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Polypeptide with potential analgesic activity and synthetic method thereof

A synthetic method and potential technology, applied in the field of biomedicine, can solve the problems of low final yield and cumbersome synthetic experimental steps, and achieve the effects of increased final yield, simple purification, and reduced burden

Pending Publication Date: 2017-08-15
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to achieve the above purpose, the present invention provides a polypeptide with potential analgesic properties, which is obtained by transforming α-conotoxin Vc1.1, and the synthesis process is simple, which solves the synthetic experimental steps of α-conotoxin Vc1.1 in the prior art cumbersome and low final yield

Method used

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  • Polypeptide with potential analgesic activity and synthetic method thereof
  • Polypeptide with potential analgesic activity and synthetic method thereof
  • Polypeptide with potential analgesic activity and synthetic method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] The method for synthesizing potential analgesic peptides is carried out according to the following steps:

[0023] Step 1. In the homology modeling process, it is necessary to provide the sequence alignment of the target protein and the template protein and the three-dimensional structure of the template protein, and then use the Modeller software to directly generate the three-dimensional structure of the target protein; the wild-type α-conotoxin Vc1. 1. Delete a pair of disulfide bonds at positions 2 and 8 of the peptide chain, and introduce histidine and phenylalanine at positions 2 and 8 of the peptide chain respectively. Choose wild-type α-conotoxin Vc1.1 as the template, and use Modeller The software, in the LINUX system environment, uses the homology modeling method to generate 100 three-dimensional structure models of the target protein using Modeller 9.14, and uses the Dope score to rank the obtained three-dimensional structure models, and select the best three-dim...

Embodiment 2

[0027] The method of synthesizing potential analgesic peptides is specifically carried out according to the following steps:

[0028] Step 1 is the same as embodiment 1;

[0029] Step 2. Use Fmoc solid-phase synthesis method to chemically synthesize the polypeptide sequence of the optimal target protein. Use 2-CTC resin. After the resin is activated, the polypeptide chain is synthesized on the resin, using 15% piperidine / The DMF solution is used to deprotect the amino acid nitrogen terminal Fmoc, and HCTU and DIPEA are used to carry out the coupling reaction between the amino acids; after the coupling is completed, the dilute solution of TFA is used as the cutting agent to cut the polypeptide chain from the resin to obtain potential Analgesic peptides. The invention adopts the Fmoc solid-phase synthesis method, because of its mild reaction conditions and few by-products, and at the same time avoids using HF as a cutting agent for polypeptides from resin.

[0030] Step 3. Cyclizati...

Embodiment 3

[0032] The method of synthesizing potential analgesic peptides is specifically carried out according to the following steps:

[0033] Step 1 is the same as embodiment 1;

[0034] Step 2. Use Fmoc solid-phase synthesis method to chemically synthesize the peptide sequence of the optimal target protein. Use 2-CTC resin. After the resin is activated, the peptide chain is synthesized on the resin, using 25% piperidine / The DMF solution is used to deprotect the amino acid nitrogen terminal Fmoc, and HCTU and DIPEA are used to carry out the coupling reaction between the amino acids; after the coupling is completed, the dilute solution of TFA is used as the cutting agent to cut the polypeptide chain from the resin to obtain potential Analgesic peptides. The invention adopts the Fmoc solid-phase synthesis method, because of its mild reaction conditions and few by-products, while avoiding the use of HF as a cutting agent for polypeptides from resin.

[0035] Step 3. Cyclization to obtain a c...

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Abstract

The invention discloses a polypeptide with potential analgesic activity and a synthetic method thereof and belongs to the technical field of biological medicines. The amino acid sequence of the polypeptide with potential analgesic activity is GHCSDPRFNYDHPEICGGAAGG. The polypeptide with potential analgesic activity, disclosed by the invention, is obtained by transforming alpha-conotoxin Vc1.1. The synthetic process is simple, and the problem that in the prior at, a synthetic experiment of the alpha-conotoxin Vc1.1 is tedious in step and low in final yield is solved.

Description

Technical field [0001] The invention belongs to the technical field of biomedicine, and relates to a polypeptide with potential analgesic properties and a synthesis method thereof, in particular to a marine polypeptide α-conotoxin analogue with a novel skeleton and a stable structure and a synthesis method thereof. Background technique [0002] Conotoxin (conotoxin or conopeptide, or CTX) is secreted by the venom tube of the marine gastropod mollusk Conus and the venom glands on the inner wall of the venom sac. It is a cocktail-like mixed toxin composed of many single venom peptides, mainly The ingredients are active peptide compounds that are highly specific to different ion channels and neuroreceptors. The venom of each Cono snail may contain 50 to 200 active polypeptides. Different species of Cono contain different active peptides. Even if the same species of Conus contains different sea areas, the toxin composition may be different. It is theoretically estimated that more th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/435C07K1/06C07K1/04
CPCC07K14/43504
Inventor 于日磊戴维克雷克赵阳陈芳玲江涛
Owner OCEAN UNIV OF CHINA
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