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Medicine binding pocket of DNA (deoxyribonucleic acid) gyrase and application thereof

A technology of gyrase and drugs, applied in the field of biomedicine, to achieve the effect of avoiding drug resistance problems

Active Publication Date: 2018-09-07
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This allows the mutant strain to also become resistant to other existing GyrB inhibitors

Method used

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  • Medicine binding pocket of DNA (deoxyribonucleic acid) gyrase and application thereof
  • Medicine binding pocket of DNA (deoxyribonucleic acid) gyrase and application thereof
  • Medicine binding pocket of DNA (deoxyribonucleic acid) gyrase and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0057] 1. Construction of the prokaryotic expression plasmid of the E. coli DNA gyrase GyrB subunit ATPase domain

[0058] Insert the DNA coding sequence of the ATPase domain (amino acid sequence 15-220) of the Escherichia coli DNA gyrase GyrB subunit (UniProKB numbering P0AES6) into the pET20b (+) vector, and insert six sets of upstream of the DNA coding sequence Amino acid tag and yeast sumo protein tag DNA sequence, constructed to express His 6 -Prokaryotic expression plasmid of sumo-GyrB fusion protein. The inserted DNA sequence was verified by sequencing.

[0059] The amino acid sequence of the Escherichia coli DNA gyrase GyrB subunit ATPase domain (amino acid sequence 15-220) is:

[0060] GGLDAVRKRPGMYIGDTDDGTGLHHMVFEVVDNAIDEALAGHCKEIIVTIHADNSVSVQDDGRGIPTGIHPEEGVSAAEVIMTVLHAGGKFDDNSYKVSGGLHGVGVSVVNALSQKLELVIQREGKIHRQIYEHGVPQAPLAVTGETEKTGTMRFWPSLETFTNVTEFEYEILAKRLRELSRDFLNSGKVSIRL

[0061] The DNA sequence encoding the Escherichia coli DNA gyrase GyrB subunit ATPase do...

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Abstract

The invention discloses a medicine binding pocket of DNA (deoxyribonucleic acid) gyrase. The medicine binding pocket is characterized in that an ATP (adenosine triphosphate) enzyme structure domain ofa B subunit of the DNA gyrase is used as a study object, a compound segment is used as a probe, and the protein heat stability transfer experiment, an ATP enzyme hydrolysis activity experiment and anX-ray crystallography diffraction method are performed, so as to find that a novel medical ligand binding pocket exists on the B subunit of the DNA gyrase of the bacteria; the medicine binding pocketis induced by the screened segment probe 4-phenoxyphenol or 4,4'-dyhydroxy diphenyl sulfide. The novel ligand binding pocket has the advantages that an inhibitor for the DNA gyrase with a novel binding mode is designed and screened; the screened compound segment provides basis elements for the segment growth, integration and connection for the design of novel antibacterial medicines; by using thenovel medical pocket as a starting point, the screened segment is spliced with the existing inhibitor to obtain the inhibitor for the DNA gyrase with high affinity and high selectivity, and the problem of medicine resistance property of the existing inhibitor is expected to be solved.

Description

technical field [0001] The invention relates to the field of biomedical technology, in particular to a drug-binding pocket of DNA gyrase and its application. Background technique [0002] Since Fleming discovered penicillin in 1928, antibiotics have become a powerful tool in the clinical fight against infectious diseases, greatly reducing the fatality rate of bacterial infectious diseases. However, the long-term overreliance and abuse of antibacterial drugs by humans has led to the gradual emergence of bacterial resistance to existing antibacterial drugs. In recent years, the problem of bacterial drug resistance has become more and more serious, which has brought severe challenges to clinical anti-infective treatment, and human beings may once again enter the "post-antibiotic era" where no drugs are available. In order to meet this challenge, in addition to strengthening the control of the use of existing antibacterial drugs, it is also necessary to accelerate the developme...

Claims

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Application Information

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IPC IPC(8): C12N9/90
CPCC12N9/90
Inventor 周晖皓黄晓杰郭俊松顾琼徐峻
Owner SUN YAT SEN UNIV
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