Tumor-targeting novel polypeptide

An alanine and sequence technology, applied in the field of medicine, can solve problems such as inability to achieve therapeutic effects, and achieve the effect of enhancing therapeutic effects

Inactive Publication Date: 2016-02-03
SICHUAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Moreover, the ideal therapeutic effect cannot be

Method used

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  • Tumor-targeting novel polypeptide

Examples

Experimental program
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Effect test

Embodiment 1

[0071] Synthesis of nRGD peptide

[0072] Synthesized by solid-phase synthesis, the sequence is CCRGDK (NAA) GPDC, synthesized by Gil Biochemical (Shanghai) Co., Ltd. outsourcing.

[0073] Results The nRGD peptide was successfully synthesized with a purity of 85%.

Embodiment 2

[0075] Preparation and Characterization of Doxorubicin Liposomes

[0076] Doxorubicin liposomes were prepared by thin film dispersion method and ammonium sulfate gradient method. 56 parts of phospholipids, 34 parts of cholesterol, 8 parts of PEG 2000 -DSPE (purchased from German Lipoid company) and 2 parts of Mal-PEG 2000 -DSPE (PEGylated liposomes without Mal-PEG 2000 -DSPE, that is, the prescription is 56 parts phospholipids, 34 parts cholesterol, 10 parts PEG 2000 -DSPE) (purchased from Lipoid Company, Germany) was dissolved in 5 mL of chloroform. The organic solvent was removed by rotary evaporation, and 123mM ammonium sulfate solution was hydrated. After the probe was sonicated, it was eluted with G75 and incubated with Dox for 8h. After removing unencapsulated doxorubicin, unmodified liposomes containing the Mal end and PEGylated liposomes (PEG-Lipo-Dox) were obtained. The iRGD liposomes (iRGD-Lipo-Dox) and nRGD liposomes were obtained by incubating with the corres...

Embodiment 3

[0081] Efficacy and toxicity evaluation of doxorubicin and its liposome

[0082] Female Balb / c mice were inoculated with 5X10 5 4T1 cells were randomly divided into 7 groups. Normal saline group (N.S), Dox, PEGylated liposome (PEG-Lipo-Dox), iRGD liposome (iRGD-Lipo-Dox), nRGD liposome (nRGD-Lipo-Dox), Dox mixed with nRGD Administration group (Dox+nRGD), PEGylated liposome and nRGD mixed administration group (PEG-Lipo-Dox+nRGD). On the 8th and 12th days, 5 mg / kg Dox equivalent drugs or various preparations were injected. The single administration of the mixed administration group consisted of two injections, one injection was 5 mg / kg Dox equivalent drug or preparation, and the other injection was 4.8 mg / kg nRGD at the same time. Volume and body weight were measured every 2 days. Partial mice were sacrificed at 20 days for mechanism and toxicity studies. Calculate the average tumor inhibition rate after weighing the tumor: TGI=(1-(the average tumor weight of the treatment ...

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Abstract

The invention provides a tumor-targeting novel polypeptide, which is a tandem polypeptide that can target not only tumor cells and blood vessels but also tumor-related macrophages to adjust the tumor microenvironment and enhance the anti-tumor effect. Peptide substrates (AAN) which target tumor blood vessels and tumor cells, contain RGD polypeptides and targeted tumor-related macrophages and are sensitive to aspartic acid endoproteinase are connected to form the polypeptide (nRGD). The polypeptide (nRGD) not only can be applied to be directly used along with drugs or vectors, but also can modify the prodrugs of anti-tumor drugs or modify drug delivery vectors, and can effectively mediate tumor-targeting delivery, thus greatly enhancing curative effect.

Description

technical field [0001] The present invention relates to a novel tumor-targeting polypeptide, in particular to a sequence containing alanine-alanine-asparagine (AAN) linked to an RGD-containing peptide, thereby obtaining a peptide that not only targets tumor cells and blood vessels, but also A tandem polypeptide (nRGD) targeting tumor-associated macrophages to regulate the tumor microenvironment and enhance the anti-tumor effect belongs to the field of medicine. Background technique [0002] There is a special tumor microenvironment at the tumor site, which provides the necessary conditions for tumor development and metastasis, such as maintaining growth-promoting signals, maintaining angiogenesis, resistance to apoptosis and growth-inhibiting signals, and the ability of tumor cells to metastasize and unlimited value-added, genome instability and susceptibility to mutation, reorganization of energy metabolism, inflammation that promotes tumor growth, and evasion of recognitio...

Claims

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Application Information

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IPC IPC(8): C07K5/09C07K5/12A61K47/42A61K47/48A61P35/00
CPCA61K47/42C07K7/50A61P35/00A61K38/12A61K47/64
Inventor 张志荣龚涛宋旭陈体佳符垚孙逊
Owner SICHUAN UNIV
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