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A Peptide Modified Segment and Its Application in the Modification of Peptide Molecular Imaging Probes

A molecular probe, peptide modification technology, applied in the direction of peptides, radioactive carriers, etc., can solve the problems of difficult industrial production and unsatisfactory effects, and achieve the effect of increasing contrast, suitable for large-scale production, and optimizing imaging quality.

Inactive Publication Date: 2011-12-14
JIANGSU INST OF NUCLEAR MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, for peptide molecular imaging probes with poor hydrophilicity, the effect of these two technical modifications is not ideal, and it is not easy to carry out industrial production

Method used

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  • A Peptide Modified Segment and Its Application in the Modification of Peptide Molecular Imaging Probes
  • A Peptide Modified Segment and Its Application in the Modification of Peptide Molecular Imaging Probes
  • A Peptide Modified Segment and Its Application in the Modification of Peptide Molecular Imaging Probes

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Embodiment 1

[0029] Experimental principle:

[0030] Take the bombesin polypeptide derivative whose target is the gastrin-releasing peptide receptor as an example. The sequence is D-Phe-Gln-Trp-Ala-Val-Gly-His-Leu-NHCH 2 CH 3 Peptides with gastrin-releasing peptide receptor targeting, can be combined with positron nuclides (such as 18 F, 68 Ga) labeling precursor 18 F-2-Fluorophenylpropionic acid, prepared by the reaction of chelating agent DOTA 18 F, 68 Ga-labeled peptide molecular imaging probes 1 and 3 were used for PET imaging, or reacted with near-infrared fluorescence imaging nuclide cy5.5 to prepare cy5.5-labeled peptide molecular imaging probe 5 for optical imaging. Peptide Molecules Imaging probes 1, 3, and 5 have poor imaging effects, and they can be modified by inserting the peptide-modified segment Gly-Gly-Gly-Arg-Asp-Asn into D-Phe-Gln-Trp-Ala-Val- Gly-His-Leu-NHCH 2 CH 3 and imaging part 18 Modified peptide molecular imaging probes prepared between F-2-fluorophenylp...

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Abstract

The invention discloses a peptide modified segment, the structural formula is as follows: (L)m-(A)n-(S)o, wherein L is a connecting segment, m is 0-10; A is a PN or NP amino acid pair , n is 1-10; S is a spacer segment, and o is 0-10. The beneficial effects of the present invention are: the peptide modified segment provided by the present invention and its application in the modification of peptide molecular imaging probes can significantly improve the pharmacokinetic properties of targeting peptides, increase the tumor uptake value and tumor The contrast with the background optimizes the image quality. The target peptide product can be conveniently prepared by using an automatic peptide synthesizer through Fmoc protection chemistry, which is suitable for large-scale production.

Description

technical field [0001] The invention relates to a peptide modified chain segment and its application, in particular to a peptide modified chain segment and its application in the modification of peptide molecular image probes. Background technique [0002] Positron emission tomography (PET) is a cutting-edge technology for biomedical research and clinical diagnosis in the 21st century. Insight into the activities of labeled drugs in normal or sick people is of great importance in the field of molecular imaging research. Compared with conventional B-ultrasound, CT, MR and other anatomical imaging methods, it can provide early functional and metabolic information; compared with SPECT, PET has high resolution and can be quantitatively analyzed, which has obvious advantages. Most of the molecular imaging probes used in PET are endogenous metabolites or analogs of human body. Nuclides for PET imaging are often essential elements in the body, such as 18 F can replace the H atom...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K2/00A61K51/08A61K101/00A61K101/02A61K103/00A61K103/10
Inventor 杨敏严勇军陈小元
Owner JIANGSU INST OF NUCLEAR MEDICINE
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