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Al-18F mark fusion peptide and application thereof

A label fusion, al-18f technology, applied in the biological field, can solve the problems of pharmaceutical, inconvenient transportation, increased use cost, clinical application obstacles, etc., to improve probe concentration, improve specificity, and improve target/non-target The effect of target ratio

Inactive Publication Date: 2014-03-05
THE FIRST AFFILIATED HOSPITAL OF XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

in addition, 11 The half-life of C isotope is relatively short, which causes inconvenient links such as pharmacy and transportation, increases the cost of use, and hinders the wide clinical application to a certain extent.

Method used

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  • Al-18F mark fusion peptide and application thereof
  • Al-18F mark fusion peptide and application thereof
  • Al-18F mark fusion peptide and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] (1) Preparation of NOTA-PEG-RGDyK-Lys-Ac-A7R:

[0037] The reaction formula is as follows:

[0038]

[0039] Specifically: RGDyK-Lys-Ac-A7R can be purchased from home and abroad (Hangzhou Zhongpei Biochemical Co., Ltd.). Dissolve [2-[2-(fluorenylmethoxycarbonyl-amino)ethoxy]ethoxy]acetic acid in 1 mL of DMF (dimethylformamide), add NHS (N-hydroxysuccinimide, also known as HOSU) and DCC (dicyclohexylcarbodiimide), stirred at room temperature for 2 hours. Add RGDyK-Lys-Ac-A7R to the above reaction solution, adjust the pH to 8.0-8.5 with DIEA (N,N-diisopropylethylamine), and stir overnight at room temperature. Add 3mL of 0.5M NH4OAc buffer solution (pH=7.0) to the reaction solution and filter, the filtrate is separated and purified by HPLC, the fractions of the target product are collected, combined and freeze-dried, the product fluorenylmethoxycarbonyl-PEG-RGDyK-Lys-Ac- Add 20% piperidine to A7R and react at room temperature for 30 minutes to remove the fluorenylmet...

Embodiment 2

[0048] This embodiment is a comparative example, and the contrast is [Al 18 F]NOTA-PEG-RGDyK, the structural formula is as follows:

[0049]

[0050] Its preparation method is as follows:

[0051] (1) RGDyK can be purchased from home and abroad. Dissolve [2-[2-(fluorenylmethoxycarbonyl-amino)ethoxy]ethoxy]acetic acid in 1 mL of DMF (dimethylformamide), add NHS (N-hydroxysuccinimide, also known as HOSU) and DCC (dicyclohexylcarbodiimide), stirred at room temperature for 2 hours. Add RGDyK to the above reaction solution, adjust the pH to 8.0-8.5 with DIEA (N,N-diisopropylethylamine), and stir overnight at room temperature. Add 3mL of 0.5M NH4OAc buffer solution (pH=7.0) to the reaction solution and filter, the filtrate is separated and purified by HPLC, the fractions of the target product are collected, combined and freeze-dried, the product fluorenylmethoxycarbonyl-PEG-RGDyK is added with 20% piperidine React at room temperature for 30 minutes to remove fluorenylmethoxyc...

Embodiment 3

[0057] This embodiment is a comparative example, and the contrast is [Al 18 F]NOTA-PEG3-A7R, the structural formula is as follows:

[0058]

[0059] (1) A7R can be purchased at home and abroad. Dissolve [2-[2-(fluorenylmethoxycarbonyl-amino)ethoxy]ethoxy]acetic acid in 1 mL of DMF (dimethylformamide), add NHS (N-hydroxysuccinimide, also known as HOSU) and DCC (dicyclohexylcarbodiimide), stirred at room temperature for 2 hours. Add ATWLPPR to the above reaction solution, adjust the pH to 8.0-8.5 with DIEA (N,N-diisopropylethylamine), and stir overnight at room temperature. Add 3mL of 0.5M NH4OAc buffer solution (pH=7.0) to the reaction solution and filter, the filtrate is separated and purified by HPLC, the fractions of the target product are collected, combined and freeze-dried, the product fluorenylmethoxycarbonyl-PEG-A7R is added with 20% piperidine React at room temperature for 30 minutes to remove fluorenylmethoxycarbonyl, then add 2,2'-(7-(2-((2,5-dioxopyrrolidin-1-...

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Abstract

The invention discloses an Al-18F mark fusion peptide and an application thereof. The Al-18F mark fusion peptide comprises glioma specific targeted polypeptides cRGDyK and A7R connected together. The preparation method comprises the following steps: (1) preparing NOTA-PEG-RGDyK-Lys-Ac-A7R; (3) preparing 18F physiological saline liquor; (3) preparing [Al18F]NOTA-PEG-RGDyK-Lys-Ac-A7R; and (4) purifying the prepared [Al18F]NOTA-PEG-RGDyK-Lys-Ac-A7R to obtain the Al-18F mark fusion peptide. The Al-18F mark fusion peptide disclosed by the invention comprises glioma specific targeted polypeptides cRGDyK and A7R connected together, and the specificity of the fusion peptide on glioma is further improved by means of different targeted biological characteristics.

Description

technical field [0001] The invention belongs to the field of biotechnology, in particular to an Al- 18 F-labeled fusion peptide and its application. Background technique [0002] Glioma is the most common primary intracranial tumor, accounting for about 40-60% of all intracranial tumors, and has the characteristics of high recurrence rate, high mortality rate, and low cure rate. One of the main reasons is that most malignant gliomas grow infiltratingly and have unclear borders with the surrounding brain tissue. Currently, it is difficult to accurately determine the extent of the tumor using imaging techniques in clinical practice, and the evaluation of recurrence after treatment (surgery, radiotherapy and chemotherapy) is even more obvious. Insufficient, to increase the difficulty of clinical diagnosis and treatment. The establishment of specific imaging techniques for gliomas is of great significance for diagnosing malignant gliomas, guiding clinical treatment strategies ...

Claims

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Application Information

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IPC IPC(8): C07K19/00C07K1/00
Inventor 吴华马玉飞陈皓鋆梁胜李业森彭添兴
Owner THE FIRST AFFILIATED HOSPITAL OF XIAMEN UNIV
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