Synthesis and biological evaluation of flavonoid-based IP6K2 inhibitors

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dc.contributor.authorAhn, Myunghwanko
dc.contributor.authorPark, Seung Eunko
dc.contributor.authorChoi, Jiyeonko
dc.contributor.authorChoi, Jiahnko
dc.contributor.authorChoi, Doyoungko
dc.contributor.authorAn, Dongjuko
dc.contributor.authorJeon, Hayoungko
dc.contributor.authorOh, Soowhanko
dc.contributor.authorLee, Kihoko
dc.contributor.authorKim, Jaehoonko
dc.contributor.authorJang, Jaebongko
dc.contributor.authorKim, Seyunko
dc.contributor.authorByun, Youngjooko
dc.date.accessioned2023-05-02T08:00:15Z-
dc.date.available2023-05-02T08:00:15Z-
dc.date.created2023-05-02-
dc.date.issued2023-12-
dc.identifier.citationJOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, v.38, no.1-
dc.identifier.issn1475-6366-
dc.identifier.urihttp://hdl.handle.net/10203/306414-
dc.description.abstractInositol polyphosphates (IPs) are a group of inositol metabolites that act as secondary messengers for external signalling cues. They play various physiological roles such as insulin release, telomere length maintenance, cell metabolism, and aging. Inositol hexakisphosphate kinase 2 (IP6K2) is a key enzyme that produces 5-diphosphoinositol 1,2,3,4,6-pentakisphosphate (5-IP7), which influences the early stages of glucose-induced exocytosis. Therefore, regulation of IP6Ks may serve as a promising strategy for treating diseases such as diabetes and obesity. In this study, we designed, synthesised, and evaluated flavonoid-based compounds as new inhibitors of IP6K2. Structure-activity relationship studies identified compound 20s as the most potent IP6K2 inhibitor with an IC50 value of 0.55 mu M, making it 5-fold more potent than quercetin, the reported flavonoid-based IP6K2 inhibitor. Compound 20s showed higher inhibitory potency against IP6K2 than IP6K1 and IP6K3. Compound 20s can be utilised as a hit compound for further structural modifications of IP6K2 inhibitors.-
dc.languageEnglish-
dc.publisherTAYLOR & FRANCIS LTD-
dc.titleSynthesis and biological evaluation of flavonoid-based IP6K2 inhibitors-
dc.typeArticle-
dc.identifier.wosid000963000700001-
dc.identifier.scopusid2-s2.0-85151663471-
dc.type.rimsART-
dc.citation.volume38-
dc.citation.issue1-
dc.citation.publicationnameJOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY-
dc.identifier.doi10.1080/14756366.2023.2193866-
dc.contributor.localauthorKim, Jaehoon-
dc.contributor.localauthorKim, Seyun-
dc.contributor.nonIdAuthorAhn, Myunghwan-
dc.contributor.nonIdAuthorChoi, Jiyeon-
dc.contributor.nonIdAuthorChoi, Jiahn-
dc.contributor.nonIdAuthorChoi, Doyoung-
dc.contributor.nonIdAuthorJeon, Hayoung-
dc.contributor.nonIdAuthorOh, Soowhan-
dc.contributor.nonIdAuthorLee, Kiho-
dc.contributor.nonIdAuthorJang, Jaebong-
dc.contributor.nonIdAuthorByun, Youngjoo-
dc.description.isOpenAccessN-
dc.type.journalArticleArticle-
dc.subject.keywordAuthorInositol polyphosphates-
dc.subject.keywordAuthorflavonoid-
dc.subject.keywordAuthorstructure-activity relationship-
dc.subject.keywordPlusINOSITOL HEXAKISPHOSPHATE KINASES-
dc.subject.keywordPlusDIPHOSPHOINOSITOL PENTAKISPHOSPHATE-
dc.subject.keywordPlusIDENTIFICATION-
dc.subject.keywordPlusPHOSPHORYLATION-
dc.subject.keywordPlusMETABOLISM-
dc.subject.keywordPlusTNP-
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