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Method for quickly constructing trace peptide base and synthetizing device for realizing method

A synthesis device and micro-quantity technology, applied in the preparation method of peptides, chemical instruments and methods, peptides, etc., can solve the problems of time-consuming and labor-intensive reaction process, low synthesis efficiency, affecting adjacent sites, etc., and achieve peptide library construction The effect of improving efficiency, improving synthesis efficiency, and improving feeding efficiency

Pending Publication Date: 2019-12-20
浙江昂拓莱司生物技术有限公司
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Problems solved by technology

[0006] Furthermore, the washing of each site after the reaction is cumbersome. It is necessary to wait for the solution or solvent on the surface of the carrier to completely dry in the shade or air before proceeding to the next round of washing, otherwise the adjacent sites will be affected.
[0007] In the process of constructing the peptide library by the traditional SPOT method, due to the above problems, the synthesis efficiency is not high, and the reaction process is time-consuming and laborious and the cycle is long

Method used

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  • Method for quickly constructing trace peptide base and synthetizing device for realizing method
  • Method for quickly constructing trace peptide base and synthetizing device for realizing method
  • Method for quickly constructing trace peptide base and synthetizing device for realizing method

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Embodiment Construction

[0076] The following are specific embodiments of the present invention and in conjunction with the accompanying drawings, the technical solutions of the present invention are further described, but the present invention is not limited to these embodiments.

[0077] The reagents and sheet-layer solid phase carriers used in the examples of the present invention can be purchased from the market.

[0078] The present invention takes Ala-Ile-X-Ile-X-Asn-Gln-Ala as the template peptide sequence, changes the third and fifth positions (indicated by X), and takes the 20 polypeptides in Table 1 as targets peptide library to synthesize.

[0079] Table 1 Target peptide library

[0080]

[0081]

[0082] In order to synthesize the target peptide sequences in Table 1, the synthetic building blocks used are shown in Table 2:

[0083] Table 2 Synthetic Blocks

[0084] Fmoc-Gly-OH Fmoc-Arg(Pbf)-OH Fmoc-Val-OH Fmoc-Ala-OH Fmoc-Asn(Trt)-OH Fmoc-Lys(Boc)-OH Fm...

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Abstract

The invention provides a method for quickly constructing a trace peptide base and a synthetizing device for realizing the method, belongs to the field of polypeptide synthesis, and solves the problemthat a peptide base constructed by a conventional SPOT method is low in efficiency. The method for quickly constructing the trace peptide base comprises the following steps of S01: performing surfacederivatization on a lamellar solid phase carrier; S02: processing the lamellar solid phase carrier into a plurality of structure units; S03: filling the structure units into a reaction tank; S04: adding coupling reaction fluid to the reaction tank, performing a coupling reaction, after the reaction, directly adding a cleaning solvent to clean the reaction tank, after cleaning is completed, addingdeprotection reaction fluid to the reaction tank, performing a deprotection reaction, and after the reaction, directly adding the cleaning solvent to clean the reaction tank; and S05: repeating the above step S04, coupling amino acids one by one, selecting coupling reaction fluid corresponding to each amino acid during coupling different amino acids, and completing a lamellar solid phase carrier loaded full-protection peptide chain; and performing pyrolysis to obtain naked peptides or loaded naked peptides. The method disclosed by the invention has the advantages of being high in peptide baseconstruction efficiency and the like.

Description

technical field [0001] The invention belongs to the field of polypeptide synthesis, and in particular relates to a method for rapidly constructing a small amount of peptide library and a synthesis device thereof. Background technique [0002] The initial stage of the research and development of new peptide drugs is mainly the discovery of drug lead compounds and the process of structure optimization. In this process, medicinal chemists do not have a large demand for the weight of the target polypeptide, but have high requirements for the diversity of its sequence structure. Therefore, it is of great significance to quickly construct a small amount of peptide library containing a large number of structurally diverse members for corresponding medicinal chemistry research. [0003] The traditional SPOT method to construct a peptide library starts with a carrier with a sheet structure; the coupling and deprotection process is realized by adding the reaction solution to each pre...

Claims

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Application Information

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IPC IPC(8): C07K1/04C07K1/06C07K1/10C40B50/14
CPCC07K1/04C07K1/06C07K1/10C40B50/14
Inventor 章砚东任天天邱鹤
Owner 浙江昂拓莱司生物技术有限公司
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