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Antibacterial polypeptide EC1-17KV and use thereof

A technology for antibacterial polypeptides and uses, applied in the field of polypeptides and their uses, and drug-resistant bacterial infections, to achieve the effect of reducing synthesis costs

Active Publication Date: 2018-02-02
CHINA PHARM UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Antibiotics have always been the first choice for humans to fight bacterial infections, but the abuse of clinical antibiotics in recent decades has led to the emergence of drug-resistant bacteria worldwide

Method used

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  • Antibacterial polypeptide EC1-17KV and use thereof
  • Antibacterial polypeptide EC1-17KV and use thereof
  • Antibacterial polypeptide EC1-17KV and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] (1) Synthesis and purification of polypeptide EC1-17KV

[0057] The amino acid sequence of the prepared EC1-17KV is: glycine-tryptophan-tryptophan-arginine-arginine-threonine-valine-lysine-lysine-valine-arginine Acids – Asparagine-Alanine-Valine-Arginine-Lysine-Valine.

[0058] Polypeptide synthesis was carried out one by one from the C-terminus to the N-terminus by Fmoc solid-phase synthesis method: Weigh 0.6g of 2-Chlorotrityl Chloride Resin resin with a degree of substitution of 0.4mmol / g, put the resin into a reaction tube, add DCM (15ml / g), shake for 30 minutes; filter the solvent through a sand core, add 3-fold molar excess of amino acid, then add 10-fold molar excess of DIEA, finally add a small amount of DMF to dissolve, and shake for 1 hour. Alternately wash 6 times with DMF and DCM. Add 15ml of 20% piperidine DMF solution (15ml / g), react for 5min, remove it and add 15ml of 20% piperidine DMF solution (15ml / g), react for 15min. Take out the piperidine solut...

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Abstract

The invention belongs to the technical field of polypeptide drugs in biochemistry, and concretely relates to a polypeptide. The amino acid sequence of the polypeptide is represented by SEQ ID NO:1, the polypeptide is a cationic polypeptide having a high inhibitory activity to drug-resistant bacteria, and the polypeptide is obtained through a solid phase synthesis method by intercepting the former17 amino acids of a parent structure EeCentrocins 1 heavy chain, mutating aspartic acid in the eighth position into lysine and mutating glycine in the fourteenth position into valine. Pharmacodynamictest proves that the polypeptide has a use in inhibition of bacterium and especially drug-resistant bacterium infection.

Description

technical field [0001] The invention belongs to the technical field of polypeptide drugs in biochemistry, and specifically relates to a polypeptide and its application, that is, the polypeptide of the invention has the application of antibacterial, especially drug-resistant bacterial infection. Background technique [0002] Antibiotics have always been the first choice for humans to fight bacterial infections, but the abuse of clinical antibiotics in recent decades has led to the emergence of drug-resistant bacteria worldwide. About 20 million people die from drug-resistant bacterial infections every year in the world, and the number of infections and deaths is still increasing year by year. [0003] Cationic antimicrobial peptides are biologically active macromolecules that evolve naturally in nature and have anti-pathogenic microbial infections, and exist in the immune system of different species. Naturally occurring cationic antimicrobial peptides are usually between 10 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/435A61K38/17A61P31/04A61P29/00A61P9/00A61P1/16
CPCA61K38/00C07K14/43504Y02A50/30
Inventor 马菱蔓周丽孙鹏博史翔宇林健安胜祥窦洁周长林
Owner CHINA PHARM UNIV
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