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188 re-labeled tumor targeting cyclic nonapeptide molecular probe and preparation method thereof

A tumor targeting and molecular probe technology, applied in the field of molecular imaging, can solve problems such as improper methods and reduced biological activity of polypeptides, and achieve the effects of maintaining stability, improving targeting, and increasing tumor uptake

Active Publication Date: 2021-05-28
WUXI MATERNAL & CHILD HEALTH HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, the common disulfide bond ring-forming target polypeptide labeling is often used as a direct method, while some labeling by indirect methods is due to improper methods, bifunctional chelating linkers and disulfide bonds can compete for binding 188 Re, both cause the reduction of the biological activity of the peptide

Method used

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  • <sup>188</sup> re-labeled tumor targeting cyclic nonapeptide molecular probe and preparation method thereof
  • <sup>188</sup> re-labeled tumor targeting cyclic nonapeptide molecular probe and preparation method thereof
  • <sup>188</sup> re-labeled tumor targeting cyclic nonapeptide molecular probe and preparation method thereof

Examples

Experimental program
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Embodiment 1188

[0026] Example 1 188 Preparation of Re-DTPA-c(CGRRAGGSC) Molecular Probe

[0027] at 200μCi 188 ReO 4 - Fill the solution with nitrogen to prevent oxidation, then add 2mg of CuCl as a reducing agent, and then add 2mg of sodium gluconate, adjust the pH of the reaction system to 5.0 with dilute hydrochloric acid, and react at 20°C for 90min. Then add an appropriate amount of Na to the reaction solution 2 S 2 o 3 , the pre-restored 188 After the color of the Re reaction solution was adjusted to blue-green, 100 μg of DTPA-c (CGRRAGGSC) was added and reacted at 25° C. for 90 min. The amino acid sequence of CGRRAGGSC is shown in SEQ ID NO.1.

Embodiment 2188

[0028] Example 2 188 Preparation of Re-DTPA-c(CGRRAGGSC) Molecular Probe

[0029] at 200μCi 188 ReO 4 - Fill the solution with nitrogen to prevent oxidation, then add 2mg of CuCl as a reducing agent, and then add 10mg of sodium gluconate, adjust the pH of the reaction system to 5.8 with dilute hydrochloric acid, and react at 60°C for 30min. Then add an appropriate amount of Na to the reaction solution 2 S 2 o 3 , the pre-restored 188 After the color of the Re reaction solution was adjusted to blue-green, 150 μg of DTPA-c (CGRRAGGSC) was added and reacted at 60° C. for 30 minutes. The amino acid sequence of CGRRAGGSC is shown in SEQ ID NO.1.

Embodiment 3188

[0030] Example 3 188 Preparation of Re-DTPA-c(CGRRAGGSC) Molecular Probe

[0031] at 200μCi 188 ReO 4 - Fill the solution with nitrogen to prevent oxidation, then add 2mg of CuCl as a reducing agent, and then add 20mg of sodium gluconate, adjust the pH of the reaction system to 5.5 with dilute hydrochloric acid, and react at 45°C for 70min. Then add an appropriate amount of Na to the reaction solution 2 S 2 o 3 , the pre-restored 188After the color of the Re reaction solution was adjusted to blue-green, 1000 μg of DTPA-c (CGRRAGGSC) was added and reacted at 45° C. for 60 min. The amino acid sequence of CGRRAGGSC is shown in SEQ ID NO.1.

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Abstract

The invention discloses a 188 Re-labeled tumor targeting cyclic nonapeptide molecular probe and preparation method thereof, described 188 Re-labeled tumor-targeting cyclic nonapeptide molecular probes including peptides and radionuclides 188 Re, radionuclide 188 Re is connected to the polypeptide through DTPA. In the cyclic nonapeptide molecular probe of the present invention, 188 The serum stability of the Re-labeled cyclic nonapeptide molecule is significantly different from that of the conventional pretinning method, the tumor uptake in tumor-bearing nude mice is significantly increased, and the SPECT imaging effect is more significant. The present invention pre-reduces with cuprous chloride 188 Re, through the action of a weak oxidant after pre-reduction, avoids the direct interaction between the strong reducing agent and the disulfide bond, maintains the stability of the cyclic peptide structure, and effectively avoids the tumor targeting biological function caused by the direct method of destroying the disulfide bond. Reduced, the cyclic nonapeptide labeled by the method of the present invention has higher in vivo and in vitro stability than the direct method.

Description

technical field [0001] The invention relates to the technical field of molecular imaging, in particular to a 188 Re-labeled tumor targeting cyclic nonapeptide molecular probe and its preparation method. Background technique [0002] At present, radionuclide-labeled peptides, as a new class of targeted drugs, have been increasingly used in the diagnosis and treatment of tumors, infections, thrombosis and other diseases. Taking advantage of the specificity, selectivity, saturation, strong affinity and obvious biological effects of the combination of receptors and their ligands, the ligands are used as carriers of radionuclides, and through ligand-receptor targeting mediation, increase The concentration of drugs in the local lesion, the improvement of synergistic effect, and the purpose of targeted therapy are currently one of the most active research frontiers. In the development process of such targeted drugs, the selection and modification of polypeptides are the basis, an...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/08A61K103/10
CPCA61K51/08
Inventor 陈萱陈钰臧嘉周洁杨蕊周彦君唐秋莎陈道桢
Owner WUXI MATERNAL & CHILD HEALTH HOSPITAL