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68Ga-NODAGA-cyclic polypeptide FG01 targeting EphA2 receptor as well as preparation method and application of 68Ga-NODAGA-cyclic polypeptide FG01

A 68ga-nodaga-, cyclic polypeptide technology, applied in the field of biomedicine, can solve the problems of not being able to know the treatment effect in time, not suitable for clinical examination of patients with hyperglycemia, and not being able to see changes in blood vessels and lymphatic vessels, etc.

Active Publication Date: 2022-04-01
QILU UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

first, 18 F-FDG can only evaluate the changes in tumor size and metabolism, but cannot see the changes in the blood vessels and lymphatic vessels inside the tumor. It is often necessary to evaluate whether the treatment is effective after a few months of treatment when the shape of the tumor changes. Therefore, Unable to understand the effects of treatment in a timely manner
Second, due to 18 F-FDG is based on the principle of glucose metabolism, so it is not suitable for clinical examination of patients with hyperglycemia

Method used

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  • 68Ga-NODAGA-cyclic polypeptide FG01 targeting EphA2 receptor as well as preparation method and application of 68Ga-NODAGA-cyclic polypeptide FG01
  • 68Ga-NODAGA-cyclic polypeptide FG01 targeting EphA2 receptor as well as preparation method and application of 68Ga-NODAGA-cyclic polypeptide FG01
  • 68Ga-NODAGA-cyclic polypeptide FG01 targeting EphA2 receptor as well as preparation method and application of 68Ga-NODAGA-cyclic polypeptide FG01

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] A targeting EphA2 receptor 68 The preparation method of Ga-NODAGA-cyclic polypeptide FG01, the specific steps are as follows:

[0055] (1) Adopt the Fmoc scheme, select Wang resin, connect the serine with the tBu protecting group at the carboxyl end of the cyclic polypeptide to the Wang resin, remove the Fmoc protecting group, and use the serine bound on the Wang resin as the starting point for synthesis According to the amino acid sequence MMPVSDPYK from the carboxy-terminus to the amino-terminus, the condensation reaction is carried out successively to form peptide bonds, in which amino acids S, D, Y, and K are all amino acids with protective groups, which are removed from Fmoc protection, condensed to form peptide bonds, and repeated This step is repeated until all the sequences are coupled completely, and the polypeptide is cleaved from the Wang resin and removed from Fmoc protection to obtain a polypeptide sequence with protective groups for amino acids S, D, Y, an...

Embodiment 2

[0071] Example 2 targeting the EphA2 receptor 68 In Vitro Radiochemical Properties of Ga-NODAGA-Cyclic Polypeptide FG01

[0072] In vitro stability: 20 μL of the prepared Example 1 68 Ga-NODAGA-cyclic polypeptide FG01 was added to 180 μL of PBS buffer with pH=7.4, incubated at 37°C for 15min, 30min, 1h, 2h, and 4h, and then 20μL of the mixture was taken out and injected into radioactive HPLC for detection. The results are as follows: Figure 4 shown.

[0073] Depend on Figure 4 known in vitro 68 The radiochemical purity of Ga-NODAGA-cyclic polypeptide FG01 has no significant change and is above 95%, and has good in vitro stability within 4 hours.

[0074] Hydrophilic and lipophilic: prepared in Example 1 of 0.15MBq 68 Ga-NODAGA-cyclic polypeptide FG01 was diluted to 500 μL with HEPES buffer at pH=7.4, and then 500 μL of n-octanol was added and shaken vigorously. Take an equal amount of liquid from each of the aqueous and organic phases to measure their radioactive count...

Embodiment 3

[0078] Example 3 Targeting the EphA2 receptor 68 Cell growth inhibition and cellular uptake of Ga-NODAGA-cyclic polypeptide FG01

[0079] Cell culture: in 5% CO 2 , non-small cell lung cancer cells (A549 and NCI-H1299) were cultured in RPMI 1640 medium containing 10% calf serum in a 37°C cell culture incubator.

[0080] MTT experiment: 10 μL of the cyclic polypeptide FG01 prepared in Example 1 with a concentration of 0.039, 0.195, 0.976, 4.88, 24.4, and 122 μM was added to non-small cell lung cancer cells (A549 and NCI-H1299) containing 90 μL of culture solution, In different time periods (5, 24, 48 and 72h), the effect of the cyclic polypeptide FG01 on cell growth was observed, and the results are shown in Figure 5, Image 6 shown.

[0081] Depend on Figure 5 with Image 6 It can be seen that the cyclic polypeptide FG01 has no significant effect on the growth of non-small cell lung cancer, indicating that the cyclic polypeptide FG01 has no cytotoxicity.

[0082] Cell u...

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Abstract

The invention relates to 68Ga-NODAGA-cyclic polypeptide FG01 of a targeted EphA2 receptor as well as a preparation method and application of the 68Ga-NODAGA-cyclic polypeptide FG01. The 68Ga-NODAGA-cyclic polypeptide FG01 forms an amido bond through an amino group of lysine in an amino acid sequence and a carboxyl group of serine, then an amino group at an amino terminal of the cyclic polypeptide FG01 and a coupling agent NODAGA-NHS are subjected to a condensation reaction, a chelating agent NODAGA in the cyclic polypeptide conjugate NODAGA-FG01 is chelated with 68Ga, and the 68Ga-labeled cyclic polypeptide conjugate is constructed. The invention verifies that the annular polypeptide FG01 has no obvious inhibition effect on tumor cells, indicates that the annular polypeptide FG01 has no cytotoxicity, and finds that the 68Ga-NODAGA-annular polypeptide FG01 of a targeted EphA2 receptor can be used for in-vivo imaging of EphA2 high-expression tumors, realizes molecular imaging of the EphA2 high-expression tumors such as non-small cell lung cancer by utilizing PET (Polyethylene Terephthalate), and is widely used as a tumor molecular imaging agent.

Description

technical field [0001] The present invention relates to a kind of targeting EphA2 receptor 68 The Ga-NODAGA-cyclic polypeptide FG01 and its preparation method and application belong to the technical field of biomedicine. Background technique [0002] With the progress of research, small molecule peptide-targeted diagnostic agents have attracted more and more attention, and more and more targeted small molecule peptides are being continuously developed, such as RGD peptide, APN peptide, BBN peptide , Octreotide, etc. Among them, octreotide and RGD peptide are the most widely studied. [0003] PET examination (Positron Emission Imaging Technology) is the most advanced diagnostic technology emerging in recent years. Compared with traditional SPECT examination (Chinese name is single photon emission computed tomography), it has high spatial resolution, high definition, high It is sensitive and can reflect the energy metabolism of cells or the expression of cell molecules. Com...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/64C07K1/16C07K1/13C07K1/06C07K1/04A61K51/08A61K103/00
CPCY02P20/55
Inventor 高峰肖加奇
Owner QILU UNIV OF TECH
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