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Screening of Kit inhibitors: suppression of Kit signaling and melanogenesis by emodin by Seong Jin Lee; Daeyoung Jeong; Woo‐Kyu Park; Jae Yang Kong; Gildon Choi; Hojeong Kim; Sangjin Kang; Heeyeong Cho is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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## Abstract In search of novel antipigmentation agents, a set of 3,840 compounds with natural‐like synthetic or natural origin were screened against Kit (stem cell factor receptor). Emodin from the seed of __Cassia tora__ and baicalin from __Scutellariae__ radix showed potent inhibitory effects (IC~50~ = 4.9 and 9.0 mm, respectively) on the phosphorylation of Kit. Emodin also blocked other receptor tyrosine kinase activities, such as epithelial growth factor receptor (EGFR), vascular endothelial growth factor receptor 2 (VEGFR‐2), fibroblast growth factor receptor 1 (FGFR‐1), platelet‐derived growth factor receptor b (PDGFR‐b). In contrast to emodin, aloe‐emodin did not inhibit Kit activity at all. Emodin also blocked the cellular kinase activities of Kit and its down‐stream p44/42 mitogen activated protein kinase (MAPK) in MO7e cells and human primary melanocytes. Emodin strongly suppressed the melanin synthesis triggered by stem cell factor (SCF) treatment. Also, emodin showed almost no toxicity up to 10 mm on cultured melanocytes as reported previously by other researchers. The results indicate that emodin is a good candidate for the development of antipigmentation agents since

Who reads Screening of Kit inhibitors: suppression of Kit signaling and melanogenesis by emodin?

Author

Seong Jin Lee; Daeyoung Jeong; Woo‐Kyu Park; Jae Yang Kong; Gildon Choi; Hojeong Kim; Sangjin Kang; Heeyeong Cho

Publisher

John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley (ISSN 0951-418X)

Published

2009

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)