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An anti-angiogenic peptide z-gp-v1 targeting FAP and its application

A Z-GP-V1, anti-angiogenesis technology, applied in the field of tumor treatment, can solve the problems of restricting the application of endogenous angiogenesis inhibitors, unable to effectively penetrate the tissue, and the use of large amounts of drugs, so as to improve the anti-tumor blood vessels. Generating effect, good medical application prospect, less toxic and side effects

Active Publication Date: 2020-06-16
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most of the existing endogenous angiogenesis inhibitors are fragments of some natural components in the process of ECM and blood coagulation, but these fragments cannot effectively penetrate tissues due to their large structures, and at the same time have defects that are easy to clear in the human body. The defects of large amount of drug used and high application cost severely limit the clinical application of endogenous angiogenesis inhibitors

Method used

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  • An anti-angiogenic peptide z-gp-v1 targeting FAP and its application
  • An anti-angiogenic peptide z-gp-v1 targeting FAP and its application
  • An anti-angiogenic peptide z-gp-v1 targeting FAP and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] The synthetic peptide Z-GP-V1 provided by the present invention has a molecular weight of 1270.47 Da and a specific sequence of: Z-Gly-Pro-Ala-Ala-Ala-Thr-Trp-Leu-Pro-Pro-Arg; It is prepared by the phase peptide synthesis method, taking a synthetic peptide Z-GP-V1 of 0.1843 g as an example, the specific preparation method is as follows.

[0041] (1) Weigh 0.3g of Wang resin into the peptide synthesizer rinsed with DMF (N,N-dimethylformamide), then add 4 mL of DMF, let it stand for 30 minutes to fully swell the resin, and use a vacuum pump to remove the DMF .

[0042] (2) Addition of the first amino acid: weigh the corresponding amounts of arginine, HoBt and DIC according to formula 1, and weigh the corresponding amounts of DMAP according to formula 2, which are 462.000 mg, 101.3475 mg, 94.65 μL, and 9.162 mg, respectively. First dissolve arginine and HoBt with 4 mL DMF and add to the synthesizer, then directly add DIC to the synthesizer, stir and react at 25°C~28°C for...

Embodiment 2

[0065] For the synthetic peptide Z-GP-V1 prepared in Example 1, the inventors conducted specific experiments to verify its anti-tumor angiogenesis effect, and the relevant experiments are briefly introduced as follows.

[0066] 1. Verification of anti-angiogenic effect in vitro

[0067] 1. Cell scratch experiment

[0068] The effect of the synthetic peptide Z-GP-V1 on the migration of human umbilical vein endothelial cells (HUVECs) was evaluated by cell scratch test. The related experimental process is briefly introduced as follows.

[0069] (1) Put HUVECs in 1×10 5 Cells / mL were seeded in a 24-well plate, and after the cell plating rate reached over 90%, use a 200 μL pipette tip to gently scratch along the mark;

[0070] (2) Subsequently, the scratched cells were washed with PBS, and the synthetic peptide Z-GP-V1 was added to each duplicate well at different concentrations (100 μM, 25 μM, 5 μM). Each concentration was an experimental group. Group 3 duplicate wells, at the ...

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Abstract

The invention belongs to the technical field of tumor treatment, and particularly relates to an anti-tumor angiogenesis synthetic peptide Z-GP-V1 for targeting FAP (familial adenomatous polyposis). The molecular weight of peptide is 1270.47 Da, and the sequence is Z-GPAAATWLPPR; the peptide is prepared by an Fmoc solid-phase multi-peptide synthetic method, and can be applied to an anti-tumor angiogenesis preparation. The anti-tumor angiogenesis synthetic peptide has the advantages that the peptide V1 is modified by a specific primer dipeptide Z-GP, the new synthetic peptide Z-GP-V1 is obtained, the new synthetic peptide has better application effects on improving of targeting property of peptide V1, improving of anti-tumor angiogenesis function, and decreasing of toxic or side effect, and the like, and the new experience and reference can be provided for the new anti-tumor angiogenesis treatment method.

Description

technical field [0001] The invention belongs to the technical field of tumor treatment, and in particular relates to a synthetic peptide Z-GP-V1 targeting FAP with anti-tumor angiogenesis effect. Background technique [0002] In recent years, the morbidity and mortality of malignant tumors have been increasing year by year. It has become the leading cause of adult death in developed countries and some developing countries. It is one of the largest public problems in the world and seriously threatens people's health and life safety. Therefore, the treatment of cancer has been widely concerned and highly valued by the international community, and finding safe and effective anti-tumor drugs with less adverse reactions has always been the focus of biomedical research. The principle of traditional clinical treatment drugs is to inhibit tumor growth by directly killing tumor cells. However, these drugs are usually cytotoxic to normal cells. Side effects such as irregular bleeding...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/06C07K1/20C07K1/06C07K1/04A61K38/08A61P35/00
CPCA61K38/00C07K7/06
Inventor 陈鲤翔王雅娟王婷陈思伟安秀丽祁元明高艳锋李国栋
Owner ZHENGZHOU UNIV
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