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Tumor vascular targeting peptide GX1

A technology of tumor blood vessels and targeting peptides, applied in the field of biomedicine, can solve the problems of lack of tumor tissue targeting, poor treatment effect, and large toxic and side effects, and achieve simple and rapid labeling process, low labeling rate, and high labeling rate Effect

Inactive Publication Date: 2009-09-16
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
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Problems solved by technology

Chemotherapy mostly targets tumor cells, which can easily induce drug resistance, and systemic administration lacks tumor tissue targeting, resulting in poor therapeutic effect and severe side effects

Method used

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  • Tumor vascular targeting peptide GX1
  • Tumor vascular targeting peptide GX1
  • Tumor vascular targeting peptide GX1

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Experimental program
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Effect test

Embodiment Construction

[0035] In the embodiment of the present invention, tumor blood vessel targeting peptide GX1 is adopted 99 Tc m Labeled tumor blood vessel targeting peptide GX1.

[0036] GX1 has obtained the national invention patent, patent number: 200410026137.0

[0037] The preparation method of tumor blood vessel targeting peptide GX1 is:

[0038] (1) Use of radionuclides 99 Tc m o 4 - , using the direct method to label GX1;

[0039] (2 pairs 99 Tc m - GX1 for quality and biological activity identification;

[0040] (3) Construct the in vitro culture model of human gastric cancer vascular endothelial cells. 99 Tc m - Test the specificity and affinity of GX1 binding to human gastric cancer vascular endothelial cells in vitro;

[0041] (4) yes 99 Tc m -Test the targeting of GX1 in vivo tumor tissue and the specific distribution characteristics of tumor tissue.

[0042] 99 Tc m o 4 - Directly label GX1, use ascorbic acid to reduce the double cysteine ​​bond (disulfide bond)...

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Abstract

The invention belongs to the technical field of biomedicine, and in particular provides tumor vascular targeting peptide GX1. The invention utilizes a radioactive nuclide <99>Tc<m>O4 <-> to successfully mark GX1 by a direct method. Quality identification proves that <99>Tc<m>-GX1 has good radiochemical purity, specific activity and in vivo / vitro stability. In vitro microcosmic receptor autoradiography shows that the <99>Tc<m>-GX1 can combine with human umbilical vein endothelial cells and has good biological activity. In vitro microcosmic autoradiography, receptor radioligand conjoint analysis and competitive inhibition analysis confirm that the combination of the <99>Tc<m>-GX1 and tumor vascular endothelial cells has good specificity and affinity. ECT imaging and biological distribution prove that the <99>Tc<m>-GX1 has good targeting property to in vivo tumor tissue and specific distribution characteristicto tumor tissue. The <99>Tc<m>-GX1 has certain theoretical significance and great potential application value in diagnosis of gastric cancer, study on vascular targeting therapy, and other aspects.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to tumor blood vessel targeting peptide GX1. Background technique [0002] Gastric cancer is the most common malignant tumor of the digestive tract. At present, the death rate of gastric cancer ranks second in the global cancer death rate. The existing treatment methods are mainly combined surgery, external radiotherapy, and chemotherapy. Chemotherapy mostly targets tumor cells, which can easily induce drug resistance, and systemic administration lacks tumor tissue targeting, resulting in poor therapeutic effect and severe side effects. Tumor vasculature inhibitory therapy targeting tumor vascular endothelium has become a research hotspot at present. Angiogenesis is essential for tumor growth and metastasis. The key to tumor vascular suppression therapy is to improve the targeting of tumor vascular endothelium. Studies have shown that blood vessels in different ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/64C07K1/13A61K51/00A61K38/12A61P35/00A61K103/10
Inventor 吴开春惠晓丽刘志国刘惊涛梁树辉樊代明
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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