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Peptoid and preparation method as well as application thereof

A type and reaction technology, applied in the field of medicine, can solve the problems of high inspection costs and not yet routinely carried out, and achieve the effects of low cost, rapid diagnosis, and simple synthesis

Active Publication Date: 2017-06-16
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this inspection is expensive and has not been routinely carried out

Method used

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  • Peptoid and preparation method as well as application thereof
  • Peptoid and preparation method as well as application thereof
  • Peptoid and preparation method as well as application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] In this example, the peptoid was synthesized by solid-phase subunit synthesis, which specifically included the following steps:

[0059] (1) Rink amide AM resin (substitution level 0.3mmol / g) was swollen and deprotected with hexahydropyridine, and cysteine ​​was mixed with 2-(3'-N-oxo-benzotriazole)-1, 1',3,3'-Tetramethyluronium hexafluorophosphate was equimolarly mixed, and coupled under the activation of N-methylmorpholine.

[0060] (2) Add 2M bromoacetic acid and 3.2M N,N'-diisopropylcarbodiimide (DIC) into Rink amideAM resin, react at 37°C for 30 minutes, and acylate the amino group at the end of the resin;

[0061] (3) Add 2M primary amine and react at 37°C for 90 minutes to replace the bromine atom through a nucleophilic substitution reaction to complete the synthesis of a subunit;

[0062] (4) Repeat steps (2) and (3) until completing the synthesis of the remaining units;

[0063] (5) After the synthesis is completed, the side chain protecting group is removed,...

Embodiment 2

[0067] In this example, the peptoid was synthesized by solid-phase subunit synthesis, which specifically included the following steps:

[0068] (1) Rink amide AM resin (substitution level 0.3mmol / g) was swollen and then deprotected with hexahydropyridine, and cysteine ​​and O-benzotriazole-N,N,N',N'-tetra Methylurea tetrafluoroboric acid was mixed equimolarly and coupled under the activation of N-methylmorpholine.

[0069] (2) Add 2M bromoacetic acid and 3.2M N,N'-diisopropylcarbodiimide (DIC) to Rink amideAM resin, react at 25°C for 60 minutes, and acylate the amino group at the end of the resin;

[0070] (3) Add 2M primary amine and react at 25°C for 50 minutes to replace the bromine atom through a nucleophilic substitution reaction to complete the synthesis of a subunit;

[0071] (4) Repeat steps (2) and (3) until completing the synthesis of the remaining units;

[0072] (5) After the synthesis is completed, the side chain protecting group is removed, and the peptoid is c...

Embodiment 3

[0074] In this example, the peptoid was synthesized by solid-phase subunit synthesis, which specifically included the following steps:

[0075] (1) Rink amide AM resin (substitution level 0.3mmol / g) was swollen and then deprotected with hexahydropyridine, and cysteine ​​and 1-hydroxybenzotriazole were mixed equimolarly, and in N-methylmorpholine Coupling was performed under activation.

[0076] (2) Add 2M bromoacetic acid and 3.2M dicyclohexylcarbodiimide to Rink amide AM resin, react at 40°C for 20 minutes, and acylate the amino group at the end of the resin;

[0077] (3) Add 2M primary amine and react at 20°C for 150 minutes to replace the bromine atom through a nucleophilic substitution reaction to complete the synthesis of a subunit;

[0078] (4) Repeat steps (2) and (3) until completing the synthesis of the remaining units;

[0079] (5) After the synthesis is completed, the side chain protecting group is removed, and the peptoid is cleaved from the resin with 95% triflu...

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Abstract

The invention provides a peptoid as well as a preparation method and application thereof. The peptoid comprises the following subunits: ethylenediamine (I), piperonylamine (II), beta-alanine (III), 1-naphthylamine (IV) and cysteine (V). The peptoid is simple in synthesis, has strong combining capacity with alpha-synuclein, can effectively screen the serum of PD patients and able-bodied persons through alpha-synuclein in the serum, and provides a novel liquid biopsy method and concept for diagnosis and monitoring of the Parkinson's disease.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a peptoid and its preparation method and application. Background technique [0002] Parkinson's disease (Parkinson's Disease, PD) is a very common neurodegenerative disease, high incidence and elderly people, the average age of onset is about 60 years old. So far, the prevalence of PD in people over 65 years old in my country has reached 1.7% (but this figure may be artificially low, because many patients in rural areas have never been diagnosed), and most Parkinson's disease patients are Sporadic cases, only less than 10% of patients have testable family history. The main pathological lesion of Parkinson's disease is the degeneration and death of dopamine (DA) neurons in the substantia nigra of the midbrain, which leads to a significant decrease in the content of DA in the striatum. However, although there are many studies on Parkinson's disease, its exact etiology is still uncle...

Claims

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Application Information

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IPC IPC(8): C07K7/06C07K1/06C07K1/04G01N33/68A61K38/08A61P25/16
CPCA61K38/00C07K7/06G01N33/6896G01N2800/2835Y02P20/55
Inventor 赵子健朱凌高厚乾刘明珠杨延莲胡志远
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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