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Article

Discovery of α-mangostin as a novel competitive inhibitor against mutant isocitrate dehydrogenase-1.

Bioorganic & medicinal chemistry letters - 1 Dec 2015

Kim Hyo-Joon, Fei Xiang, Cho Seok-Cheol, Choi Bu Young, Ahn Hee-Chul, Lee Kyeong, Seo Seung-Yong, Keum Young-Sam

Abstract excerpt

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 α-mangostin as a novel selective inhibitor of mutant IDH1 (IDH1-R132H). We have observed that α-mangostin competitively inhibits the binding of α-ketoglutarate (α-KG) to IDH1-R132H. The...

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Source

Identifiers

PMID: 26508549
DOI: 10.1016/j.bmcl.2015.10.034

Genes

IDH1

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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