Please use this identifier to cite or link to this item: http://hdl.handle.net/10397/89325
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dc.contributorDepartment of Applied Biology and Chemical Technologyen_US
dc.creatorYe, Jen_US
dc.creatorChu, AJen_US
dc.creatorLin, Len_US
dc.creatorChan, STen_US
dc.creatorHarper, Ren_US
dc.creatorXiao, Men_US
dc.creatorArtsimovitch, Ien_US
dc.creatorZuo, Zen_US
dc.creatorMa, Cen_US
dc.creatorYang, Xen_US
dc.date.accessioned2021-03-12T09:35:58Z-
dc.date.available2021-03-12T09:35:58Z-
dc.identifier.issn0223-5234en_US
dc.identifier.urihttp://hdl.handle.net/10397/89325-
dc.language.isoenen_US
dc.publisherElsevier Massonen_US
dc.rights© 2020 Elsevier Masson SAS. All rights reserved.en_US
dc.rights© 2020. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/.en_US
dc.rightsThe following publication Ye, J., Chu, A. J., Lin, L., Chan, S. T., Harper, R., Xiao, M., Artsimovitch, I., Zuo, Z., Ma, C., & Yang, X. (2020). Benzyl and benzoyl benzoic acid inhibitors of bacterial RNA polymerase-sigma factor interaction. European Journal of Medicinal Chemistry, 208, 112671 is available at https://dx.doi.org/10.1016/j.ejmech.2020.112671.en_US
dc.subjectAntimicrobialen_US
dc.subjectBacterial transcriptionen_US
dc.subjectInhibitoren_US
dc.subjectRNA polymeraseen_US
dc.subjectSigma factoren_US
dc.titleBenzyl and benzoyl benzoic acid inhibitors of bacterial RNA polymerase-sigma factor interactionen_US
dc.typeJournal/Magazine Articleen_US
dc.identifier.volume208en_US
dc.identifier.doi10.1016/j.ejmech.2020.112671en_US
dcterms.abstractTranscription is an essential biological process in bacteria requiring a core enzyme, RNA polymerase (RNAP). Bacterial RNAP is catalytically active but requires sigma (σ) factors for transcription of natural DNA templates. σ factor binds to RNAP to form a holoenzyme which specifically recognizes a promoter, melts the DNA duplex, and commences RNA synthesis. Inhibiting the binding of σ to RNAP is expected to inhibit bacterial transcription and growth. We previously identified a triaryl hit compound that mimics σ at its major binding site of RNAP, thereby inhibiting the RNAP holoenzyme formation. In this study, we modified this scaffold to provide a series of benzyl and benzoyl benzoic acid derivatives possessing improved antimicrobial activity. A representative compound demonstrated excellent activity against Staphylococcus epidermidis with minimum inhibitory concentrations reduced to 0.5 μg/mL, matching that of vancomycin. The molecular mechanism of inhibition was confirmed using biochemical and cellular assays. Low cytotoxicity and metabolic stability of compounds demonstrated the potential for further studies.en_US
dcterms.accessRightsopen accessen_US
dcterms.bibliographicCitationEuropean journal of medicinal chemistry, 15 Dec. 2020, v. 208, 112671en_US
dcterms.isPartOfEuropean journal of medicinal chemistryen_US
dcterms.issued2020-12-15-
dc.identifier.scopus2-s2.0-85090423780-
dc.identifier.eissn1768-3254en_US
dc.identifier.artn112671en_US
dc.description.validate202103 bcvcen_US
dc.description.oaAccepted Manuscripten_US
dc.identifier.FolderNumbera0615-n01-
dc.identifier.SubFormID600-
dc.description.fundingSourceRGCen_US
dc.description.fundingSourceOthersen_US
dc.description.fundingTextRGC: 25100017, 15100019, C5008-19G||Others: P0009742, P0030472, P000016en_US
dc.description.pubStatusPublisheden_US
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