title: A Novel Role of Serotonin Receptor 2B Agonist as an Anti-Melanogenesis Agent.
abstract: BW723C86, a serotonin receptor 2B agonist, has been investigated as a potential therapeutic for various conditions such as anxiety, hyperphagia and hypertension. However, the functional role of BW723C86 against melanogenesis remains unclear. In this study, we investigate the effect of serotonin receptor 2B (5-HTR2B) agonist on melanogenesis and elucidate the mechanism involved. BW723C86 reduced melanin synthesis and intracellular tyrosinase activity in melan-A cells and normal human melanocytes. The expression of melanogenesis-related proteins (tyrosinase, TRP-1 and TRP-2) and microphthalmia-associated transcription factor (MITF) in melan-A cells decreased after BW723C86 treatment. The promoter activity of MITF was also reduced by BW723C86 treatment. The reduced level of MITF was associated with inhibition of protein kinase A (PKA) and cAMP response element-binding protein (CREB) activation by BW723C86 treatment. These results suggest that the serotonin agonist BW723C86 could be a potential therapeutic agent for skin hyperpigmentation disorders.
authors.affiliation: Department of Genetic Engineering, Graduate School of Biotechnology, Kyung Hee University, Yongin 446-701, Korea. singey@naver.com.
authors.forename: Eun Ju
authors.initials: EJ
authors.lastname: Oh
authors.affiliation: Department of Genetic Engineering, Graduate School of Biotechnology, Kyung Hee University, Yongin 446-701, Korea. rystrong@khu.ac.kr.
authors.forename: Jong Il
authors.initials: JI
authors.lastname: Park
authors.affiliation: Department of Genetic Engineering, Graduate School of Biotechnology, Kyung Hee University, Yongin 446-701, Korea. jieun0405@khu.ac.kr.
authors.forename: Ji Eun
authors.initials: JE
authors.lastname: Lee
authors.affiliation: Department of Genetic Engineering, Graduate School of Biotechnology, Kyung Hee University, Yongin 446-701, Korea. audjoin2@naver.com.
authors.forename: Cheol Hwan
authors.initials: CH
authors.lastname: Myung
authors.affiliation: Department of Dermatology, Asan Medical Center, University of Ulsan College of Medicine, 388-1 Pungnap-dong Songpa-gu, Seoul 138-736, Korea. u2u2star@naver.com.
authors.forename: Su Yeon
authors.initials: SY
authors.lastname: Kim
authors.affiliation: Department of Dermatology, Asan Medical Center, University of Ulsan College of Medicine, 388-1 Pungnap-dong Songpa-gu, Seoul 138-736, Korea. csesnumd@gmail.com.
authors.forename: Sung Eun
authors.initials: SE
authors.lastname: Chang
authors.affiliation: Department of Genetic Engineering, Graduate School of Biotechnology, Kyung Hee University, Yongin 446-701, Korea. jshwang@khu.ac.kr.
authors.forename: Jae Sung
authors.initials: JS
authors.lastname: Hwang
mesh_terms: D000818:Animals; D002460:Cell Line; D015536:Down-Regulation; D006801:Humans; D007211:Indoles / Q000494:pharmacology*; D008543:Melanins / Q000378:metabolism*; D008544:Melanocytes / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D051379:Mice; D011505:Protein-Tyrosine Kinases / Q000235:genetics / Q000378:metabolism; D058826:Serotonin 5-HT2 Receptor Agonists / Q000494:pharmacology*; D015398:Signal Transduction / Q000187:drug effects; D013876:Thiophenes / Q000494:pharmacology*
chemical_list: C092430:1-(5-(2-thenyloxy)-1H-indol-3-yl)propan-2-amine; D007211:Indoles; D008543:Melanins; D058826:Serotonin 5-HT2 Receptor Agonists; D013876:Thiophenes; D011505:Protein-Tyrosine Kinases
keywords: BW723C86; CREB; MITF; PKA; melanogenesis