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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.available | 2020-02-28T06:45:12Z | - |
| dc.date.created | 2020-02-06 | - |
| dc.date.issued | 2015-12-01 | - |
| dc.identifier.issn | 0960-894X | - |
| dc.identifier.uri | https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/9821 | - |
| 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.language | 영어 | - |
| dc.language.iso | en | - |
| dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
| dc.relation.isPartOf | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
| dc.subject | CANCER | - |
| dc.subject | IDH1 | - |
| dc.subject | OPPORTUNITIES | - |
| dc.subject | MUTATIONS | - |
| dc.subject | CELLS | - |
| dc.title | Discovery of alpha-mangostin as a novel competitive inhibitor against mutant isocitrate dehydrogenase-1 | - |
| dc.type | Article | - |
| dc.type.rims | ART | - |
| dc.description.journalClass | 1 | - |
| dc.identifier.wosid | 000364535400034 | - |
| dc.identifier.doi | 10.1016/j.bmcl.2015.10.034 | - |
| dc.identifier.bibliographicCitation | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.25, no.23, pp.5625 - 5631 | - |
| dc.identifier.scopusid | 2-s2.0-84946557630 | - |
| dc.citation.endPage | 5631 | - |
| dc.citation.startPage | 5625 | - |
| dc.citation.title | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
| dc.citation.volume | 25 | - |
| dc.citation.number | 23 | - |
| dc.contributor.affiliatedAuthor | Fei, Xiang | - |
| dc.contributor.affiliatedAuthor | Seo, Seung-Yong | - |
| dc.type.docType | Article | - |
| 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) | - |
| dc.subject.keywordPlus | CANCER | - |
| dc.subject.keywordPlus | IDH1 | - |
| dc.subject.keywordPlus | OPPORTUNITIES | - |
| dc.subject.keywordPlus | MUTATIONS | - |
| dc.subject.keywordPlus | CELLS | - |
| dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
| dc.relation.journalResearchArea | Chemistry | - |
| dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
| dc.relation.journalWebOfScienceCategory | Chemistry, Organic | - |
| dc.description.journalRegisteredClass | scie | - |
| dc.description.journalRegisteredClass | scopus | - |
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Related Researcher
- Seo, Seung Yong
- Pharmacy (Dept.of Pharmacy)