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A kind of bivalent targeting polypeptide probe and preparation method thereof
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A technology for targeting polypeptides and probes, which is applied in the field of bivalent targeting polypeptide probes and its preparation, and can solve problems such as weak affinity between polypeptides and target molecules
Active Publication Date: 2021-01-15
INST OF CHEM CHINESE ACAD OF SCI +1
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Problems solved by technology
However, compared with antibodies, the affinity of peptides to target molecules is relatively weak. Therefore, improving the affinity of tumor-targeting peptides is an urgent scientific problem to be solved.
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Embodiment 1
[0065] Embodiment 1, FITC-2PEG 9 -Synthesis of 2AP2H (probe-3)
[0066] The synthesis of the peptide probe is mainly divided into three steps, that is, the synthesis of the backbone core peptide, the synthesis of the branch targeting peptide and the Click reaction under the liquid phase condition.
[0067] The synthesis process is as image 3 shown.
[0068] 1. Synthesis of backbone core peptide
[0069] The peptide KGGKG was synthesized from the C-terminus on the Fmoc-Gly-Wang resin by FMOC solid-phase peptide synthesis, and the amino acids were coupled to the resin one by one, and then Fmoc- PEG 9 -CH 2 -CH 2 -COOH molecule, and then link azidoacetic acid, and couple FITC on the epsilon amino group of C-terminal lysine. The peptide chain is then cleaved from the resin under strong acid, simultaneously removing the remaining side chain protecting groups. The specific experimental steps are as follows:
[0070] Take 100 mg of Fmoc-Gly-Wang resin, swell with DMF for 20...
Embodiment 2
[0078] Example 2. Characterization of the affinity of polypeptide ligands and tumor cells by flow cytometry
[0079] experimental method:
[0080] Prepare EDTA cell digest solution. Weigh 3.639g of EDTA-2Na salt solid, add it to 19.55mL of PBS solution (pH7.4), add an appropriate amount of NaOH to adjust the pH of the buffer solution until EDTA-2Na is completely dissolved, and the pH is about 8.0 at this time, so the EDTA mother solution (concentration is 0.5mol / L). When digesting the cells in the experiment, dilute the EDTA stock solution to 5mmol / L with PBS.
[0081] Digest HepG2 cells with 5 mmol / L EDTA solution for 10 min, pipette the cells to suspend the adherent cells evenly in the digestion solution, centrifuge the cell suspension for 5 min with a centrifuge at 1000 r / min (centrifugal force 180 g), discard the supernatant, Cells were resuspended in PBS and washed 2 times. Finally, the cells were suspended in Hanks dextrose buffer solution (HBSS) containing calcium a...
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Abstract
The invention discloses a divalent targeted polypeptide probe and a preparation method and application thereof. The probe comprises A) two tumor specific targeting polypeptide; B) two PEG linking arms; C) skeleton core peptide and D) fluorescence molecules. Each tumor specific targeting polypeptide is connected with the PEG linking arm via a group as shown in the formula I; the amino acid sequenceof the skeleton core peptide is KGGKG; the skeleton core peptide is coupled to the two tumor specific targeting polypeptide via the PEG linking arms; and the fluorescence molecules are connected to the skeleton core peptide via chemical bonds. According to the multivalent targeted probe FITC-2PEG9-2AP2H, two targeted ligands AP2H are coupled to the skeleton core peptide via PEG chains, the PEG chains can improve the dissolvability of the targeted polypeptide probe in an aqueous solution as well as the flexibility of the probe, and thus, the probe can identify and be combined with a target object.
Description
technical field [0001] The invention relates to a bivalent targeting polypeptide probe and a preparation method thereof. Background technique [0002] Malignant tumors are a serious threat to human life and health. Because their pathogenesis has not been fully elucidated, there have always been problems such as difficulty in early diagnosis, few innovative drugs at the source, and lack of effective treatment methods. Early diagnosis and treatment of malignant tumors can significantly improve patient survival and cure rate. At present, the diagnosis and treatment methods based on the specific recognition principle of antibodies and tumor markers are very effective methods in tumor diagnosis and treatment. Antibodies have the advantages of high affinity and strong specificity. Immunogenicity. Therefore, in recent years, more and more small-molecule targeting ligands, such as peptide ligands and nucleic acid aptamers, have attracted extensive attention from researchers, have ...
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