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Discovery of thiophen-2-ylmethylene bis-dimedone derivatives as novel WRN inhibitors for treating cancers with microsatellite instability
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Yang, Hwa Sun | - |
dc.contributor.author | Kang, Mi So | - |
dc.contributor.author | Jang, Seon Yeong | - |
dc.contributor.author | Baek, Soo Yeon | - |
dc.contributor.author | Kim, Ji Won | - |
dc.contributor.author | Kim, Gyeong Un | - |
dc.contributor.author | Kim, Dong Woo | - |
dc.contributor.author | Ha, Jun Su | - |
dc.contributor.author | Kim, Jong Seung | - |
dc.contributor.author | Jung, Cheul Hee | - |
dc.contributor.author | Kim, Nam Jung | - |
dc.contributor.author | Cho, Sung Yup | - |
dc.contributor.author | Shin, Woong Hee | - |
dc.contributor.author | Lee, Ju Yong | - |
dc.contributor.author | Ko, Jun Su | - |
dc.contributor.author | Lee, An Soo | - |
dc.contributor.author | Keum, Gyo Chang | - |
dc.contributor.author | Lee, Sang Hee | - |
dc.contributor.author | Kang, Taek | - |
dc.date.accessioned | 2024-05-13T04:59:18Z | - |
dc.date.available | 2024-05-13T04:59:18Z | - |
dc.date.created | 2024-02-19 | - |
dc.date.created | 2024-02-19 | - |
dc.date.issued | 2024-02 | - |
dc.identifier.citation | Bioorganic & Medicinal Chemistry, Vol.100, p. 117588 | - |
dc.identifier.issn | 0968-0896 | - |
dc.identifier.uri | https://hdl.handle.net/10371/201497 | - |
dc.description.abstract | Microsatellite instability (MSI) is a hypermutable condition caused by DNA mismatch repair system defects, contributing to the development of various cancer types. Recent research has identified Werner syndrome ATP-dependent helicase (WRN) as a promising synthetic lethal target for MSI cancers. Herein, we report the first discovery of thiophen-2-ylmethylene bis-dimedone derivatives as novel WRN inhibitors for MSI cancer therapy. Initial computational analysis and biological evaluation identified a new scaffold for a WRN inhibitor. Subsequent SAR study led to the discovery of a highly potent WRN inhibitor. Furthermore, we demonstrated that the optimal compound induced DNA damage and apoptotic cell death in MSI cancer cells by inhibiting WRN. This study provides a new pharmacophore for WRN inhibitors, emphasizing their therapeutic potential for MSI cancers. | - |
dc.language | 영어 | - |
dc.publisher | Pergamon Press Ltd. | - |
dc.title | Discovery of thiophen-2-ylmethylene bis-dimedone derivatives as novel WRN inhibitors for treating cancers with microsatellite instability | - |
dc.type | Article | - |
dc.identifier.doi | 10.1016/j.bmc.2024.117588 | - |
dc.citation.journaltitle | Bioorganic & Medicinal Chemistry | - |
dc.identifier.wosid | 001175410100001 | - |
dc.identifier.scopusid | 2-s2.0-85183896561 | - |
dc.citation.startpage | 117588 | - |
dc.citation.volume | 100 | - |
dc.description.isOpenAccess | N | - |
dc.contributor.affiliatedAuthor | Cho, Sung Yup | - |
dc.contributor.affiliatedAuthor | Lee, Ju Yong | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.subject.keywordPlus | EMPIRICAL SCORING FUNCTIONS | - |
dc.subject.keywordPlus | WERNER SYNDROME HELICASE | - |
dc.subject.keywordPlus | SYNTHETIC LETHALITY | - |
dc.subject.keywordPlus | SMALL-MOLECULE | - |
dc.subject.keywordPlus | SYNDROME PROTEIN | - |
dc.subject.keywordPlus | DNA-DAMAGE | - |
dc.subject.keywordPlus | DOCKING | - |
dc.subject.keywordAuthor | Anticancer | - |
dc.subject.keywordAuthor | bis-Dimedone | - |
dc.subject.keywordAuthor | Microsatellite instability | - |
dc.subject.keywordAuthor | Synthetic lethality | - |
dc.subject.keywordAuthor | Thiophene | - |
dc.subject.keywordAuthor | WRN inhibitor | - |
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