Non-natural amino acid short peptide and application thereof in tumor resistance

An unnatural amino acid, amino acid technology, applied in antitumor drugs, medical preparations containing active ingredients, peptides, etc., can solve the problems of inaccurate targeting of natural active peptides, normal cell toxicity, poor stability, etc. The effect of tumor cell proliferation and migration ability

Active Publication Date: 2021-04-06
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, it has been found that natural active peptides are easily degraded in the body and have poor stability; at the same time, some natural active peptides are not accurate enough to target and easily cause toxic effects on normal cells

Method used

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  • Non-natural amino acid short peptide and application thereof in tumor resistance
  • Non-natural amino acid short peptide and application thereof in tumor resistance
  • Non-natural amino acid short peptide and application thereof in tumor resistance

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1: Synthesis and screening of small molecule short peptides

[0031] (1) Synthesis of unnatural amino acid short peptides

[0032] The present invention is based on the heptapeptide library established by our laboratory, and synthesizes non-natural amino acid short peptides through chemical synthesis. For the specific synthesis method, please refer to the Chinese patent application (CN111228508A-a multi-target anti-tumor polypeptide drug couple) Compound and its preparation method and application) Example 1:

[0033] Amide resin (RINK AMIDE RESIN; C 30 h 26 NO 5 R) Purchased from P3BioSystems in the United States (the degree of substitution is 0.503mmol / g); pretreatment before use: add DMF (N,N-dimethylformamide) to the amide resin, soak for 2-3 hours, and then discard Remove the solution to obtain the pretreated amide resin;

[0034] Fmoc-Lys(Dde)-OH, Fmoc-AEEA ([2-[2-(Fmoc-amino)ethoxy]ethoxy]acetic acid), Fmoc-Glu(OtBu)-OH, Fmoc-Lys(Boc) , Fmoc-AEEA-OH,...

Embodiment 2

[0054] Example 2: Detection of broad-spectrum anti-tumor properties of short peptide CR1

[0055] (1) Select the test cell line

[0056] Alternative cell lines are A549 (human lung cancer cells), MHCC-97H (human highly metastatic liver cancer cells), MCF-7 (human breast cancer cells), DU145 (human prostate tumor cells), all of which were purchased from Shanghai cell bank.

[0057] (2) Test method

[0058] The test method is the same as step ② in Example 1, and the cell lines are A549, MHCC-97H, MCF-7, and DU145.

[0059] (3) Test results

[0060] The result is as figure 2 As shown: the CR1 short peptide has a certain level of inhibition on the proliferation of the above four cell lines, and all of them are concentration-gradient dependent. The maximum inhibitory efficiency can be obtained with a basic administration concentration of no more than 20 μM.

Embodiment 3

[0061] Example 3: Detection of CR1 short peptide inhibiting migration of MHCC-97H in vitro

[0062] (1) Select experimental cells

[0063] MHCC-97H cells themselves have good migration ability, and CR1 short peptide has a significant effect on the proliferation of MHCC-97H cells in the experiment of inhibiting cell proliferation, so MHCC-97H cells were selected as the experimental subjects in this experiment.

[0064] (2) Test method

[0065] A. Cultivate MHCC-97H cells in RPMI 1640 medium supplemented with 10% (v / v) fetal bovine serum to the logarithmic phase, digest and collect the cells, spread them evenly in a 12-well plate, and wait until the cells are confluent to 90% DMEM medium containing 0.5% (v / v) fetal bovine serum was starved for 24 hours, then scratched, and washed 3 times with PBS buffer, and then the medium was changed to add 0.5% (v / v) fetal bovine serum and CR1 short peptide in DMEM medium, and the scratches were photographed and recorded, and three replicat...

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Abstract

The invention discloses a non-natural amino acid short peptide and application thereof in tumor resistance. The amino acid sequence of the non-natural amino acid short peptide is shown as {D-Tyr(Me)}-Asp-Dpr-Asn-{D-Glu}-Thr-Cha. The non-natural amino acid oligopeptide can be synthesized by adopting an existing conventional method. The short peptide can inhibit proliferation and migration of tumor cells, achieves an anti-tumor effect, and does not harm the activity of normal cells. Therefore, the non-natural amino acid short peptide can be used for preparing antitumor drugs for treating esophageal cancer, lung cancer, liver cancer, breast cancer, prostate cancer, gastric cancer, colorectal cancer and other malignant tumors.

Description

technical field [0001] The invention belongs to the fields of biotechnology and medicine, in particular to a non-natural amino acid short peptide and its application in antitumor. Background technique [0002] Cancer, that is, malignant tumor, is recognized as a type of disease that is extremely difficult to cure, and is a social problem that seriously endangers human life and health. It is estimated that the number of people suffering from cancer in the world is "growing rapidly". Although with the development of medical technology, there are many clinical anti-tumor treatment methods, but patients still have problems such as multi-drug resistance, poor curative effect, recurrence and metastasis. Traditional radiotherapy and chemotherapy may cause unpredictable side effects, and tumor cells Chemotherapy drug antagonism also complicates treatment considerably. Therefore, how to effectively overcome tumor treatment resistance and develop effective anti-tumor drugs has become...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06A61K38/08A61P35/00
CPCA61K38/00A61P35/00C07K7/06
Inventor 洪岸陈小佳蔡玉玲
Owner JINAN UNIVERSITY
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