Identification of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4-one derivatives as inhibitors of the phosphatase SerB653 in Porphyromonas gingivalis, implicated in periodontitis

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dc.contributor.authorS K Jung-
dc.contributor.authorY Ko-
dc.contributor.authorKeum Ran Yu-
dc.contributor.authorJu Hee Kim-
dc.contributor.authorJ Y Lee-
dc.contributor.authorC H Chae-
dc.contributor.authorS Ji-
dc.contributor.authorC H Kim-
dc.contributor.authorH K Lee-
dc.contributor.authorE B Choi-
dc.contributor.authorBo Yeon Kim-
dc.contributor.authorR L Erikson-
dc.contributor.authorSang Jeon Chung-
dc.contributor.authorSeung Jun Kim-
dc.date.accessioned2017-04-19T09:28:52Z-
dc.date.available2017-04-19T09:28:52Z-
dc.date.issued2012-
dc.identifier.issn0960-894X-
dc.identifier.uri10.1016/j.bmcl.2012.01.011ko
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/10607-
dc.description.abstractThe serine phosphatase SerB653 plays a crucial role in the infection of Porphyromonas gingivalis, which contributes to the pathogenesis of periodontitis, an inflammatory disease of teeth-supporting tissues. Because functional loss of SerB653 eliminates the virulence of P. gingivalis, SerB653 inhibitors are considered potential periodontitis therapeutic or preventive agents. To identify SerB653 inhibitors with potent anti-periodontitis activity, we conducted a high-throughput screen of a representative 6800-compound subset of a synthetic chemical library of the Korea Chemical Bank (KCB) for compounds with activity against SerB653. The primary screening yielded 150 hits, and subsequent confirmatory studies identified eight compounds, mainly within a single cluster of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4-one derivatives, that showed greater than 50% inhibition of SerB653 activity at a concentration of 50 μM. A second screening with a focused library identified 10 compounds with IC 50 values less than 10 μM. In antibacterial tests, three of these compounds showed a minimum inhibitory concentration against P. gingivalis growth of 5-50 nM.-
dc.publisherElsevier-
dc.titleIdentification of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4-one derivatives as inhibitors of the phosphatase SerB653 in Porphyromonas gingivalis, implicated in periodontitis-
dc.title.alternativeIdentification of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4-one derivatives as inhibitors of the phosphatase SerB653 in Porphyromonas gingivalis, implicated in periodontitis-
dc.typeArticle-
dc.citation.titleBioorganic & Medicinal Chemistry Letters-
dc.citation.number5-
dc.citation.endPage2088-
dc.citation.startPage2084-
dc.citation.volume22-
dc.contributor.affiliatedAuthorKeum Ran Yu-
dc.contributor.affiliatedAuthorJu Hee Kim-
dc.contributor.affiliatedAuthorBo Yeon Kim-
dc.contributor.affiliatedAuthorSang Jeon Chung-
dc.contributor.affiliatedAuthorSeung Jun Kim-
dc.contributor.alternativeName정숙경-
dc.contributor.alternativeName고영경-
dc.contributor.alternativeName유금란-
dc.contributor.alternativeName김주희-
dc.contributor.alternativeName이주연-
dc.contributor.alternativeName채종학-
dc.contributor.alternativeName지숙-
dc.contributor.alternativeName김창현-
dc.contributor.alternativeName이현규-
dc.contributor.alternativeName최은복-
dc.contributor.alternativeName김보연-
dc.contributor.alternativeNameErikson-
dc.contributor.alternativeName정상전-
dc.contributor.alternativeName김승준-
dc.identifier.bibliographicCitationBioorganic & Medicinal Chemistry Letters, vol. 22, no. 5, pp. 2084-2088-
dc.identifier.doi10.1016/j.bmcl.2012.01.011-
dc.subject.keywordCompetitive inhibitor-
dc.subject.keywordGram-negative anaerobe-
dc.subject.keywordHaloacid dehalogenase-
dc.subject.keywordHTS-
dc.subject.keywordMalachite green colorimetric method-
dc.subject.keywordPeriodontitis-
dc.subject.localcompetitive inhibitor-
dc.subject.localCompetitive inhibitor-
dc.subject.localGram-negative anaerobe-
dc.subject.localHalo-acid dehalogenase-
dc.subject.localHaloacid dehalogenase-
dc.subject.localHTS-
dc.subject.localMalachite green colorimetric method-
dc.subject.localPeriodontitis-
dc.description.journalClassY-
Appears in Collections:
Ochang Branch Institute > Chemical Biology Research Center > 1. Journal Articles
Critical Diseases Diagnostics Convergence Research Center > 1. Journal Articles
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