DC Field | Value | Language |
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dc.contributor.author | S K Jung | - |
dc.contributor.author | Y Ko | - |
dc.contributor.author | Keum Ran Yu | - |
dc.contributor.author | Ju Hee Kim | - |
dc.contributor.author | J Y Lee | - |
dc.contributor.author | C H Chae | - |
dc.contributor.author | S Ji | - |
dc.contributor.author | C H Kim | - |
dc.contributor.author | H K Lee | - |
dc.contributor.author | E B Choi | - |
dc.contributor.author | Bo Yeon Kim | - |
dc.contributor.author | R L Erikson | - |
dc.contributor.author | Sang Jeon Chung | - |
dc.contributor.author | Seung Jun Kim | - |
dc.date.accessioned | 2017-04-19T09:28:52Z | - |
dc.date.available | 2017-04-19T09:28:52Z | - |
dc.date.issued | 2012 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | 10.1016/j.bmcl.2012.01.011 | ko |
dc.identifier.uri | https://oak.kribb.re.kr/handle/201005/10607 | - |
dc.description.abstract | The 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.publisher | Elsevier | - |
dc.title | Identification 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.alternative | Identification of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4-one derivatives as inhibitors of the phosphatase SerB653 in Porphyromonas gingivalis, implicated in periodontitis | - |
dc.type | Article | - |
dc.citation.title | Bioorganic & Medicinal Chemistry Letters | - |
dc.citation.number | 5 | - |
dc.citation.endPage | 2088 | - |
dc.citation.startPage | 2084 | - |
dc.citation.volume | 22 | - |
dc.contributor.affiliatedAuthor | Keum Ran Yu | - |
dc.contributor.affiliatedAuthor | Ju Hee Kim | - |
dc.contributor.affiliatedAuthor | Bo Yeon Kim | - |
dc.contributor.affiliatedAuthor | Sang Jeon Chung | - |
dc.contributor.affiliatedAuthor | Seung Jun Kim | - |
dc.contributor.alternativeName | 정숙경 | - |
dc.contributor.alternativeName | 고영경 | - |
dc.contributor.alternativeName | 유금란 | - |
dc.contributor.alternativeName | 김주희 | - |
dc.contributor.alternativeName | 이주연 | - |
dc.contributor.alternativeName | 채종학 | - |
dc.contributor.alternativeName | 지숙 | - |
dc.contributor.alternativeName | 김창현 | - |
dc.contributor.alternativeName | 이현규 | - |
dc.contributor.alternativeName | 최은복 | - |
dc.contributor.alternativeName | 김보연 | - |
dc.contributor.alternativeName | Erikson | - |
dc.contributor.alternativeName | 정상전 | - |
dc.contributor.alternativeName | 김승준 | - |
dc.identifier.bibliographicCitation | Bioorganic & Medicinal Chemistry Letters, vol. 22, no. 5, pp. 2084-2088 | - |
dc.identifier.doi | 10.1016/j.bmcl.2012.01.011 | - |
dc.subject.keyword | Competitive inhibitor | - |
dc.subject.keyword | Gram-negative anaerobe | - |
dc.subject.keyword | Haloacid dehalogenase | - |
dc.subject.keyword | HTS | - |
dc.subject.keyword | Malachite green colorimetric method | - |
dc.subject.keyword | Periodontitis | - |
dc.subject.local | competitive inhibitor | - |
dc.subject.local | Competitive inhibitor | - |
dc.subject.local | Gram-negative anaerobe | - |
dc.subject.local | Halo-acid dehalogenase | - |
dc.subject.local | Haloacid dehalogenase | - |
dc.subject.local | HTS | - |
dc.subject.local | Malachite green colorimetric method | - |
dc.subject.local | Periodontitis | - |
dc.description.journalClass | Y | - |
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