Please use this identifier to cite or link to this item:
http://hdl.handle.net/10397/89325
DC Field | Value | Language |
---|---|---|
dc.contributor | Department of Applied Biology and Chemical Technology | en_US |
dc.creator | Ye, J | en_US |
dc.creator | Chu, AJ | en_US |
dc.creator | Lin, L | en_US |
dc.creator | Chan, ST | en_US |
dc.creator | Harper, R | en_US |
dc.creator | Xiao, M | en_US |
dc.creator | Artsimovitch, I | en_US |
dc.creator | Zuo, Z | en_US |
dc.creator | Ma, C | en_US |
dc.creator | Yang, X | en_US |
dc.date.accessioned | 2021-03-12T09:35:58Z | - |
dc.date.available | 2021-03-12T09:35:58Z | - |
dc.identifier.issn | 0223-5234 | en_US |
dc.identifier.uri | http://hdl.handle.net/10397/89325 | - |
dc.language.iso | en | en_US |
dc.publisher | Elsevier Masson | en_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.rights | The 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.subject | Antimicrobial | en_US |
dc.subject | Bacterial transcription | en_US |
dc.subject | Inhibitor | en_US |
dc.subject | RNA polymerase | en_US |
dc.subject | Sigma factor | en_US |
dc.title | Benzyl and benzoyl benzoic acid inhibitors of bacterial RNA polymerase-sigma factor interaction | en_US |
dc.type | Journal/Magazine Article | en_US |
dc.identifier.volume | 208 | en_US |
dc.identifier.doi | 10.1016/j.ejmech.2020.112671 | en_US |
dcterms.abstract | Transcription 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.accessRights | open access | en_US |
dcterms.bibliographicCitation | European journal of medicinal chemistry, 15 Dec. 2020, v. 208, 112671 | en_US |
dcterms.isPartOf | European journal of medicinal chemistry | en_US |
dcterms.issued | 2020-12-15 | - |
dc.identifier.scopus | 2-s2.0-85090423780 | - |
dc.identifier.eissn | 1768-3254 | en_US |
dc.identifier.artn | 112671 | en_US |
dc.description.validate | 202103 bcvc | en_US |
dc.description.oa | Accepted Manuscript | en_US |
dc.identifier.FolderNumber | a0615-n01 | - |
dc.identifier.SubFormID | 600 | - |
dc.description.fundingSource | RGC | en_US |
dc.description.fundingSource | Others | en_US |
dc.description.fundingText | RGC: 25100017, 15100019, C5008-19G||Others: P0009742, P0030472, P000016 | en_US |
dc.description.pubStatus | Published | en_US |
Appears in Collections: | Journal/Magazine Article |
Files in This Item:
File | Description | Size | Format | |
---|---|---|---|---|
Ye_Benzyl_Benzoyl_Benzoic.pdf | Pre-Published version | 2.02 MB | Adobe PDF | View/Open |
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