Identification and Validation of a Selective Small Molecule Inhibitor Targeting the Diacylglycerol Acyltransferase 2 Activity
DC Field | Value | Language |
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dc.contributor.author | Kim, Mun Ock | - |
dc.contributor.author | Lee, Su Ui | - |
dc.contributor.author | Lee, Hyun-Jun | - |
dc.contributor.author | Choi, Kwangman | - |
dc.contributor.author | Kim, Hyeongki | - |
dc.contributor.author | Lee, Sangku | - |
dc.contributor.author | Oh, Soo Jin | - |
dc.contributor.author | Kim, Sunhong | - |
dc.contributor.author | Kang, Jong Soon | - |
dc.contributor.author | Lee, Hyun Sun | - |
dc.contributor.author | Kwak, Young-Shin | - |
dc.contributor.author | Cho, Sungchan | - |
dc.date.accessioned | 2021-09-06T00:00:31Z | - |
dc.date.available | 2021-09-06T00:00:31Z | - |
dc.date.created | 2021-06-14 | - |
dc.date.issued | 2013-07 | - |
dc.identifier.issn | 0918-6158 | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/102758 | - |
dc.description.abstract | Diacylglycerol acyltransferase 2 (DGAT2) is one of two distinct DGAT enzymes that catalyze the last step in triacylglycerol (TG) synthesis. Findings from previous studies suggest that inhibition of DGAT2 is a promising strategy for the treatment of hepatic steatosis and insulin resistance. Here, we identified compound 122 as a potent and selective inhibitor of human DGAT2, which appeared to act competitively against oleoyl-CoA in vitro. The selective inhibition of DGAT2 was also confirmed by the reductions in enzymatic activity and de novo TG synthesis in DGAT2-overexpressing HEK293 cells and hepatic cells HepG2. Compound 122, as a newly identified inhibitor of DGAT2, will be useful for the research on DGAT2-related lipid metabolism as well as the development of therapeutic drug for several metabolic diseases. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | PHARMACEUTICAL SOC JAPAN | - |
dc.subject | INSULIN-RESISTANCE | - |
dc.subject | TRIGLYCERIDE SYNTHESIS | - |
dc.subject | HEPATIC STEATOSIS | - |
dc.subject | MICE | - |
dc.subject | DGAT1 | - |
dc.subject | OVEREXPRESSION | - |
dc.subject | ENZYMES | - |
dc.title | Identification and Validation of a Selective Small Molecule Inhibitor Targeting the Diacylglycerol Acyltransferase 2 Activity | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Kwak, Young-Shin | - |
dc.identifier.doi | 10.1248/bpb.b13-00152 | - |
dc.identifier.scopusid | 2-s2.0-84880426625 | - |
dc.identifier.wosid | 000321176400016 | - |
dc.identifier.bibliographicCitation | BIOLOGICAL & PHARMACEUTICAL BULLETIN, v.36, no.7, pp.1167 - 1173 | - |
dc.relation.isPartOf | BIOLOGICAL & PHARMACEUTICAL BULLETIN | - |
dc.citation.title | BIOLOGICAL & PHARMACEUTICAL BULLETIN | - |
dc.citation.volume | 36 | - |
dc.citation.number | 7 | - |
dc.citation.startPage | 1167 | - |
dc.citation.endPage | 1173 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Pharmacology & Pharmacy | - |
dc.subject.keywordPlus | INSULIN-RESISTANCE | - |
dc.subject.keywordPlus | TRIGLYCERIDE SYNTHESIS | - |
dc.subject.keywordPlus | HEPATIC STEATOSIS | - |
dc.subject.keywordPlus | MICE | - |
dc.subject.keywordPlus | DGAT1 | - |
dc.subject.keywordPlus | OVEREXPRESSION | - |
dc.subject.keywordPlus | ENZYMES | - |
dc.subject.keywordAuthor | metabolic disease | - |
dc.subject.keywordAuthor | triacylglycerol | - |
dc.subject.keywordAuthor | diacylglycerol acyltransferase 2 | - |
dc.subject.keywordAuthor | small molecule inhibitor | - |
dc.subject.keywordAuthor | isatin | - |
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