A small molecule inhibitor of Mitf‐E‐box DNA binding and its depigmenting effect in melan‐a cells

Abstract

The results show that Compound #17 is the first small molecule inhibitor of Mitf-E-box DNA binding with depigmenting activity.

Asiaticoside, a component of Centella asiatica, inhibits melanogenesis in B16F10 mouse melanoma

“…4, asiaticoside inhibits melanogenesis by interfering with the DNA binding of MITF. Similarly, Um et al (25) reported that {1-[2-(4-chloro-phenoxy)-ethyl]-1H-benzoimidazol-2-ylsulfanyl}-acetic acid inhibits melanogenesis by interfering with direct MITF binding to E-box DNA. In addition, MITF DNA binding is inhibited by PIAS3, a protein inhibitor of activated signal transduction and activator of transcription 3 (26).…”

Making a melanoma: Molecular and cellular changes underlying melanoma initiation

“…Along with regulation of neural crest genes, the expression and function of the MITF melanocyte specification factor is important in melanomas. Inhibition of MITF in melanomas can lead to apoptosis and cell cycle arrest (Du et al., 2004; McGill et al., 2002), and targeting MITF activity with small molecule inhibitors has been pursued as a therapeutic approach (Faloon et al., 2010; Um et al., 2012; Yokoyama et al., 2011). The expression level of MITF is critical to its function in melanocyte development and melanomas.…”