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Diagnostic and therapeutic gastric cancer vascular specific binding peptide GEBP11 isotope probe

A 131I-GEBP11, specific binding technology, applied in the field of biomedicine, can solve problems such as human error, invasiveness, and inability to functionally evaluate angiogenesis activity

Active Publication Date: 2010-12-29
FOURTH MILITARY MEDICAL UNIVERSITY
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Problems solved by technology

[0004] At present, the evaluation of tumor angiogenesis still mainly relies on the traditional pathological method of immunohistochemical staining to count MVD. The development of molecular imaging technology provides an opportunity to solve this problem. Using specific molecular probes, cells and molecular events in the process of tumor development can be monitored in vivo, in real time, and dynamically. real-time tracking

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  • Diagnostic and therapeutic gastric cancer vascular specific binding peptide GEBP11 isotope probe
  • Diagnostic and therapeutic gastric cancer vascular specific binding peptide GEBP11 isotope probe
  • Diagnostic and therapeutic gastric cancer vascular specific binding peptide GEBP11 isotope probe

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Embodiment Construction

[0044] Tumor molecular imaging and radiation receptor therapy are hot spots in the emerging field of tumor research in recent years, and their development depends on specific targeting molecules with high affinity. The present invention is based on the gastric cancer blood vessel-specific binding peptide GEBP11 obtained in the previous work, using radioactive isotopes 99 Tc m o 4 - , 131 I was labeled separately, and the diagnostic and therapeutic gastric cancer blood vessel-specific isotope-labeled short peptide probes were successfully prepared. After quality identification, the labeled peptides had good radiochemical purity, specific activity, in vivo and in vitro stability, and biological activity. Receptor radioligand binding analysis, isotope tracer experiments in vivo, immunofluorescence or chemical staining and other experiments further identified that the GEBP11 isotope probe has good specificity and affinity for gastric cancer vascular endothelial cells, and can b...

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Abstract

The invention belongs to the field of biomedical technology, and in particular relates to a diagnostic and therapeutic gastric cancer vascular specific isotope-labeled short peptide probe <99>TC<m>-GEBP11 or <131>I-GEBP11 and a preparation method thereof. The probe is characterized in that the diagnostic isotope <99>Tc<m>O4<-> or therapeutic isotope <131>I is connected to GEBP11 short peptide, so that the short peptide probe is endowed with double functions of gastric cancer vascular targeting and diagnosis or therapy. In-vivo tracer experiments of the isotope show that the GEBP11 isotope probe has the characteristics of good in-vivo gastric cancer tissue targeting and specific distribution. SPECT imaging of <99>Tc<m>-GEBP11 in a gastric cancer bearing nude mice excellently shows a lesion site of transplanted tumor, and the ideal imaging time interval is within 18 to 24 hours after the injection. Results of tumor-suppressing experiments show that <131>I-GEBP11 has obvious effects of suppressing tumor growth and prolonging life time of the tumor bearing mice and weak toxic or side effect. The GEBP11 isotope probe has certain theoretical significance and great potential application value in gastric cancer diagnosis, vascular targeting therapy and evaluation of therapeutic effect and the like.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, in particular to a diagnostic and therapeutic gastric cancer blood vessel-specific isotope-labeled short peptide probe 99 Tc m -GEBP11, 131 I-GEBP11 and its preparation method also relate to the application of the probe in this field. Background technique [0002] Gastric cancer is the most common malignant tumor of the digestive tract, and its mortality rate ranks second in the global cancer mortality rate. Traditional treatment methods such as surgery, chemotherapy and external radiotherapy cannot achieve ideal therapeutic effects. Studies have found that angiogenesis is one of the important conditions in the process of tumor development, and the process, nature and density of tumor micro-vascularization are directly related to the ability of tumor growth, invasion, metastasis and prognosis. Based on the theory and facts of tumor vascular dependence, vascular suppression therapy has bec...

Claims

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Application Information

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IPC IPC(8): A61K51/08A61P1/00A61P35/00A61K103/10A61K101/02
Inventor 梁树辉丁杰惠晓丽吕艳香刘洋吴开春樊代明
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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