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Radioactive rhenium marked polypeptide containing RGD sequence as well as preparation method and application thereof

A radioactivity and sequence technology, applied in the field of peptides, can solve problems such as affecting the activity of peptides, and achieve the effects of high labeling rate, simple operation, and easy availability of raw materials.

Inactive Publication Date: 2009-05-06
SHANGHAI INST OF APPLIED PHYSICS - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Therefore, the technical problem to be solved in the present invention is to provide a radioactive rhenium-labeled polypeptide containing RGD sequence and its preparation method and application, aiming at the defect that the existing radioactive rhenium-labeled polypeptide containing RGD sequence will affect the activity of the polypeptide. Does not change the structure of the peptide, does not affect the biological activity of the peptide, and has a high labeling rate

Method used

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  • Radioactive rhenium marked polypeptide containing RGD sequence as well as preparation method and application thereof
  • Radioactive rhenium marked polypeptide containing RGD sequence as well as preparation method and application thereof
  • Radioactive rhenium marked polypeptide containing RGD sequence as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0023] Example 1 Preparation of Compound 1

[0024] 1. According to the prior art, fac-[ 188 Re(CO) 3 (H 2 O) 3 ] + Synthesis and identification of

[0025] Weigh 4.5mg BH 3 .NH 3 (chemical name borane ammonium complex) is added in a clean and dry 10ml vial, and sealed with a cap. Pass CO gas into the vial for about 20 minutes. 8 μl of phosphoric acid with a concentration > 85% and 1 ml of Na with a radioactivity of 3 mCi / ml 188 ReO 4The normal saline eluent was mixed, and then injected into the vial that had been filled with CO gas in advance. React in a 70°C water bath for 15 minutes. Immediately after the reaction, it was cooled with ice water. The reaction mixture was filtered through a QMA Spe-Pak column for separation and purification. The resulting fac-[ 188 Re(CO) 3 (H 2 O) 3 ] + The radioactive purity reaches more than 95%.

[0026] The reaction products were identified by thin-plate chromatography (TLC) and high-performance liquid chromatography (H...

Embodiment 2

[0034] Example 2 Preparation of Compound 2

[0035] fac-[ 188 Re(CO) 3 (H 2 O) 3 ] + The synthesis is the same as in Example 1. Take 50μl concentration as 10 -4 mol of polypeptide b (its structure is shown in Table 1, synthesized by Shanghai Jier Biological Co., Ltd.) and 450 μl of fac-[ 188 Re(CO) 3 (H 2 O) 3 ] + Mix well. React at 65°C for 20 minutes to obtain the corresponding complex (namely compound 2). The same HPLC and double developing agent TLC as in Example 1 were used to determine the labeling rate of the reaction. For HPLC purification of peptides and 188 The Re-RGD retention times are summarized in Table 2. The marking rate is 93%.

Embodiment 3

[0036] Example 3 Preparation of compound 3

[0037] fac-[ 188 Re(CO) 3 (H 2 O) 3 ] + The synthesis is the same as in Example 1. Take 50μl concentration as 10 -4 mol / ml of polypeptide c (its structure is shown in Table 1, synthesized by Shanghai Jier Biological Co., Ltd.) and 450 μl of fac-[ 188 Re(CO) 3 (H 2 O) 3 ] + Mix well. React at 65°C for 20 minutes to obtain the corresponding complex (namely compound 3). The same HPLC and double developing agent TLC as in Example 1 were used to determine the labeling rate of the reaction. For HPLC purification of peptides and 188 The Re-RGD retention times are summarized in Table 2. The marking rate is 95%.

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Abstract

The invention discloses a polypeptide which is marked by radioactive rhenium and contains RGD amino acid sequence, a preparation method and application thereof, wherein N terminal of the polypeptide is histidine residue which is chelated with radioactive rhenium. The structure of the polypeptide is shown as general formula (I), wherein X is a polypeptide chain containing Arg-Gly-Asp sequence. The polypeptide adopts raw materials available. The whole experiment process has simple operation, does not have special requirements such as high temperature and high pressure, adopts a [Re(CO)3(H2O)3]<+> precursor to mark the polypeptide, does not change the structure of the polypeptide, does not affect the biological activity of the polypeptide, and has important realistic significance on early diagnosis and treatment of angiogenesis and tumor transfer.

Description

technical field [0001] The invention belongs to the field of polypeptides, in particular to a radioactive rhenium-labeled polypeptide containing RGD sequence, its preparation method and application. Background technique [0002] Angiogenesis, the process of generating new blood vessels on the basis of existing blood vessels, is the basis of tumor growth and metastasis. Integrin alpha v beta 3 Plays an important role in the process of angiogenesis. Integrin alpha v beta 3 It plays a role mainly by binding to ligands containing RGD sequences in the extracellular matrix. The RGD (arginyl-glycyl-aspartic acid, Arg-Gly-Asp) sequence is the basic unit of the widely distributed cell recognition system and the unique structure of fibronectin. Therefore, peptides containing RGD sequences and their analogues can be used as antagonists to compete with integrins, thereby blocking the messenger transmission of vascular epithelial cell proliferation, terminating cell proliferation, ...

Claims

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Application Information

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IPC IPC(8): C07K5/117C07K7/06C07K7/08C07K1/13A61K49/22A61K51/00A61P35/00A61K103/10
Inventor 于俊峰马玉飞唐林尹端沚
Owner SHANGHAI INST OF APPLIED PHYSICS - CHINESE ACAD OF SCI
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