Target gene Rv0233 screened by antituberculous inhibitor and application

A technology of rv0233 and inhibitor, which is applied in the field of drug molecules to achieve the effect of high hit rate, small workload and less resistance to drug resistance
CN103123672AInactive Publication Date: 2013-05-29HUAZHONG AGRI UNIV

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
HUAZHONG AGRI UNIV
Publication Date
2013-05-29
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention belongs to the technical field of drug molecules and particularly relates to an application of mycobacterium tuberculosis gene Rv0233 in screening an antituberculous inhibitor target. The gene is characterized in that a nucleotide sequence of the gene is as shown in a sequence table: sequencer (SEQ) ID NO: 1, and a coded protein sequence of the gene is as shown in the sequence table: sequencer (SEQ) ID NO: 2. Eighteen small molecule compounds which have a high affinity with a binding site of natural substrate of Rv0233 screened out from a small molecular compound database through a molecular docking program aiming at an active centre of the natural substrate of the Rv0233 by the way of virtual screening. One bacteriostatic compound (pyrazole compound 51#) is obtained. The name of the compound is 2-({[1-(4-methyl pheny)-H-pyrazol-4-y1] methyl} amino) ethanol. The target gene evaluates the bacteriostatic effect of the compound on the mycobacterium tuberculosis.
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Description

technical field

[0001] The invention belongs to the technical field of drug molecules, and in particular relates to the application of a Mycobacterium tuberculosis gene Rv0233 in screening targets of anti-tuberculosis inhibitors. Background technique

[0002] Mycobacterium tuberculosis is a pathogen that seriously endangers human health. According to the statistics of the World Health Organization, about three million people die of tuberculosis every year in the world, and about one-third of the world's population is infected with latent tuberculosis. Mycobacteria (WHO, 2009). Currently, TB chemotherapy consists of a mixture of first-line and second-line drugs. Actual TB treatment takes 6 to 9 months, leading to severe toxicity and drug resistance. Drug-resistant Mycobacterium tuberculosis strains have been emerging since the introduction of anti-tuberculosis drugs. In fact, mycobacteria are naturally resistant to most commonly used antibiotics due to their unusual cell w...

Claims

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