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http://hdl.handle.net/10397/89971
Title: | Simple method for studying in vitro protein-protein interactions based on protein complementation and its application in drug screening targeting bacterial transcription | Authors: | Tsang, TF Qiu, Y Lin, L Ye, J Ma, C Yang, X |
Issue Date: | 12-Apr-2019 | Source: | ACS infectious diseases, 12 Apr. 2019, v. 5, no. 4, p. 521-527 | Abstract: | Protein-protein interactions (PPIs) underpin essential cellular processes of all organisms and are increasingly considered as drug targets. A number of techniques have been established to study PPIs; however, development of a simple and cost-effective method for in vitro high throughput screening of PPI inhibitors is still in demand or desirable. We report herein a simple method based on protein complementation for the in vitro study of PPIs, as well as screening of inhibitors against the PPI of interest. We have validated this system utilizing bacterial transcription factors NusB and NusE. Three derivatives of an inhibitor targeting the NusB-NusE interaction were synthesized and characterized with the system, which showed specific inhibition and antimicrobial activities. We have further confirmed the system with the RNA polymeraseâ'σ interaction and an inhibitor. This system is expected to be suitable for more extensive high throughput screening of large chemical libraries. Additionally, our vector system can be easily adapted to study other PPI pairs, followed by inhibitor screening for hit identification in the application of early stage drug discovery. | Keywords: | Antimicrobial agent Bacterial transcription In vitro drug screening Protein complementation assay Protein-protein interactions |
Publisher: | American Chemical Society | Journal: | ACS infectious diseases | EISSN: | 2373-8227 | DOI: | 10.1021/acsinfecdis.9b00020 | Rights: | © 2019 American Chemical Society This document is the Accepted Manuscript version of a Published Work that appeared in final form in ACS Infectious Diseases, 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/acsinfecdis.9b00020. |
Appears in Collections: | Journal/Magazine Article |
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a0734-n02_1301.pdf | Pre-Published version | 2.12 MB | Adobe PDF | View/Open |
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