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Myung, Kyungjae
Center for Genomic Integrity
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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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