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EphB4 acceptor targeting polypeptide and applications thereof

A technology targeting peptides and receptors, which is applied in the field of radiopharmaceutical labeling and nuclear medicine, can solve the problems of being unable to be used directly, the short biological half-life of TNYL-RAW, and the poor targeting of EphB4, and achieve the effect of improving the half-life of metabolism

Inactive Publication Date: 2016-06-29
BEIJING RUIDEOU BIOLOGICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The TNYL-RAW used in this technology has a short biological half-life and poor EphB4 targeting, and the nuclides that are indirectly coupled through CCPM nanoparticles cannot be used directly

Method used

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  • EphB4 acceptor targeting polypeptide and applications thereof
  • EphB4 acceptor targeting polypeptide and applications thereof
  • EphB4 acceptor targeting polypeptide and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1 Preparation of EphB4 receptor targeting polypeptide NOTA-c-(TNYL-RAW) (1)

[0037] c-(TNYL-RAW) was mixed with the chelating agent NOTA at a molar ratio of 1:1. At the same time, EDC with a molar ratio of c-(TNYL-RAW) of 1:1 was added, and the reaction was protected from light for 2 hours, and the reaction was monitored by HPLC. Essentially complete, NOTA-c-(TNYL-RAW) was obtained by semi-preparative HPLC separation. And configured as a 5mg / ml aqueous solution kit.

Embodiment 2

[0038] Example 2 Preparation of EphB4 receptor targeting polypeptide NOTA-c-(TNYL-RAW) (2)

[0039] c-(TNYL-RAW) was mixed with the chelating agent NOTA at a molar ratio of 1:3. At the same time, EDC with a molar ratio of c-(TNYL-RAW) of 1:2 was added, and reacted in the dark for 12 hours, and was monitored by HPLC until the reaction Essentially complete, NOTA-c-(TNYL-RAW) was obtained by semi-preparative HPLC separation. And configured as a 5mg / ml NOTA-c-(TNYL-RAW) aqueous solution kit.

Embodiment 3

[0040] Example 3 Preparation of EphB4 receptor targeting polypeptide NOTA-c-(TNYL-RAW) (3)

[0041] c-(TNYL-RAW) was mixed with the chelating agent NOTA at a molar ratio of 1:5. At the same time, EDC with a molar ratio of c-(TNYL-RAW) of 1:3 was added, and the reaction was protected from light for 24 hours, and the reaction was monitored by HPLC. Essentially complete, NOTA-c-(TNYL-RAW) was obtained by semi-preparative HPLC separation. And configured as a 5mg / ml aqueous solution kit.

[0042] The NOTA-c-(TNYL-RAW) prepared in Example 1-3 is used for the following radionuclide labeling of the present invention to prepare imaging agents, and it is found that the obtained radionuclide-labeled molecular probes can be used for EphB4 high-expression tumors Early diagnosis and precise positioning, especially the molecular probe prepared from the labeled precursor obtained in Example 2 has the best imaging effect.

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Abstract

The invention provides a EphB4 acceptor targeting polypeptide and applications thereof, and belongs to the technical fields of radioactive drug labeling and nuclear medicine. A polypeptide (TNYLFSPNGPIARAW, TNYL-RAW for short), which is affinity to EphB4, is taken as the matrix; then the polypeptide is modified by a chemical method and a biological method to obtain a EphB4 targeting molecular probe precursor NOTA-C-(TNYL-RAW); and then the molecular probe precursor is labeled by nuclides for diagnosis or nuclides for treatment to obtain nuclide labeled molecular probe NOTA-c-(TNYL-RAW). The polypeptide can be used to prepare a kit that can be applied to early diagnosis and precise positioning of tumors with high expression of EphB4 and drugs for biological target treatment of tumors with high expression of EphB4.

Description

technical field [0001] The invention relates to the technical fields of radiopharmaceutical labeling and nuclear medicine, in particular to EphB4 receptor-targeting polypeptides, radionuclide-labeled EphB4 receptor-targeting polypeptides and applications thereof. Background technique [0002] Eph is the largest subfamily of known receptor tyrosine kinases (RTKs). As the first definite receptor, EphA1 has been found to be expressed in various solid tumors such as liver cancer, lung cancer, breast cancer, and colon cancer. The expression level of EphA2 is also increased in human melanoma, breast cancer, prostate cancer, and colon cancer, and the increased level is positively correlated with the malignant degree and metastasis behavior of the tumor. Studies have shown that EphB4 receptors are expressed at the initial stage of tumors, and more than 60% of solid tumors have abnormal expression of EphB4 receptors. High expression of EPh receptors is closely related to the growth...

Claims

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Application Information

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IPC IPC(8): C07K7/64A61K51/08A61P35/00
Inventor 黄卫
Owner BEIJING RUIDEOU BIOLOGICAL TECH CO LTD
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