Discovery of G Protein-Biased Ligands against 5-HT7R
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Lee, Jieon | - |
dc.contributor.author | Kwag, Rina | - |
dc.contributor.author | Lee, Soyeon | - |
dc.contributor.author | Kim, Doyoung | - |
dc.contributor.author | Woo, Jiwan | - |
dc.contributor.author | Cho, Yakdol | - |
dc.contributor.author | Kim, Hak Joong | - |
dc.contributor.author | Kim, Jeongjin | - |
dc.contributor.author | Jeon, Byungsun | - |
dc.contributor.author | Choo, Hyunah | - |
dc.date.accessioned | 2021-11-18T08:40:41Z | - |
dc.date.available | 2021-11-18T08:40:41Z | - |
dc.date.created | 2021-08-30 | - |
dc.date.issued | 2021-06-10 | - |
dc.identifier.issn | 0022-2623 | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/127854 | - |
dc.description.abstract | There has been significant attention concerning the biased agonism of G protein-coupled receptors (GPCRs), and it has resulted in various pharmacological benefits. 5-HT7R belongs to a GPCR, and it is a promising pharmaceutical target for the treatment of neurodevelopmental and neuropsychiatric disorders. Based on our previous research, we synthesized a series of 6-chloro-2'-methoxy biphenyl derivatives 1, 2, and 3 with a variety of amine scaffolds. These compounds were evaluated for their binding affinities to 5-HTR subtypes and their functional selectivity toward the Gs protein and the beta-arrestin signaling pathways of 5-HT7R. Among them, 2-(6-chloro- 2'-methoxy-[1,1'-biphenyl]-3-yl)-N-ethylethan-1-amine, 2b, was found to be a G-protein-biased ligand of 5-HT7R. In an in vivo study with Shank3 transgenic mice, the self-grooming behavior test was performed with 2b, which increased the duration of self-grooming. The experiments further suggested that 5-HT7R is associated with autism spectrum disorders (ASDs) and could be a therapeutic target for the treatment of stereotypy in ASDs. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | AMER CHEMICAL SOC | - |
dc.subject | AUTISM SPECTRUM DISORDER | - |
dc.subject | SEROTONIN RECEPTOR 7 | - |
dc.subject | OXIDATIVE IODINATION | - |
dc.subject | DEACTIVATED ARENES | - |
dc.subject | AGONIST | - |
dc.subject | STIMULATION | - |
dc.subject | ACTIVATION | - |
dc.subject | CLONING | - |
dc.subject | UNIQUE | - |
dc.subject | DRUG | - |
dc.title | Discovery of G Protein-Biased Ligands against 5-HT7R | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Kim, Hak Joong | - |
dc.identifier.doi | 10.1021/acs.jmedchem.1c00110 | - |
dc.identifier.scopusid | 2-s2.0-85108021367 | - |
dc.identifier.wosid | 000662187100023 | - |
dc.identifier.bibliographicCitation | JOURNAL OF MEDICINAL CHEMISTRY, v.64, no.11, pp.7453 - 7467 | - |
dc.relation.isPartOf | JOURNAL OF MEDICINAL CHEMISTRY | - |
dc.citation.title | JOURNAL OF MEDICINAL CHEMISTRY | - |
dc.citation.volume | 64 | - |
dc.citation.number | 11 | - |
dc.citation.startPage | 7453 | - |
dc.citation.endPage | 7467 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.subject.keywordPlus | AUTISM SPECTRUM DISORDER | - |
dc.subject.keywordPlus | SEROTONIN RECEPTOR 7 | - |
dc.subject.keywordPlus | OXIDATIVE IODINATION | - |
dc.subject.keywordPlus | DEACTIVATED ARENES | - |
dc.subject.keywordPlus | AGONIST | - |
dc.subject.keywordPlus | STIMULATION | - |
dc.subject.keywordPlus | ACTIVATION | - |
dc.subject.keywordPlus | CLONING | - |
dc.subject.keywordPlus | UNIQUE | - |
dc.subject.keywordPlus | DRUG | - |
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