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dc.contributor.author윤문영-
dc.date.accessioned2018-04-14T11:13:25Z-
dc.date.available2018-04-14T11:13:25Z-
dc.date.issued2011-01-
dc.identifier.citationBiochemical and Biophysical Research Communications, 2011, 404(1), P.517-522en_US
dc.identifier.issn0006-291X-
dc.identifier.issn1090-2104-
dc.identifier.urihttps://www.sciencedirect.com/science/article/pii/S0006291X10022400?via%3Dihub-
dc.description.abstractInhibitors of anthrax lethal factor (LF) are currently being sought as effective therapeutics for the treatment of anthrax. Here we report a novel screening approach for inhibitors of LF, a yeast-hybrid-based assay system in which the expression of reporter genes from a Gal4 promoter is repressed by LF proteolytic activity. Yeast cells were co-transformed with LF and a chimeric transcription factor that contains an LF substrate sequence inserted between the DNA-binding and activation domains of Gal4. In the resulting yeast cells, LF cleaves the substrate, thus inactivating the chimeric Gal4 and resulting in lack of expression of reporter genes. Compounds that inhibit LF cleavage of its substrate are identified by changes in reporter gene activity. Relative to in vitro screens for inhibitors of LF proteolytic activity, this screen has the advantage of excluding compounds that are toxic or non-permeable to eukaryotic cells. Additionally, the screen has the advantage of being fast, easy and cheap because exogenous LF and substrate are not needed. An initial chemical library screen with this system has identified four candidate inhibitors which were confirmed to inhibit LF protease activity in an in vitro assay. Furthermore, FBS-00831, one of the compounds identified, protects Raw 264.7 macrophages from anthrax lethal toxin and the possible binding site on LF was also evaluated by molecular docking.en_US
dc.description.sponsorshipThis work was supported in part by a BioGreen 21 Program Grant #20080401034006 from the Rural Development Administration, Republic of Korea.en_US
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.subjectAnthrax lethal factoren_US
dc.subjectCell-based high-throughput assayen_US
dc.subjectChemical library screeningen_US
dc.subjectYeasten_US
dc.titleYeast-hybrid based high-throughput assay for identification of anthrax lethal factor inhibitorsen_US
dc.typeArticleen_US
dc.relation.no1-
dc.relation.volume404-
dc.identifier.doi10.1016/j.bbrc.2010.12.015-
dc.relation.page517-522-
dc.relation.journalBIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS-
dc.contributor.googleauthorKim, Joungmok-
dc.contributor.googleauthorPark, Hae-Chul-
dc.contributor.googleauthorGedi, Vinayakumar-
dc.contributor.googleauthorPark, Hye-Yeon-
dc.contributor.googleauthorRoberts, Arthur G-
dc.contributor.googleauthorAtkins, William M-
dc.contributor.googleauthorYoon, Moon-Young-
dc.relation.code2011201235-
dc.sector.campusS-
dc.sector.daehakCOLLEGE OF NATURAL SCIENCES[S]-
dc.sector.departmentDEPARTMENT OF CHEMISTRY-
dc.identifier.pidmyyoon-
dc.identifier.researcherIDA-3209-2014-
dc.identifier.orcidhttp://orcid.org/0000-0002-7042-0321-
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COLLEGE OF NATURAL SCIENCES[S](자연과학대학) > CHEMISTRY(화학과) > Articles
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