Monooxygenase / antagonists & inhibitors*
  • Monophenol Monooxygenase / metabolism
  • Nitric Oxide / antagonists & inhibitors
  • Signal Transduction
  • Wnt Signaling Pathway

Substances

  • Melanins
  • Microphthalmia-Associated Transcription Factor
  • Nitric Oxide
  • Monophenol Monooxygenase
  • Mitogen-Activated Protein Kinases
  • Copper-Transporting ATPases