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Active targeting response type polypeptide drug as well as preparation method and application thereof

An active targeting and responsive technology, applied in the medical field, can solve the problem of low expression, achieve low toxicity and side effects, achieve long-term treatment, and good biocompatibility

Pending Publication Date: 2020-10-09
NINGBO INST OF MATERIALS TECH & ENG CHINESE ACADEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, studies have shown that overexpression of neuropeptide Y1 receptors has been found in clinical cases of breast cancer, brain cancer, ovarian cancer, kidney cancer and other diseases, and the expression of this receptor in normal tissues and organs is low

Method used

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  • Active targeting response type polypeptide drug as well as preparation method and application thereof
  • Active targeting response type polypeptide drug as well as preparation method and application thereof
  • Active targeting response type polypeptide drug as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Synthesis of Example 1 Compound C1[Phe6, Pro34]pNPY-GPLGLLAGQ-Docetaxel

[0027] Compound C1 was synthesized according to the following steps:

[0028] PEG-1000 type polyurethane resin was selected as the substrate, and the peptide activated raw materials (Boc type) were placed one by one in the material box of the automatic peptide synthesizer according to the sequence, and the peptide synthesizer was started. After all the raw materials have been reacted, take a small amount of resin for cutting analysis, and after confirming that it is the desired polypeptide, put docetaxel with an activated carboxyl group in material tank 1 for reaction. After the reaction, a small amount of resin was taken for detection. After confirming the product, the synthesized resin was cleaved with 1% TFA to remove amino acid side chain protection, and then purified to a purity of 99% by preparative chromatography, and the purification process was self-monitored by preparative chromatograph...

Embodiment 2

[0029] Synthesis of Example 2 Compound C2[Asn28, Pro30, Trp32]NPY(25-36)-PLGLAG-Adriamycin

[0030] Compound C2 was synthesized according to the following steps:

[0031] PEG-1000 type polyurethane resin was selected as the substrate, and the peptide activated raw materials (Boc type) were placed one by one in the material box of the automatic peptide synthesizer according to the sequence, and the peptide synthesizer was started. After all the raw materials have been reacted, take a small amount of resin for cutting analysis, and after confirming that it is the desired polypeptide, place doxorubicin with activated carboxyl groups in material tank 1 for reaction. After the reaction, a small amount of resin was taken for detection. After confirming the product, the synthesized resin was cleaved with 1% TFA to remove amino acid side chain protection, and then purified to a purity of 99% by preparative chromatography, and the purification process was self-monitored by preparative...

Embodiment 3

[0032] Synthesis of Example 3 Compound C3[Pro30, Nal32, Leu34]NPY(28-36)-PLGVRG-paclitaxel

[0033] Compound C3 was synthesized according to the following steps:

[0034] PEG-1000 type polyurethane resin was selected as the substrate, and the peptide activated raw materials (Boc type) were placed one by one in the material box of the automatic peptide synthesizer according to the sequence, and the peptide synthesizer was started. After all the raw materials have been reacted, take a small amount of resin for cutting analysis, and after confirming that it is the desired polypeptide, place paclitaxel with activated carboxyl groups in material tank 1 for reaction. After the reaction, a small amount of resin was taken for detection. After confirming the product, the synthesized resin was cleaved with 1% TFA to remove amino acid side chain protection, and then purified to a purity of 99% by preparative chromatography, and the purification process was self-monitored by preparative ...

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Abstract

The invention discloses an active targeting response type polypeptide drug. The active targeting response type polypeptide drug is formed by sequentially connecting an active targeting peptide fragment, a response type fragment and a small molecular drug group. The active target response type polypeptide drug has the characteristic of high specificity response to overexpressed enzymes and molecules of a tumor site, the effective concentration of a focus site is remarkably improved through drug release after response, the active target response type polypeptide drug can stay in a response region for a long time, and the active target response type polypeptide drug has great significance in long-time treatment and application research of the tumor site.

Description

technical field [0001] The invention relates to the field of medical technology, in particular, to an active target-responsive polypeptide drug and its preparation method and application. Background technique [0002] Drug therapy is still one of the most commonly used methods for treating cancer clinically, and it is often combined with other methods for co-treatment. However, most of the small-molecule drugs currently used in clinical practice can also cause damage to normal tissues and cells while killing tumor cells, causing serious adverse reactions and toxic side effects. At the same time, due to the lack of targeting, most small molecule drugs themselves are less enriched in the affected area, and the lower enrichment concentration is difficult to effectively kill tumor cells and is easily excreted by tumor cells and produces drug resistance. According to the different physiological conditions of the lesion, the chemical composition of the drug used can be changed by...

Claims

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Application Information

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IPC IPC(8): A61K47/64A61K45/00A61P35/00
CPCA61K47/64A61K45/00A61P35/00
Inventor 李娟蒋振奇吴爱国王胤杰李彦莹
Owner NINGBO INST OF MATERIALS TECH & ENG CHINESE ACADEMY OF SCI
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