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A kind of inhibitor of bacterial type I topoisomerase and its application

A technology of topoisomerase and inhibitor, which is applied in the field of molecular biology and can solve problems such as poor selectivity and toxic side effects

Active Publication Date: 2019-10-29
CF PHARMTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although small-molecule inhibitors targeting bTopo I have been studied and applied, most small-molecule chemical drugs have poor selectivity and tend to act on topoisomeras I in mammals, causing toxic side effects

Method used

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  • A kind of inhibitor of bacterial type I topoisomerase and its application
  • A kind of inhibitor of bacterial type I topoisomerase and its application
  • A kind of inhibitor of bacterial type I topoisomerase and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 verifies the inhibitory effect of 3-mis on bTopo I and draws IC 50

[0030] Experimental Materials

[0031] E.coli Toposomerase I (purchased from NEB, product number #M0301S), pUC 19 (purchased from NEB, product number #N3041S), Mismatch single strand (see Table 1 for the sequence, synthesized by Shanghai Jierui Company), agarose, TAE buffer, horizontal electrophoresis tank, pipette gun, dry thermostat, microcentrifuge, Bio-Rad gel imager, 1M sodium chloride solution, loadingdying, 50mM KAc, 20mM Tris-Ac, 10mM Mg(Ac) 2 , 100μg / ml BSA (pH 7.9@25℃) EB staining solution, etc.

[0032] Experimental procedure

[0033] (1) Preparation of Mismatch DNA

[0034] The single-stranded sequence (Table 1) was synthesized with the assistance of Shanghai Jierui Company. The single-stranded DNA provided by the company was diluted at 2OD to 25 μl and the final configuration was 100 μM. The corresponding 3-mis two single-stranded DNAs in the table were diluted 50 times and a...

Embodiment 2

[0040] Example 2 verifies the inhibitory effect of 5-mis on bTopo I and draws IC 50

[0041] Experimental Materials

[0042] E.coli Toposomerase I (purchased from NEB, product number #M0301S), pUC 19 (purchased from NEB, product number #N3041S), Mismatch single strand (see Table 1 for the sequence, synthesized by Shanghai Jierui Company), agarose, TAE buffer, horizontal electrophoresis tank, pipette gun, dry thermostat, microcentrifuge, Bio-Rad gel imager, 1M sodium chloride solution, loadingdying, 50mM KAc, 20mM Tris-Ac, 10mM Mg(Ac) 2 , 100μg / ml BSA (pH 7.9@25℃) EB staining solution, etc.

[0043] Experimental procedure

[0044] (1) Preparation of Mismatch DNA

[0045]The single-stranded sequence (Table 1) was synthesized with the assistance of Shanghai Jierui Company. The single-stranded DNA provided by the company was diluted at 2OD to 25 μl and the final configuration was 100 μM. The corresponding 5-mis two single-stranded DNAs in the table were diluted 50 times and ad...

Embodiment 3

[0051] Example 3 verifies the inhibitory effect of 7-mis on bTopo I and draws IC 50

[0052] Experimental Materials

[0053] E.coli Toposomerase I (purchased from NEB, product number #M0301S), pUC 19 (purchased from NEB, product number #N3041S), Mismatch single strand (see Table 1 for the sequence, synthesized by Shanghai Jierui Company), agarose, TAE buffer, horizontal electrophoresis tank, pipette gun, dry thermostat, microcentrifuge, Bio-Rad gel imager, 1M sodium chloride solution, loadingdying, 50mM KAc, 20mM Tris-Ac, 10mM Mg(Ac) 2 , 100μg / ml BSA (pH 7.9@25℃) EB staining solution, etc.

[0054] Experimental procedure

[0055] (1) Preparation of Mismatch DNA

[0056] The single-stranded sequence (Table 1) was synthesized with the assistance of Shanghai Jierui Company. The single-stranded DNA provided by the company was diluted to 2OD to 25 μl and the final configuration was 100 μM. The corresponding 7-mis two single-stranded DNAs in the table were diluted 50 times and a...

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Abstract

The invention discloses an inhibitor of bTopo I (bacterial toposomerase I) and an application of the inhibitor and belongs to the field of molecular biology. According to the characteristic that bTopo I recognizes a reaction substrate, double-chain nucleotide adopting an unmatched basic group structure acts on bTopo I, and a targeted antibacterial effect is realized. Besides, due to the fact that bTopo I and topoisomerase I of mammal animals have different acting mechanisms, novel antibacterial molecules with the double-chain nucleotide adopting the unmatched basic group structure as a basis have an important function on interfering bacteria without influencing host cells and a theoretical basis and a novel development direction are provided for research of antibacterial medicines.

Description

technical field [0001] The invention relates to an inhibitor of bacterial type I topoisomerase and application thereof, belonging to the field of molecular biology. Background technique [0002] Bacterial Toposomerase I (bTopo I) is a key ribozyme present in prokaryotic bacteria, consisting of 590 amino acids, with a molecular weight of 67kD, and the N-terminus was found to have relaxing DNA negative supercoiling The key structure of bTopo I, by relaxing the negative supercoiled structure of bacterial DNA, changes the topology of bacterial DNA, maintains the normal replication and transcription of bacterial nucleic acid, and ensures the normal growth and reproduction of bacteria. [0003] At present, the research results on the function of nucleic acid show that, in addition to the function of encoding protein, nucleic acid also plays a key role in other life activities. Currently, there are various functional non-coding RNA molecules, non-coding DNA, RNA molecules that cau...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C12N15/113A23L3/3553A61K48/00A61K31/713A61P31/04
CPCA23L3/3553A23V2002/00A61K31/713C12N15/113A23V2200/10A61K2300/00
Inventor 杨兆琪姜拓昱仲晗实刘元法
Owner CF PHARMTECH