Please use this identifier to cite or link to this item: http://hdl.handle.net/10397/75859
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dc.contributorDepartment of Applied Biology and Chemical Technology-
dc.contributorChinese Mainland Affairs Office-
dc.creatorYang, X-
dc.creatorLuo, MJ-
dc.creatorYeung, ACM-
dc.creatorLewis, PJ-
dc.creatorChan, PKS-
dc.creatorIp, M-
dc.creatorMa, C-
dc.date.accessioned2018-05-10T02:54:47Z-
dc.date.available2018-05-10T02:54:47Z-
dc.identifier.issn0006-2960-
dc.identifier.urihttp://hdl.handle.net/10397/75859-
dc.language.isoenen_US
dc.publisherAmerican Chemical Societyen_US
dc.rights© 2017 American Chemical Societyen_US
dc.rightsThis document is the Accepted Manuscript version of a Published Work that appeared in final form in Biochemistry, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see https://doi.org/10.1021/acs.biochem.7b00349.en_US
dc.titleFirst-in-class inhibitor of ribosomal RNA synthesis with antimicrobial activity against staphylococcus aureusen_US
dc.typeJournal/Magazine Articleen_US
dc.identifier.spage5049-
dc.identifier.epage5052-
dc.identifier.volume56-
dc.identifier.issue38-
dc.identifier.doi10.1021/acs.biochem.7b00349-
dcterms.abstractWe report the discovery of the first bacterial ribosomal RNA (rRNA) synthesis inhibitor that has specific antimicrobial activity against methicillin-resistant Staphylococcus aureus (MRSA). A pharmacophore model was constructed on the basis of the proteinprotein interaction between essential bacterial rlINA transcription factors NusB and NusE and employed for an in silico screen to identify potential leads. One compound, (E)-2-{[(3-ethynylphenyl)imino]methyl}-4-nitrophenol (MC4); demonstrated antimicrobial activity against a panel of S. aureus strains, including MRSA, without significant toxicity to mammalian cells. MC4 resulted in a decrease in the rRNA level in bacteria, and the target specificity of MC4 was confirmed at the molecular level. Results obtained from this work validated the bacterial rRNA transcription machinery as a novel antimicrobial target. This approach may be extended to other factors in rRNA transcription,.. and MC4 could be applied as a chemical probe to dissect the relationship among MRSA infection, MRSA, growth rate, and rRNA synthesis, in addition to its therapeutic potential.-
dcterms.accessRightsopen access-
dcterms.bibliographicCitationBiochemistry, 26 Sept. 2017, v. 56, no. 38, p. 5049-5052-
dcterms.isPartOfBiochemistry-
dcterms.issued2017-09-26-
dc.identifier.isiWOS:000411918000004-
dc.identifier.scopus2-s2.0-85029955336-
dc.identifier.pmid28782938-
dc.identifier.rosgroupid2017000178-
dc.description.ros2017-2018 > Academic research: refereed > Publication in refereed journal-
dc.description.validate201805 bcrc-
dc.description.oaAccepted Manuscript-
dc.identifier.FolderNumbera0734-n01-
dc.identifier.SubFormID1300-
dc.description.fundingSourceOthers-
dc.description.fundingTextP0001178, P0020297-
dc.description.pubStatusPublished-
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