Synthetic peptide NK3R-A2 based on NK3 receptor and application thereof

A technology of NK3R-A2, synthetic peptide, applied in the field of tumor treatment

Active Publication Date: 2016-10-12
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, although there have been many basic studies on the biological regulation mechanism of NKB and its receptor NK3, it is still in the preliminary exploration stage, and further research on its application in anti-tumor angiogenesis still needs to be further explored.

Method used

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  • Synthetic peptide NK3R-A2 based on NK3 receptor and application thereof
  • Synthetic peptide NK3R-A2 based on NK3 receptor and application thereof
  • Synthetic peptide NK3R-A2 based on NK3 receptor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The synthetic peptide NK3R-A2 provided by the present invention has a molecular weight of 1536.70Da; the specific sequence is Cys-Asn-Gly-Arg-Cys-Gly-Gly-Asp-Phe-Phe-MePhe-Gly-Leu-Met-NH 2 ; or abbreviated as: CNGRC-GG-DFF(MeF)GLM-NH 2 . The synthetic peptide is prepared by the Fmoc solid-phase peptide synthesis method; taking a synthetic peptide NK3R-A2 of 0.2495 g in a certain synthesis as an example, the specific preparation steps are described in detail as follows.

[0048] (1) Weigh 0.3g Rink resin into the peptide synthesizer rinsed with DMF, then add 4mL DMF, let it stand for 30 minutes to make the resin fully swell, and then use a vacuum pump to remove the DMF; deprotection twice:

[0049] The deprotection refers to adding 4mL of deprotection solution (the volume ratio of piperidine to DMF is 1:3) into the synthesizer, stirring and reacting at 25°C~28°C for 20min, and vacuum pumping to dry;

[0050] (2) Wash the deprotected resin in step (1) in the following o...

Embodiment 2

[0073] For the synthetic peptide NK3R-A2 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.

[0074] one, Validation of anti-angiogenic effect in vitro

[0075] 1 , Cell proliferation assay

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Abstract

The invention belongs to the technical field of tumor treatment, and particularly relates to a synthetic peptide NK3R-A2 based on an NK3 receptor. The synthetic peptide NK3R-A2 based on the NK3 receptor has the tumor angiogenesis resisting effect. The molecular weight of the synthetic peptide is 1536.70 Da, and the specific sequence of the synthetic peptide is CNGRCGGDFF(MeF)GLM-NH2. The synthetic peptide is prepared through an Fmoc solid-phase polypeptide synthesis method and can be used for preparing anti-tumor preparations. Through in-vitro cell viability experiments, cell scratch experiments and cell migration experiments, the angiogenesis resisting effect of the synthetic peptide is verified; meanwhile, through further chicken chorioallantoic membrane carrier experiments and euangiotic mice S180 transplantation tumor model experiments on the synthetic peptide, it is verified that the synthetic peptide is obvious in tumor inhibiting effect, has the tumor angiogenesis resisting effect and has no obvious toxic or side effect; the synthetic peptide has good medical application prospects and also provides a targeting sequence with great potential for tumor treatment.

Description

technical field [0001] The invention belongs to the technical field of tumor treatment, and in particular relates to a synthetic peptide NK3R-A2 based on NK3 receptor with anti-tumor angiogenesis effect. Background technique [0002] In recent years, with the rapid development of the global economy, the level of clinical diagnosis, surgical treatment, chemotherapy and radiotherapy has also been continuously improved. In recent decades, the number of cancer patients has increased linearly, and people are in urgent need of new and effective tumor treatment strategies and means. Since Folkman discovered tumor angiogenesis factor (TAF) in the 1970s, people have gained a new understanding of angiogenesis, especially in the past 10 years, people have conducted a lot of research on the relationship between angiogenesis and tumor development, Tumors are found to be vascular-dependent malignant cells, and their growth, metastasis, recurrence and prevention are closely related to tum...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/08C07K1/06C07K1/04A61K38/10A61P35/00
CPCA61K38/00C07K7/08
Inventor 陈鲤翔陈思伟石梁王婷王成功祁元明安秀丽高艳锋李国栋
Owner ZHENGZHOU UNIV
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