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dc.contributor.authorPeng, Yao
dc.contributor.authorZhao, Simeng
dc.contributor.authorWu, Yiran
dc.contributor.authorCao, Haijie
dc.contributor.authorXu, Yueming
dc.contributor.authorLiu, Xiaoyan
dc.contributor.authorShui, Wenqing
dc.contributor.authorCheng, Jianjun
dc.contributor.authorZhao, Suwen
dc.contributor.authorShen, Ling
dc.contributor.authorMa, Jun
dc.contributor.authorQuinn, Ronald J
dc.contributor.authorStevens, Raymond C
dc.contributor.authorZhong, Guisheng
dc.contributor.authorLiu, Zhi-Jie
dc.date.accessioned2020-02-07T03:59:19Z
dc.date.available2020-02-07T03:59:19Z
dc.date.issued2018
dc.identifier.issn2364-3439en_US
dc.identifier.doi10.1007/s41048-018-0047-1en_US
dc.identifier.urihttp://hdl.handle.net/10072/391207
dc.description.abstractG protein-coupled receptors (GPCRs) constitute the largest human protein family with over 800 members, which are implicated in many important medical conditions. Serotonin receptors belong to the aminergic GPCR subfamily and play important roles in physiological and psychological activities. Structural biology studies have revealed the structures of many GPCRs in atomic details and provide the basis for the identification and investigation of the potential ligands, which interact with and modulate the receptors. Here, an integrative approach combining a focused target-specific natural compound library, a thermal-shift-based screening method, affinity mass spectrometry, molecular docking, and in vitro as well as in vivo functional assay, was applied to identify (-)-crebanine and several other aporphine alkaloids as initial hits for a human serotonin receptor subtype, the 5-HT2C receptor. Further studies illuminated key features of their binding affinity, downstream signaling and tissue reaction, providing a molecular explanation for the interaction between (-)-crebanine and human 5-HT2C receptor.en_US
dc.description.peerreviewedYesen_US
dc.languageEnglish
dc.language.isoeng
dc.publisherSpringer Science and Business Media LLCen_US
dc.relation.ispartofpagefrom50en_US
dc.relation.ispartofpageto61en_US
dc.relation.ispartofissue1en_US
dc.relation.ispartofjournalBiophysics Reportsen_US
dc.relation.ispartofvolume4en_US
dc.subject.keywords5-HT2C receptoren_US
dc.subject.keywordsAlkaloidsen_US
dc.subject.keywordsGPCRen_US
dc.subject.keywordsNatural producten_US
dc.titleIdentification of natural products as novel ligands for the human 5-HT2C receptoren_US
dc.typeJournal articleen_US
dc.type.descriptionC1 - Articlesen_US
dcterms.bibliographicCitationPeng, Y; Zhao, S; Wu, Y; Cao, H; Xu, Y; Liu, X; Shui, W; Cheng, J; Zhao, S; Shen, L; Ma, J; Quinn, RJ; Stevens, RC; Zhong, G; Liu, Z-J, Identification of natural products as novel ligands for the human 5-HT2C receptor., Biophysics Reports, 2018, 4 (1), pp. 50-61en_US
dcterms.dateAccepted2017-05-15
dcterms.licensehttp://creativecommons.org/licenses/by/4.0/en_US
dc.date.updated2020-02-07T03:56:47Z
dc.description.versionVersion of Record (VoR)en_US
gro.rights.copyright© The Author(s) 2018. This article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made.en_US
gro.hasfulltextFull Text
gro.griffith.authorQuinn, Ronald J.


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