Materials and methods for identifying gyrase inhibitors

    公开(公告)号:US11613780B2

    公开(公告)日:2023-03-28

    申请号:US16009735

    申请日:2018-06-15

    摘要: The disclosure describes the effects of transcription mediated from a promoter on the transcription mediated by divergently coupled supercoiling-sensitive promoter. Transcription initiated from a promoter inhibits transcription mediated by a specific supercoiling-sensitive promoter that is divergently coupled to the promoter. A gyrase inhibitor relieves this inhibition and substantially increases the transcription mediated by the specific supercoiling-sensitive promoter that is divergently coupled to another promoter. Accordingly, the invention pertains to a method for identifying a compound as a gyrase inhibitor or not a gyrase inhibitor based on differential expression of genes under the control of divergently coupled promoters in the presence of the compound. Another embodiment of the invention provides an assay for identifying one or more compounds from a library of compounds as a gyrase inhibitor. Polynucleotides and cells containing such polynucleotides that are suitable for carrying out the methods described herein are also provided.

    T5 exonuclease-based method to identify DNA topoisomerase inhibitors

    公开(公告)号:US11286514B1

    公开(公告)日:2022-03-29

    申请号:US17072502

    申请日:2020-10-16

    IPC分类号: C12Q1/533 G01N21/64 C12Q1/44

    摘要: The present invention provides assays and methods for studying DNA topology and topoisomerases. The assays and methods utilize a circular plasmid DNA comprising one or more hairpin structures and the ability of T5 exonuclease (T5E) to digest the circular plasmid DNA in a specific configuration. The assays and methods can be used as a high throughput screening for inhibitors of, for example, DNA gyrases and DNA topoisomerases I for anticancer drug and antibiotics discovery.

    T5 exonuclease-based method to identify DNA topoisomerase inhibitors

    公开(公告)号:US11268129B1

    公开(公告)日:2022-03-08

    申请号:US17343918

    申请日:2021-06-10

    IPC分类号: C12Q1/533 G01N21/64 C12Q1/44

    摘要: The present invention provides assays and methods for studying DNA topology and topoisomerases. The assays and methods utilize a circular plasmid DNA comprising one or more hairpin structures and the ability of T5 exonuclease (T5E) to digest the circular plasmid DNA in a specific configuration. The assays and methods can be used as a high throughput screening for inhibitors of, for example, DNA gyrases and DNA topoisomerases I for anticancer drug and antibiotics discovery.

    T5 EXONUCLEASE-BASED METHOD TO IDENTIFY DNA TOPOISOMERASE INHIBITORS

    公开(公告)号:US20220119858A1

    公开(公告)日:2022-04-21

    申请号:US17072502

    申请日:2020-10-16

    IPC分类号: C12Q1/533 C12Q1/44 G01N21/64

    摘要: The present invention provides assays and methods for studying DNA topology and topoisomerases. The assays and methods utilize a circular plasmid DNA comprising one or more hairpin structures and the ability of T5 exonuclease (T5E) to digest the circular plasmid DNA in a specific configuration. The assays and methods can be used as a high throughput screening for inhibitors of, for example, DNA gyrases and DNA topoisomerases I for anticancer drug and antibiotics discovery.