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Polypeptide molecule exerting selective killing and migration inhibiting effect on cancer cells, and design method and application thereof

A technology of inhibition and migration inhibition, applied in chemical instruments and methods, peptide/protein components, medical preparations containing active ingredients, etc., can solve the problems of high toxicity and side effects, poor selectivity of cancer cells, etc., and achieve strong selective killing The effect of action

Active Publication Date: 2016-04-27
SOUTHWEST JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the vast majority of anti-cancer chemotherapy drugs have limitations such as poor selectivity of cancer cells and high toxicity and side effects. Targeted drug research targeting tumor-related and overexpressed proteins is an important direction for the development of anti-cancer drugs

Method used

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  • Polypeptide molecule exerting selective killing and migration inhibiting effect on cancer cells, and design method and application thereof
  • Polypeptide molecule exerting selective killing and migration inhibiting effect on cancer cells, and design method and application thereof
  • Polypeptide molecule exerting selective killing and migration inhibiting effect on cancer cells, and design method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1. Design and synthesis of polypeptide molecules

[0031]1. Design and synthesis of 9R-P201 polypeptide

[0032] In view of the fact that P201 is a DNA-binding domain protein molecularly targeted to FoxM1c, the polypeptide sequence obtained by screening the phage random peptide library, and FoxM1c is a transcription factor in the nucleus, P201 must enter the cell (nucleus) to exert its inhibitory effect on FoxM1c, a An effective way is to enhance the membrane-penetrating ability of the polypeptide by adding the N-terminal of the cell penetrating peptide (cellpenetratingpeptide), and the addition of polyarginine is an effective way to achieve this purpose. For this reason, on the basis of the amino acid sequence of the P201 polypeptide, the cell-penetrating peptide of 9R (9 poly D-type arginine, RRRRRRRR) is added at the N-terminus of the P201 polypeptide to improve the membrane-penetrating ability of the polypeptide and add (GS ) 2 Dimerization of glycine and ...

Embodiment 2

[0066] Example 2. The Killing Effect of Polypeptide 9R-P201 on Cancer Cell Lines

[0067] 1. The killing effect of 9R-P201 on liver cancer cells HepG2 was detected by culturing CCK-8 with complete serum

[0068] (1) Experimental method

[0069] Cell culture: HepG2 liver cancer cells were resuscitated and cultured according to routine cells, and the complete medium was DMEM+10% fetal bovine serum+100 U / ml penicillin and 100 μg / ml streptomycin. 37°C, 5% CO 2 Incubate the cultures in the incubator.

[0070] Cell treatment: complete medium by 6 × 10 3 The number of cells / well was plated on a 96-well cell culture plate, and 9R-P201 polypeptides with equal concentrations of 10, 20, 40, 60, 80, and 100 μg / mL prepared in complete medium were added after 24 hours, and photographs were taken at each time point of 12 and 24 hours. Check cell viability.

[0071] CCK-8 cell viability assay: continue to culture the above 96-well cell culture plate to the corresponding time point, add 1...

Embodiment 3

[0094] Example 3: CCK-8 detects the effect of 9R-P201 on human normal cell lines

[0095] 1. The effect of 9R-P201 on human umbilical vein endothelial cells HUVEC was detected by complete medium CCK-8

[0096] (1) Experimental method:

[0097] Cell culture: same as embodiment 2-1.

[0098] Cell treatment: similar to Example 2-1, the difference is that 9R-P201 polypeptide at different concentrations of 10, 20, 40, 60, 80, 100, 120 μg / mL prepared in complete serum medium was added to each well after cell culture for 24 hours , 24h photography and detection of cell morphology changes and cell viability.

[0099] Determination of CCK-8 activity: same as Example 2-1.

[0100] (2) Experimental results

[0101] For the changes in cell morphology and cell viability, see the appendix Figure 4 , it can be seen that under the condition of complete serum medium, with the increase of cell culture time and polypeptide treatment, the survival rate of HUVEC gradually decreased, and the ...

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Abstract

The invention discloses a polypeptide molecule exerting selective killing and migration inhibiting effect on cancer cells, and a design method and application thereof, belonging to the technical field of application of biopharmacy. The polypeptide molecule comprises a polypeptide amino acid sequence and constituent (SEQ ID No. 1) and contains altogether 12 amino acids. Through 9R or 8R coupling reconstruction and designing, the polypeptide molecule has strong killing effect on malignant cells of human liver cancer, prostatic cancer, breast cancer and the like and low killing effect on normal human hepatic cells, embryonic kidney cells and umbilical vein endothelial cells; in particular, the polypeptide molecule has strong selective killing effect on liver cancer cells and inhibitory effect on migration of human liver cancer and umbilical vein endothelial cells compared with normal human hepatic cells. The polypeptide molecule is mainly applied to preparation of drugs used for selective killing and migration inhibiting of malignant cells of human liver cancer.

Description

technical field [0001] The invention belongs to the application field of biotechnology and pharmacy. In particular, it relates to the technical field of polypeptide molecules as lead drug molecules. Background technique [0002] Cancer seriously endangers human life and health. There are about 13 million new cancer patients every year in the world. According to the "2012 China Tumor Registration Annual Report" released by my country Tumor Registry Center, there are about 3.12 million new cancer cases in China every year, and cancer deaths The number of cases reached 2.7 million, and malignant tumors including liver cancer have become the number one killer of human disease deaths. The research and development of anticancer drugs has become the research focus of medical and life science workers. [0003] At present, the vast majority of anti-cancer chemotherapy drugs have limitations such as poor selectivity for cancer cells and high toxicity and side effects. Targeted drug r...

Claims

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Application Information

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IPC IPC(8): C07K14/47A61K38/17A61P35/00
CPCA61K38/00C07K14/47
Inventor 茆灿泉崔健邬怡然毕振飞黄家明郭泰林
Owner SOUTHWEST JIAOTONG UNIV
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