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A kind of dar2 polypeptide radiopharmaceutical and preparation method thereof

A technology of radiopharmaceuticals and radionuclides, applied in the field of Dar polypeptide-based radiopharmaceuticals and its preparation, can solve instability and other problems, and achieve the effect of increasing intake and improving metabolic stability

Active Publication Date: 2021-03-19
INSITUTE OF BIOPHYSICS CHINESE ACADEMY OF SCIENCES +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in vivo metabolic stability experiments showed that the radionuclide-labeled cKiE dimer peptide probe 99m Tc-HYNIC-(GGG-cKiE) 2 There is a problem that the body is partially decomposed and unstable

Method used

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  • A kind of dar2 polypeptide radiopharmaceutical and preparation method thereof
  • A kind of dar2 polypeptide radiopharmaceutical and preparation method thereof
  • A kind of dar2 polypeptide radiopharmaceutical and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0051] This embodiment takes the in vitro specificity and affinity determination of the Dar2 polypeptide (ie Dar polypeptide dimer) as an example.

[0052]Fluorescence staining of Cy5.5-Dar2 in HepG2 cells and tumor tissue sections: Fluorescein Cy5.5 was coupled with Dar2 polypeptide to synthesize Cy5.5-Dar2. When Cy5.5-Dar2 was incubated with HepG2 cells and tumor tissue slices, obvious fluorescent signals could be seen on the cell membranes of HepG2 cells and tumor tissue slices. In the blocking experiment, the fluorescent signals were significantly decreased ( figure 2 ), indicating that the Dar2 polypeptide can specifically interact with integrin α 6 combined.

[0053] In vitro affinity determination of Dar2 polypeptide: Biotin is coupled with Dar2 polypeptide to synthesize Biotin-Dar2. Different concentrations of Biotin-Dar2 and human integrin α 6 beta 4 Protein binding, detection of Biotin-Dar2 and human integrin α 6 beta 4 protein binding affinity K d The value ...

Embodiment 99

[0055] This embodiment takes 99m Tc-HYNIC-PEG 4 -(GGG-Dar) 2 Polypeptide radiopharmaceuticals and their preparation methods are taken as examples.

[0056] 99m Tc-HYNIC-PEG 4 -(GGG-Dar) 2 Among them, the Dar polypeptide monomer is a D-type polypeptide anedywr, and the Dar polypeptide dimer is a Dar polypeptide dimer formed by linking the linker GGG with the Dar polypeptide monomer, and then dimerizing two Dar polypeptide monomers connected with GGG. polymers, radionuclides 99m Tc marks the Dar polypeptide dimer through a bifunctional chelating agent HYNIC, and a pharmacokinetic modification molecule PEG is also connected between the Dar polypeptide dimer and the bifunctional chelating agent HYNIC 4 , the Dar2 polypeptide radiopharmaceutical is 99m Tc-HYNIC-PEG 4 -(GGG-Dar) 2 , the Dar2 polypeptide radiopharmaceutical is a colorless transparent liquid injection.

[0057] 99m Tc-HYNIC-PEG 4 -(GGG-Dar) 2 The preparation method is as follows:

[0058] HYNIC-PEG 4 Pr...

Embodiment 3

[0070] This embodiment takes 99m Tc-HYNIC-Aoc-(GGG-Dar) 2 Polypeptide radiopharmaceuticals and their preparation methods are taken as examples.

[0071] 99m Tc-HYNIC-Aoc-(GGG-Dar) 2 Among them, the Dar polypeptide monomer is a D-type polypeptide anedywr, and the Dar polypeptide dimer is a Dar polypeptide dimer formed by linking the linker GGG with the Dar polypeptide monomer, and then dimerizing two Dar polypeptide monomers connected with GGG. polymers, radionuclides 99m Tc marks the Dar polypeptide dimer through a bifunctional chelating agent HYNIC, and a pharmacokinetic modification molecule Aoc is also connected between the Dar polypeptide dimer and the bifunctional chelating agent, and the Dar2 polypeptide radiopharmaceutical is 99m Tc-HYNIC-Aoc-(GGG-Dar) 2 , the Dar2 polypeptide radiopharmaceutical is a colorless transparent liquid injection.

[0072] 99m Tc-HYNIC-Aoc-(GGG-Dar) 2 The preparation method is as follows:

[0073] Preparation of HYNIC-Aoc-COOH: Dissol...

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Abstract

The invention discloses a Dar2 polypeptide radioactive drug and a preparation method thereof. The drug comprises a Dar polypeptide dimer and a radioactive nuclide, wherein the radioactive nuclide canmark the Dar polypeptide dimer through a bifunctional chelating agent; the Dar polypeptide dimer is a polypeptide dimer which is synthesized through the steps of enabling GGG to be connected with twoDar polypeptide monomers and performing dimerization on the two Dar polypeptide monomers connected to the GGG; and each Dar polypeptide monomer is D type amino acid linear heptatomic polypeptide, andthe sequence is anedywr. According to the drug disclosed by the invention, the radioactive nuclide is marked on Dar polypeptide dimer molecules through the bifunctional chelating agent, the in vivo marked drug is concentrated to tumor positions through the targeting effects of Dar polypeptide, and through a single-photon emission computed tomography (SPECT) technique or a positron emission computed tomography (PET) technique of nuclear medicine, tomography diagnosis is performed on integrin alpha 6 positive tumor.

Description

technical field [0001] The invention relates to the technical field of radiopharmaceuticals, in particular to a novel Dar polypeptide-based radiopharmaceutical and a preparation method thereof. Background technique [0002] The integrin family is a class of heterodimeric transmembrane glycoproteins formed by non-covalent bonding of α and β subunits. Eighteen α subunits and eight β subunits have been found in mammals so far. These subunits can combine to form 24 integrins. Different combinations of subunits lead to different distribution and physiological functions of integrins. An integrin can have multiple ligands, and a ligand can bind to multiple receptors. Integrins usually participate in intracellular and extracellular signal transduction to regulate various important cellular functions, such as adhesion, polarity, differentiation, migration and cell division. Integrin alpha 6 As a member of the integrin family, major and β 1 or beta 4 The subunits combine to for...

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 王凡史继云罗麒贾兵
Owner INSITUTE OF BIOPHYSICS CHINESE ACADEMY OF SCIENCES
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