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Polypeptide for carrying out targeting on mitochondria, and preparation method and application of polypeptide

A mitochondrial and targeted technology, applied in the field of biomedicine, can solve the problems of difficult multi-functional targeted modification and inability to target release of active substances without traces, and achieves a simple synthesis method, convenient multi-functional modification, and good biocompatibility. Effect

Active Publication Date: 2021-11-09
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For this reason, the present invention proposes a mitochondria-targeted polypeptide, which solves the technical problems that the existing mitochondrial-targeted peptides are difficult to carry out multi-functional targeted modification, and the active substances carried cannot be released in the mitochondria without trace targeting

Method used

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  • Polypeptide for carrying out targeting on mitochondria, and preparation method and application of polypeptide
  • Polypeptide for carrying out targeting on mitochondria, and preparation method and application of polypeptide
  • Polypeptide for carrying out targeting on mitochondria, and preparation method and application of polypeptide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Example 1 Preparation of Mitochondria-targeted Polypeptides

[0059] In this example, a kind of polypeptide MTPs targeting mitochondria is prepared, and the specific process is as follows:

[0060] 1. Synthesis of Rink Amide resin

[0061] Tentagel resin (0.26mmol / g, 2g, 1eq) was placed in a peptide solid-phase synthesis tube, DCM was added to swell the resin, shaken gently for 3 minutes, and then the solvent was removed by vacuum filtration; repeated three times. Add DMF to the resin, shake gently for 3 min, and then remove the solvent by vacuum filtration; repeat three times. Rink Amide linker (1.1232g, 4eq) and HATU (0.7904g, 4eq) were dissolved in DMF, then DIEA (0.72mL, 8eq) was added, the mixture was mixed well, the solution was poured into the resin and shaken overnight. After the reaction, the remaining solution was removed by vacuum filtration. Wash 3 times with DMF, DCM, DMF respectively.

[0062] 2. Fmoc solid-phase synthesis method to synthesize mitochon...

Embodiment 2

[0073] Example 2 Preparation of Mitochondria-targeted Polypeptides of Different Structures

[0074] In this example, mitochondria-targeted polypeptides with different structures were prepared. The structures are shown in Table 1. The preparation method is shown in Example 1. By designing sequences 1 (intermediate pentapeptide), 2 (MTP2), 3 (MTP3 ), 4 (MTP4), 5 (MTP5), by changing the number of arginine in the sequence to explore its impact on mitochondrial localization. Mitochondrial targeting peptides with different structures were characterized by LC-MS (results such as Figure 1-4 shown).

[0075] Table 1

[0076]

[0077] Characterization experiment results such as Figure 1-4 As shown, among them, Figure 1-4 They are the LC-MS characterization results of polypeptides MTP2, MTP3, MTP4, and MTP5 respectively. It can be seen from the figure that pure MTPs are prepared through the scheme of the present invention.

Embodiment 3

[0078] Example 3 Synthesis of Mitochondria Targeted Fluorescent Probes

[0079] Mitochondria-targeted fluorescent probes were synthesized with mitochondria-targeted polypeptides and used as carriers to deliver different types of fluorescent groups.

[0080] 1. Synthesize mitochondrial targeting fluorescent probes 8-12, the synthesis steps are as follows:

[0081] The synthesized mitochondria-targeted polypeptide 1, MTP2, MTP3, MTP4, MTP5 (6×10 -3 mmol, 1eq) were dissolved in DMF respectively. 1-pyrenebutyric acid (18×10 -3 mmol, 3eq) was dissolved in DMF, with HOBt (18 × 10 -3 mmol, 3eq), HBTU (18×10 -3 mmol, 3eq) and TEA (36×10 -3mmol, 6eq) for preactivation. The pre-activated solution was mixed with the mitochondria-targeted peptide solution, then stirred overnight at room temperature, and the resulting crude sample was purified by preparative high-performance liquid chromatography. Characterized by LC-MS analysis, the characterization results are as follows Figure ...

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Abstract

The invention discloses a polypeptide for carrying out targeting on mitochondria, and a preparation method and application of the polypeptide. The polypeptide is briefly recorded as MTPs. The polypeptide, which is prepared by the scheme of the invention, for carrying out the targeting on the mitochondria has a simple in synthesis method, and the obtained polypeptide can specifically carry out targeting on the cell mitochondria, is almost non-toxic to cells, has good cell membrane penetration characteristics, can be conveniently subjected to further multifunctional derivative modification, and provides a potential delivery tool for preparation of mitochondrial targeting drugs.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a mitochondria-targeting polypeptide and its preparation method and application. Background technique [0002] Cancer (malignant tumor) has become a major disease that seriously endangers human health, and has brought enormous pressure to people's lives and economic and social development. Although tremendous progress has been made in the prevention, detection, and treatment of cancer, there are currently no effective therapies for treating tumors. A long-standing problem in cancer chemotherapy is the non-specific distribution of therapeutic drugs and lack of tumor selectivity, which can lead to systemic toxicity and other serious side effects during treatment, such as alopecia, anemia, kidney, liver and bone marrow damage, etc. Therefore, it is of great significance to develop an effective anticancer drug delivery system to distinguish cancer cells from normal cells, so a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/64C07K7/06C07K19/00A61K49/00A61K31/704A61P35/00
CPCA61K47/64C07K7/06A61K49/0056A61K31/704A61P35/00C07K2319/10C07K2319/00Y02P20/55A61K31/4745A61K38/00A61K47/551A61K47/645A61K49/0021A61K49/0041A61K47/62A61K47/545A61K47/549
Inventor 肖奇才高理钱周士哲
Owner SUN YAT SEN UNIV
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