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DC Field | Value | Language |
---|---|---|
dc.citation.endPage | 19696 | - |
dc.citation.number | 47 | - |
dc.citation.startPage | 19684 | - |
dc.citation.title | JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | - |
dc.citation.volume | 143 | - |
dc.contributor.author | Yoon, Nam Gu | - |
dc.contributor.author | Lee, Hakbong | - |
dc.contributor.author | Kim, So-Yeon | - |
dc.contributor.author | Hu, Sung | - |
dc.contributor.author | Kim, Darong | - |
dc.contributor.author | Yang, Sujae | - |
dc.contributor.author | Hong, Ki Bum | - |
dc.contributor.author | Lee, Ji Hoon | - |
dc.contributor.author | Kang, Soosung | - |
dc.contributor.author | Kim, Byung-Gyu | - |
dc.contributor.author | Myung, Kyungjae | - |
dc.contributor.author | Lee, Changwook | - |
dc.contributor.author | Kang, Byoung Heon | - |
dc.date.accessioned | 2023-12-21T14:50:59Z | - |
dc.date.available | 2023-12-21T14:50:59Z | - |
dc.date.created | 2021-12-13 | - |
dc.date.issued | 2021-12 | - |
dc.description.abstract | Heat shock protein 90 (Hsp90) family proteins are molecular chaperones that modulate the functions of various substrate proteins (clients) implicated in pro-tumorigenic pathways. In this study, the mitochondria-targeted antioxidant mitoquinone (MitoQ) was identified as a potent inhibitor of mitochondrial Hsp90, known as a tumor necrosis factor receptor-associated protein 1 (TRAP1). Structural analyses revealed an asymmetric bipartite interaction between MitoQ and the previously unrecognized drug binding sites located in the middle domain of TRAP1, believed to be a client binding region. MitoQ effectively competed with TRAP1 clients, and MitoQ treatment facilitated the identification of 103 TRAP1-interacting mitochondrial proteins in cancer cells. MitoQ and its redox-crippled SB-U014/SB-U015 exhibited more potent anticancer activity in vitro and in vivo than previously reported mitochondria-targeted TRAP1 inhibitors. The findings indicate that targeting the client binding site of Hsp90 family proteins offers a novel strategy for the development of potent anticancer drugs. | - |
dc.identifier.bibliographicCitation | JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, v.143, no.47, pp.19684 - 19696 | - |
dc.identifier.doi | 10.1021/jacs.1c07099 | - |
dc.identifier.issn | 0002-7863 | - |
dc.identifier.scopusid | 2-s2.0-85119488886 | - |
dc.identifier.uri | https://scholarworks.unist.ac.kr/handle/201301/55119 | - |
dc.identifier.url | https://pubs.acs.org/doi/10.1021/jacs.1c07099 | - |
dc.identifier.wosid | 000750622600003 | - |
dc.language | 영어 | - |
dc.publisher | AMER CHEMICAL SOC | - |
dc.title | Mitoquinone Inactivates Mitochondrial Chaperone TRAP1 by Blocking the Client Binding Site | - |
dc.type | Article | - |
dc.description.isOpenAccess | FALSE | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Multidisciplinary | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.type.docType | Article | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.subject.keywordPlus | REGULATES AUTOPHAGY | - |
dc.subject.keywordPlus | HSP90 INHIBITORS | - |
dc.subject.keywordPlus | PHOSPHORYLATION | - |
dc.subject.keywordPlus | SPECIFICITY | - |
dc.subject.keywordPlus | EFFICACY | - |
dc.subject.keywordPlus | CELLS | - |
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