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An anti-angiogenic peptide z-gp-v2 targeting FAP and its application

A Z-GP-V2, anti-angiogenesis technology, applied in the field of tumor treatment, can solve the problems of limiting the application of endogenous angiogenesis inhibitors, inability to penetrate tissues effectively, and using a large amount of drugs, so as to improve anti-tumor vascular 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-v2 targeting FAP and its application
  • An anti-angiogenic peptide z-gp-v2 targeting FAP and its application
  • An anti-angiogenic peptide z-gp-v2 targeting FAP and its application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] The synthetic peptide Z-GP-V2 provided by the present invention has a molecular weight of 1149.6, specifically: Z-Gly-Pro-Ala-Ala-Asn-Leu-Leu-Met-Ala-Ala-Ser, solidified by Fmoc It is prepared by the phase peptide synthesis method, taking a synthetic peptide Z-GP-V2 of 0.2073 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, then add 4 mL of DMF, let it stand for 30 minutes to fully swell the resin, and then use a vacuum pump to remove the DMF.

[0042] (2) Addition of the first amino acid: Weigh the corresponding amount of serine, HoBt and DIC according to formula 1, and weigh the corresponding amount of DMAP according to formula 2, which are 287.55mg, 101.3475mg, 94.65μL, and 9.162mg respectively. Add 4 mL of DMF dissolved serine and HoBt to the synthesizer, then directly add DIC to the synthesizer, stir and react at 25°C to 28°C for 10 minutes, then add DMAP dissolved in...

Embodiment 2

[0064] For the synthetic peptide Z-GP-V2 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.

[0065] 1. Verification of anti-angiogenic effect in vitro

[0066] 1. Cell scratch experiment

[0067] The effect of the synthetic peptide Z-GP-V2 on the migration of human umbilical vein endothelial cells (HUVECs) was evaluated by cell scratch test. The relevant experimental process is briefly introduced as follows.

[0068] (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;

[0069] (2) Afterwards, the scratched cells were washed with PBS, and Z-GP-V2 was added to each duplicate well at different concentrations (100, 25, 5 μM), each concentration was an experimental group, and each group had 3 At the same time, serum-free RPMI 1640 m...

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Abstract

The invention belongs to the technical field of tumor therapies, and particularly relates to an FAP-targeted anti-angiogenesis peptide Z-GP-V2 with an anti-tumor angiogenesis effect. The molecular weight of the synthetic peptide is 1149.6, and the sequence of the synthetic peptide is Z-GPAANLLMAAS; the synthetic peptide is prepared by adopting an Fmoc solid-phase polypeptide synthesis method and used for preparing an anti-tumor angiogenesis preparation. Accordingly, the novel synthetic peptide Z-GP-V2 is obtained by modifying a V2 peptide through a specific substrate dipeptide Z-GP, and the novel synthetic peptide has the good application effects on improvement of the targeting property and the anti-tumor angiogenesis effect of the V2 peptide, reduction of the toxic and side effects of the V2 peptide and the like and provides new use for reference for a novel anti-tumor angiogenesis therapeutic 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-V2 targeting FAP with an 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 bleed...

Claims

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Application Information

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