The p300 KAT inhibitor, A-485, inhibits melanogenesis and melanin content in human melanocytes
biorxiv(2024)
摘要
Hyperpigmentation disorders are commonly diagnosed dermatologic conditions that can be cosmetically distressing for patients and cause negative psychosocial impacts. There is a need to better understand the underlying pathophysiology of pigmentary disorders as well as develop improvements in the management of these disorders. Here, we evaluated a p300 (CBP/p300) histone acetyltransferase (HAT) inhibitor, A-485, to determine if epigenetically targeting melanogenesis could be of therapeutic value. We find that A-485 treatment of primary human melanocytes and SK-MEL-30 melanoma cells drastically reduces the mRNA and protein expression of MITF and DCT, genes involved in melanin synthesis, and that this is accompanied by a reduction in melanin content. These results suggest that epigenetically targeting melanin synthesis with the A-485 p300 HAT inhibitor may be beneficial for the treatment of hyperpigmentation disorders.
### Competing Interest Statement
RMA is a cofounder of Acylin Therapeutics and holds equity in the company. Acylin Therapeutics has an interest in developing epigenetic inhibitors, including A-485. RA and ARW have submitted intellectual property for utilizing A-485 to treat hyperpigmentation disorders through the Boston University Office of Technology Development.
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