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Anti-tumor polypeptide, preparation method and anti-tumor applications thereof

An anti-tumor, polypeptide sequence technology, applied in the field of anti-tumor applications, can solve the problems of insensitivity, residue, drug resistance, etc., and achieve the effect of easy and accurate quantification and enhanced targeting

Inactive Publication Date: 2013-02-13
HARBIN PHARMA GROUP TECH CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Tumor is a multi-gene and multi-factor disease. Traditional tumor treatment includes surgery, chemotherapy, radiotherapy, etc., mainly targeting tumor cells directly. There are postoperative residues, drug delivery and penetration problems, and chemotherapy, radiotherapy Disadvantages such as insensitivity and drug resistance

Method used

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  • Anti-tumor polypeptide, preparation method and anti-tumor applications thereof
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  • Anti-tumor polypeptide, preparation method and anti-tumor applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] 1 The chemical synthesis of the preferred polypeptide sequence SEQ ID NO: 4 of the present invention

[0032] (1) Swell Fmoc-Asp(OtBu)-Wang with DMF for 30 minutes, remove DMF, add 20% PIP / DMF solution, stir for 5 minutes, wash with DMF, and wash twice.

[0033] (2) Add 20% PIP / DMF solution, stir and react for 25 minutes, wash with DMF twice, and the ninhydrin test should be positive.

[0034] (3) Weighing Fmoc-Gly-OH (3-5 times the number of moles of amino groups contained in the resin) and equimolar 1-hydroxy-benzo-triazole (HOBt) were dissolved in DMF and cooled in an ice bath for 30 min; Take equimolar DIC, dilute it twice with DCM, pre-cool in a water bath at 0°C to -10°C, add the cooled DIC solution to the DMF solution of Fmoc-Gly-OH, continue cooling and stirring for more than 60 minutes, add to Condensation reaction was carried out in the reaction column, and after the reaction (no color detected by ninhydrin chromogenic method) was washed with DMF for 3 times ...

Embodiment 2

[0045] 1 Chemical synthesis of the preferred polypeptide sequence SEQ ID NO: 5 of the present invention

[0046] (1) Swell Fmoc-Asp(OtBu)-Wang with DMF for 30 minutes, remove DMF, add 20% PIP / DMF solution, stir for 5 minutes, wash with DMF, and wash twice.

[0047] (2) Add 20% PIP / DMF solution, stir and react for 25 minutes, wash with DMF twice, and the ninhydrin test should be positive.

[0048] (3) Weighing Fmoc-Gly-OH (3-5 times the number of moles of amino groups contained in the resin) and equimolar 1-hydroxy-benzo-triazole (HOBt) were dissolved in DMF and cooled in an ice bath for 30 min; Take equimolar DIC, dilute it twice with DCM, pre-cool in a water bath at 0°C to -10°C, add the cooled DIC solution to the DMF solution of Fmoc-Gly-OH, continue cooling and stirring for more than 60 minutes, add to Condensation reaction was carried out in the reaction column, and after the reaction (no color detected by ninhydrin chromogenic method) was washed with DMF for 3 times to c...

Embodiment 3

[0059] 1 Chemical synthesis of the preferred polypeptide sequence SEQ ID NO: 6 of the present invention

[0060] (1) Swell Fmoc-Asp(OtBu)-Wang with DMF for 30 minutes, remove DMF, add 20% PIP / DMF solution, stir for 5 minutes, wash with DMF, and wash twice.

[0061] (2) Add 20% PIP / DMF solution, stir and react for 25 minutes, wash with DMF twice, and the ninhydrin test should be positive.

[0062] (3) Weighing Fmoc-Gly-OH (3-5 times the number of moles of amino groups contained in the resin) and equimolar 1-hydroxy-benzo-triazole (HOBt) were dissolved in DMF and cooled in an ice bath for 30 min; Take equimolar DIC, dilute it twice with DCM, pre-cool in a water bath at 0°C to -10°C, add the cooled DIC solution to the DMF solution of Fmoc-Gly-OH, continue cooling and stirring for more than 60 minutes, add to Condensation reaction was carried out in the reaction column, and after the reaction (no color detected by ninhydrin chromogenic method) was washed with DMF for 3 times to c...

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Abstract

The invention relates to an anti-tumor polypeptide, a preparation method and anti-tumor applications thereof. A purpose of the present invention is to provide a polypeptide having an anti-tumor function and a preparation method thereof. A structure of the polypeptide comprises three histidine structures containing an endostatin N-terminal zinc ion binding site, a beta-pleated sheet structure and a serial RGD sequence. According to the invention, a chemical synthesis method for the polypeptide drug is disclosed, and a tumor proliferation inhibition effect of the polypeptide is proved.

Description

technical field [0001] The invention relates to polypeptide drugs in the field of biotechnology and pharmacy, its preparation method and anti-tumor application. Background technique [0002] Tumor is a multi-gene and multi-factor disease. Traditional tumor treatment includes surgery, chemotherapy, radiotherapy, etc., mainly targeting tumor cells directly. There are postoperative residues, drug delivery and penetration problems, and chemotherapy, radiotherapy Insensitivity, drug resistance and other shortcomings. The growth of tumors is dependent on blood vessels. When the tumor diameter is less than or equal to 2mm, tumor cells absorb nutrients through diffusion, which is called "pre-vascular"; when the tumor grows further, new capillaries are needed to provide nutrients, which is called For the "vascular phase". Angiogenesis is closely related to the occurrence, development and metastasis of tumors. Therefore, in the early 1970s, Folkman proposed anti-angiotherapy therapy...

Claims

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Application Information

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IPC IPC(8): C07K14/00C07K1/06C07K1/04C07K1/02C07K1/20A61K38/16A61P35/00
Inventor 王莹李郑武姜媛媛孙磊徐岩李国军刘贺煜黄岩李会成陈玉军张秀芹黄宇红王丽娜李曲亮高晶曹翊婕刘宇庭
Owner HARBIN PHARMA GROUP TECH CENT
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