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Brain tumor targeting polypeptide and derivative and application thereof

A technology of peptide derivatives and brain tumors, applied in the field of medical biology, can solve the problems of slow research progress, lack of candidate ligands, and limited selection, and achieve the effects of broad application prospects, easy synthesis and modification, and low cost

Pending Publication Date: 2022-04-12
SHENZHEN INST OF ADVANCED TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as of now, the selection of relevant mediator ligands that can both cross the blood-brain barrier and target tumor lesions is very limited.
Compared with the huge clinical needs, the progress of research in this area is still very slow, and the available candidate ligands are also lacking

Method used

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  • Brain tumor targeting polypeptide and derivative and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Embodiment 1: Preparation of polypeptide sequence

[0049] Synthesize the polypeptide sequence across the blood-brain barrier by artificial synthesis method,

[0050] The polypeptide sequence is as follows:

[0051] YLGASVPSPDPLEPT SEQ ID No. 1;

[0052] YLGASVPSPDPLEPTREQCELNPACDELSDQYGLKTAYKRIYGITI SEQ ID No. 2;

[0053] YLYQWLGAPVPYPDPLEPR SEQ ID No. 3;

[0054] YLYQWLGAPVPYPDPLEPREVCELNPDCDELADHIGFQEAYRRFYGPV SEQ ID No. 4.

[0055] The above-mentioned polypeptides are synthesized by conventional solid-phase synthesis or liquid-phase synthesis methods. Among them, the solid-phase synthetic peptide method is used to react from the amino acid at the C-terminal to the N-terminal. After the steps of resin activation, amino acid linkage, elution protection, and detection, the amino acid linkage is completed one by one, and then precipitated and centrifuged with excess ether, and the crude peptide is purified by HPLC. Afterwards, mass spectrometry was performed, and f...

Embodiment 2

[0057] Embodiment 2: the preparation of polypeptide probe

[0058] This embodiment provides a polypeptide probe, using the polypeptide prepared in Example 1, and combining it with ICG through an organic chemical reaction.

[0059] The specific method is purchase or synthesis. In this example, the probe is prepared by linking the polypeptide with ICG by click chemistry method, and the linker is the universal DBCO. ICG with an activating functional group containing the amino group NH 2 , carboxyl COOH, activated lipid NHS, maleimide MAL, mercapto SH, azide N 3 , alkyne ALK, and then coupled with the polypeptide prepared in Example 1 to obtain the blood-brain barrier polypeptide ICG probe.

Embodiment 3

[0060] Example 3: Modeling of brain tumor mice and detection of targeting ability

[0061] Using an adult mouse, human U87 glioma was transplanted to the cerebral cortex of the mouse through a brain locator, and after 3 days, the polypeptide ICG probe prepared in Example 2 (containing SEQ ID NO.1), Scrambled peptide probe, ICG solution (2mM) and PBS were injected into each mouse in 100 microliters, and after 24 hours, detected under the small animal imager.

[0062] See the experimental results figure 1 , by comparing the results of the 4 groups, it can be known that the peptide probe group (group A) has a specific signal at the brain tumor site, while the other three groups (group S: scrambled polypeptide probe; group N: ICG solution group; PBS group) have no signal. Shows fluorescent signal in the brain. The above experimental results show that the polypeptide probe of the present invention can achieve the effect of targeting brain tumors across the blood-brain barrier.

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Abstract

The invention discloses a brain tumor targeting polypeptide as well as a derivative and application thereof, and belongs to the field of biological medicines. The invention specifically discloses application of polypeptide in preparation of brain tumor targeted drugs or detection reagents. The polypeptide is selected from metabonotin or osteocalcin. The invention also discloses a derivative, and the derivative is a product obtained by modifying the tail end or the side chain of polypeptide. The polypeptide molecule can cross a blood brain barrier to enter a brain tissue and be combined in a brain tumor area, and a specific targeted delivery means is provided for diagnosis and treatment of brain tumor diseases.

Description

technical field [0001] The invention belongs to the field of medical biology, and relates to a polypeptide targeting brain tumors, derivatives and applications thereof. Background technique [0002] In the diagnosis and treatment of brain tumors, due to the existence of the blood-brain barrier, the corresponding drugs are greatly consumed in the process of systemic administration, and the drugs that can reach the brain tumor site are very limited, which affects the diagnosis and treatment of brain tumors. Therefore, it is very valuable to find tool molecules that can mediate drug targeting to tumor lesions. However, up to now, the selection of related mediator ligands that can cross the blood-brain barrier and target tumor lesions is still very limited. Compared with the huge clinical needs, the progress of research in this area is still very slow, and the available candidate ligands are also lacking. Contents of the invention [0003] With regard to the bottleneck probl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/64A61K45/00A61P35/00A61K49/00A61K51/08C07K14/575C07K14/47
CPCA61K45/00A61K47/64A61K49/00A61K51/08A61P35/00C07K14/47C07K14/575
Inventor 赵华山朱雯张键张鹏飞
Owner SHENZHEN INST OF ADVANCED TECH
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