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Discovery of alpha-mangostin as a novel competitive inhibitor against mutant isocitrate dehydrogenase-1
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| DC Field | Value | Language |
|---|---|---|
| dc.contributor.author | Kim, Hyo-Joon | - |
| dc.contributor.author | Fei, Xiang | - |
| dc.contributor.author | Cho, Seok-Cheol | - |
| dc.contributor.author | Choi, Bu Young | - |
| dc.contributor.author | Ahn, Hee-Chul | - |
| dc.contributor.author | Lee, Kyeong | - |
| dc.contributor.author | Seo, Seung-Yong | - |
| dc.contributor.author | Keum, Young-Sam | - |
| dc.date.accessioned | 2024-08-08T07:00:53Z | - |
| dc.date.available | 2024-08-08T07:00:53Z | - |
| dc.date.issued | 2015-12 | - |
| dc.identifier.issn | 0960-894X | - |
| dc.identifier.issn | 1464-3405 | - |
| dc.identifier.uri | https://scholarworks.dongguk.edu/handle/sw.dongguk/19226 | - |
| dc.description.abstract | Somatic heterozygous mutations of isocitrate dehydrogenase-1 (IDH1) are abundantly found in several types of cancer and strongly implicate altered metabolism in carcinogenesis. In the present study, we have identified alpha-mangostin as a novel selective inhibitor of mutant IDH1 (IDH1-R132H). We have observed that alpha-mangostin competitively inhibits the binding of alpha-ketoglutarate (alpha-KG) to IDH1-R132H. The structure-relationship study reveals that alpha-mangostin exhibits the strongest core inhibitor structure. Finally, we have observed that alpha-mangostin selectively promotes demethylation of 5-methylcytosine (5mC) and histone H3 trimethylated lysine residues in IDH1 (+/R132H) MCF10A cells, presumably via restoring the activity of cellular alpha-KG-dependent DNA hydroxylases and histone H3 lysine demethylases. Collectively, we provide evidence that alpha-mangostin selectively inhibits IDH1-R132H. (C) 2015 Elsevier Ltd. All rights reserved. | - |
| dc.format.extent | 7 | - |
| dc.language | 영어 | - |
| dc.language.iso | ENG | - |
| dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
| dc.title | Discovery of alpha-mangostin as a novel competitive inhibitor against mutant isocitrate dehydrogenase-1 | - |
| dc.type | Article | - |
| dc.publisher.location | 영국 | - |
| dc.identifier.doi | 10.1016/j.bmcl.2015.10.034 | - |
| dc.identifier.scopusid | 2-s2.0-84946557630 | - |
| dc.identifier.wosid | 000364535400034 | - |
| dc.identifier.bibliographicCitation | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.25, no.23, pp 5625 - 5631 | - |
| dc.citation.title | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
| dc.citation.volume | 25 | - |
| dc.citation.number | 23 | - |
| dc.citation.startPage | 5625 | - |
| dc.citation.endPage | 5631 | - |
| dc.type.docType | Article | - |
| dc.description.isOpenAccess | N | - |
| dc.description.journalRegisteredClass | sci | - |
| dc.description.journalRegisteredClass | scie | - |
| dc.description.journalRegisteredClass | scopus | - |
| dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
| dc.relation.journalResearchArea | Chemistry | - |
| dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
| dc.relation.journalWebOfScienceCategory | Chemistry, Organic | - |
| dc.subject.keywordPlus | CANCER | - |
| dc.subject.keywordPlus | IDH1 | - |
| dc.subject.keywordPlus | OPPORTUNITIES | - |
| dc.subject.keywordPlus | MUTATIONS | - |
| dc.subject.keywordPlus | CELLS | - |
| dc.subject.keywordAuthor | Isocitrate dehydrogenase-1 ( IDH1) | - |
| dc.subject.keywordAuthor | alpha-Mangostin | - |
| dc.subject.keywordAuthor | alpha-Ketoglutarate (alpha-KG) | - |
| dc.subject.keywordAuthor | (R)-2-Hydroxyglutarate (R-2HG) | - |
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Related Researcher
- Keum, Young Sam
- College of Pharmacy (Department of Pharmacy)