A novel synthetic Piper amide derivative NED-180 inhibits hyperpigmentation by activating the PI3K and ERK pathways and by regulating Ca2+ influx via TRPM1 channels
DC Field | Value | Language |
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dc.contributor.author | Hwang, Eunson | - |
dc.contributor.author | Lee, Taek Hwan | - |
dc.contributor.author | Lee, Wook-Joo | - |
dc.contributor.author | Shim, Won-Sik | - |
dc.contributor.author | Yeo, Eui-Ju | - |
dc.contributor.author | Kim, Sanghee | - |
dc.contributor.author | Kim, Sun Yeou | - |
dc.date.available | 2020-02-28T03:42:05Z | - |
dc.date.created | 2020-02-06 | - |
dc.date.issued | 2016-01 | - |
dc.identifier.issn | 1755-1471 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/8695 | - |
dc.description.abstract | Piper amides have a characteristic, unsaturated amide group and exhibit diverse biological activities, including proliferation and differentiation of melanocytes, although the molecular mechanisms underlying its antimelanogenesis effect remain unknown. We screened a selected chemical library of newly synthesized Piper amide derivatives and identified (E)-3-(4-(tert-butyl) phenyl)-N-(2,3-dihydrobenzo[b][1,4] dioxin-6-yl) acrylamide (NED-180) as one of the most potent compounds in suppressing melanogenesis. In murine melan-a melanocytes, NED-180 downregulated the expression of melanogenic regulatory proteins including tyrosinase, Tyrp1, Dct, and MITF. PI3K/ Akt-dependent phosphorylation of GSK3b by NED-180 decreases MITF phosphorylation and inhibits melanogenesis without any effects on cytotoxicity and proliferation. Furthermore, topical application of NED-180 significantly ameliorated UVB-induced skin hyperpigmentation in guinea pigs. Interestingly, data obtained using calcium imaging techniques suggested that NED-180 reduced the TPA-induced activation of TRPM1 (melastatin), which could explain the NED-180-induced inhibition of melanogenesis. All things taken together, NED-180 triggers activation of multiple pathways, such as PI3K and ERK, and inhibits TRPM1/TRPV1, leading to inhibition of melanogenesis. | - |
dc.language | 영어 | - |
dc.language.iso | en | - |
dc.publisher | WILEY | - |
dc.relation.isPartOf | PIGMENT CELL & MELANOMA RESEARCH | - |
dc.subject | TRANSCRIPTION FACTOR EXPRESSION | - |
dc.subject | MELANIN SYNTHESIS | - |
dc.subject | HUMAN MELANOCYTES | - |
dc.subject | ION CHANNELS | - |
dc.subject | SKIN COLOR | - |
dc.subject | MELANOGENESIS | - |
dc.subject | CELLS | - |
dc.subject | TYROSINASE | - |
dc.subject | PROTEIN | - |
dc.subject | MICROPHTHALMIA | - |
dc.title | A novel synthetic Piper amide derivative NED-180 inhibits hyperpigmentation by activating the PI3K and ERK pathways and by regulating Ca2+ influx via TRPM1 channels | - |
dc.type | Article | - |
dc.type.rims | ART | - |
dc.description.journalClass | 1 | - |
dc.identifier.wosid | 000366859300010 | - |
dc.identifier.doi | 10.1111/pcmr.12430 | - |
dc.identifier.bibliographicCitation | PIGMENT CELL & MELANOMA RESEARCH, v.29, no.1, pp.81 - 91 | - |
dc.identifier.scopusid | 2-s2.0-84949995257 | - |
dc.citation.endPage | 91 | - |
dc.citation.startPage | 81 | - |
dc.citation.title | PIGMENT CELL & MELANOMA RESEARCH | - |
dc.citation.volume | 29 | - |
dc.citation.number | 1 | - |
dc.contributor.affiliatedAuthor | Lee, Wook-Joo | - |
dc.contributor.affiliatedAuthor | Shim, Won-Sik | - |
dc.contributor.affiliatedAuthor | Yeo, Eui-Ju | - |
dc.contributor.affiliatedAuthor | Kim, Sun Yeou | - |
dc.type.docType | Article | - |
dc.subject.keywordAuthor | Piper amides | - |
dc.subject.keywordAuthor | melanogenesis | - |
dc.subject.keywordAuthor | TRPM1 | - |
dc.subject.keywordAuthor | skin lightening agent | - |
dc.subject.keywordPlus | TRANSCRIPTION FACTOR EXPRESSION | - |
dc.subject.keywordPlus | MELANIN SYNTHESIS | - |
dc.subject.keywordPlus | HUMAN MELANOCYTES | - |
dc.subject.keywordPlus | ION CHANNELS | - |
dc.subject.keywordPlus | SKIN COLOR | - |
dc.subject.keywordPlus | MELANOGENESIS | - |
dc.subject.keywordPlus | CELLS | - |
dc.subject.keywordPlus | TYROSINASE | - |
dc.subject.keywordPlus | PROTEIN | - |
dc.subject.keywordPlus | MICROPHTHALMIA | - |
dc.relation.journalResearchArea | Oncology | - |
dc.relation.journalResearchArea | Cell Biology | - |
dc.relation.journalResearchArea | Dermatology | - |
dc.relation.journalWebOfScienceCategory | Oncology | - |
dc.relation.journalWebOfScienceCategory | Cell Biology | - |
dc.relation.journalWebOfScienceCategory | Dermatology | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
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