L-765,314 Suppresses Melanin Synthesis by Regulating Tyrosinase Activity

Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Jinhwan KimYoungsup Song

Abstract

Although melanin production is a key self-defense mechanism against ultraviolet radiation (UVR)-induced skin damage, uneven or excessive deposition of melanin causes hyperpigmentary disorders. Currently available whitening agents are unsatisfactory because of issues with efficacy and safety. To develop more effective depigmenting agents, we performed high-throughput melanin content assay screening using the B16F10 melanoma cell line and identified L-765,314 as a drug that suppressed melanin production in cultured melanocytes in a dose-dependent manner as well as cAMP- or 12-O-tetradecanoylphorbol 13-acetate (TPA)-stimulated melanin production without cytotoxicity. Interestingly, melanogenic gene expression was not altered by L-765,314. Rather, diminished melanin production by L-765,314 appeared to be caused by downregulation of tyrosinase activity via inhibition of protein kinase C (PKC). Because L-765,314 did not show any adverse effect in melanocytes, altogether our data suggest that L-765,314 could be a potential therapeutic candidate for skin hyperpigmentary disorders and further discovery of selective inhibitors targeting PKC might be a promising strategy for the development of depigmenting agents to treat hyperpigmentary ...Continue Reading

References

Nov 1, 1989·The Journal of Investigative Dermatology·P R Gordon, B A Gilchrest
Jan 1, 1984·Journal of Cardiovascular Pharmacology·S Z Langer, P E Hicks
Nov 1, 1995·The Journal of Investigative Dermatology·A E AllanB A Gilchrest
Oct 1, 1994·Archives of Biochemistry and Biophysics·M RacchiM Trabucchi
Apr 1, 1994·Journal of Natural Products·I KuboY Yokokawa
May 29, 1999·The Journal of Biological Chemistry·H Y ParkB A Gilchrest
Feb 14, 2004·The Journal of Investigative Dermatology·Hee-Young ParkBarbara A Gilchrest
Aug 27, 2004·Journal of Molecular Histology·Reiko TakeyamaSeiji Kawana
Apr 26, 2008·Photochemistry and Photobiology·Michaela Brenner, Vincent J Hearing
Aug 13, 2011·Pigment Cell & Melanoma Research·Andrzej SlominskiJohn Pawelek
May 10, 2017·Pigment Cell & Melanoma Research·Seunghyun BangSung Eun Chang
Sep 27, 2018·Physiological Reviews·Liliana D'Alba, Matthew D Shawkey

❮ Previous
Next ❯

Methods Mentioned

BETA
reverse transcription PCR

Software Mentioned

GraphPad Prism

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.