DC Field | Value | Language |
---|---|---|
dc.contributor.author | Lee, Yeongju | - |
dc.contributor.author | Yoon, Heeseok | - |
dc.contributor.author | Hwang, Sung-Min | - |
dc.contributor.author | Shin, Min-Kyung | - |
dc.contributor.author | Lee, Ji Hoon | - |
dc.contributor.author | Oh, Misook | - |
dc.contributor.author | Im, Sin-Hyeog | - |
dc.contributor.author | Song, Jaeyoung | - |
dc.contributor.author | Lim, Hyun-Suk | - |
dc.date.accessioned | 2018-06-15T05:25:54Z | - |
dc.date.available | 2018-06-15T05:25:54Z | - |
dc.date.created | 2017-12-21 | - |
dc.date.issued | 2017-11 | - |
dc.identifier.issn | 0002-7863 | - |
dc.identifier.uri | https://oasis.postech.ac.kr/handle/2014.oak/50467 | - |
dc.description.abstract | The complex formation between transcription factors (TFs) and coactivator proteins is required for transcriptional activity, and thus disruption of aberrantly activated TF/coactivator interactions could be an attractive therapeutic strategy. However, modulation of such protein protein interactions (PPIs) has proven challenging. Here we report a cell-permeable, proteolytically stable, stapled helical peptide directly targeting nuclear receptor coactivator 1 (NCOA1), a coactivator required for the transcriptional activity of signal transducer and activator of transcription 6 (STAT6). We demonstrate that this stapled peptide disrupts the NCOA1/STAT6 complex, thereby repressing STAT6-mediated transcription. Furthermore, we solved the first crystal structure of a stapled peptide in complex with NCOA1. The stapled peptide therefore represents an invaluable chemical probe for understanding the precise role of the NCOA1/STAT6 interaction and an excellent starting point for the development of a novel class of therapeutic agents. | - |
dc.language | English | - |
dc.publisher | AMER CHEMICAL SOC | - |
dc.relation.isPartOf | JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | - |
dc.subject | TRANSCRIPTION FACTOR | - |
dc.subject | COACTIVATOR INTERACTION | - |
dc.subject | SIGNAL TRANSDUCER | - |
dc.subject | STAT6 | - |
dc.subject | MODULATORS | - |
dc.subject | ACTIVATOR | - |
dc.subject | PEPTIDES | - |
dc.subject | MOLECULE | - |
dc.subject | DOMAIN | - |
dc.subject | HELIX | - |
dc.title | Targeted Inhibition of the NCOA1/STAT6 Protein-Protein Interaction | - |
dc.type | Article | - |
dc.identifier.doi | 10.1021/jacs.7b08972 | - |
dc.type.rims | ART | - |
dc.identifier.bibliographicCitation | JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, v.139, no.45, pp.16056 - 16059 | - |
dc.identifier.wosid | 000415785900009 | - |
dc.date.tcdate | 2019-02-01 | - |
dc.citation.endPage | 16059 | - |
dc.citation.number | 45 | - |
dc.citation.startPage | 16056 | - |
dc.citation.title | JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | - |
dc.citation.volume | 139 | - |
dc.contributor.affiliatedAuthor | Lee, Yeongju | - |
dc.contributor.affiliatedAuthor | Shin, Min-Kyung | - |
dc.contributor.affiliatedAuthor | Im, Sin-Hyeog | - |
dc.contributor.affiliatedAuthor | Lim, Hyun-Suk | - |
dc.identifier.scopusid | 2-s2.0-85034227080 | - |
dc.description.journalClass | 1 | - |
dc.description.journalClass | 1 | - |
dc.description.wostc | 5 | - |
dc.type.docType | Article | - |
dc.subject.keywordPlus | TRANSCRIPTION FACTOR | - |
dc.subject.keywordPlus | COACTIVATOR INTERACTION | - |
dc.subject.keywordPlus | SIGNAL TRANSDUCER | - |
dc.subject.keywordPlus | STAT6 | - |
dc.subject.keywordPlus | MODULATORS | - |
dc.subject.keywordPlus | ACTIVATOR | - |
dc.subject.keywordPlus | PEPTIDES | - |
dc.subject.keywordPlus | MOLECULE | - |
dc.subject.keywordPlus | DOMAIN | - |
dc.subject.keywordPlus | HELIX | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Multidisciplinary | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Chemistry | - |
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