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Integrin blocking agent AP-25 expressed by modification of polyethylene glycol and protein fusion and its application

An integrin blocker, AP-25 technology, applied to peptide/protein components, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as cumbersome process and difficulty in industrialization

Inactive Publication Date: 2014-05-28
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Fusion expression also has some shortcomings, such as cumbersome process and not easy to industrialize, etc.

Method used

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  • Integrin blocking agent AP-25 expressed by modification of polyethylene glycol and protein fusion and its application
  • Integrin blocking agent AP-25 expressed by modification of polyethylene glycol and protein fusion and its application
  • Integrin blocking agent AP-25 expressed by modification of polyethylene glycol and protein fusion and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Example 1 Integrin blocking agent AP-25

[0084] Ala-Cys-Asp-Cys-Arg-Gly-Asp-Cys-Phe-Cys-Gly-Gly-Gly-Gly-Ile-Val-Arg-Arg-Ala-Asp-Arg-Ala-Ala-Val-Pro Solid-phase synthesis method, which uses Fmoc-Pro-2Cl resin as the starting material, and then uses protected amino acids to connect dipeptides to pentapentapeptides sequentially. After the peptide connection is completed, it is fully washed, and then peptides are cut and post-treated to obtain AP- 25 crude. Purify the crude product by first dissolving it, then using preparative high-performance liquid phase for two purifications, and finally concentrating and freeze-drying to obtain the pure product. Specific steps are as follows:

[0085] 1. Synthesis:

[0086] Weigh 1g of Fmoc-Pro-2Cl resin, pour it into a 1L glass sand core reaction column, add CH 2 Cl 2 10mi to fully expand the resin.

[0087] Uncapping: add 10ml of hexahydropyridine / DMF decapping solution, seal it and place it in a shaker for 5 minutes, the temp...

Embodiment 2

[0112] Synthesis of PEG

[0113] PEG is commissioned to be synthesized by Shanghai Jill Biochemical Co., Ltd., and PEG has four molecular weights of 5000D, 10000D, 20000D and 40000D.

Embodiment 3

[0114] Example 3 Steps for Polyethylene Glycol Modification of Polypeptides

[0115] mPEG-SC 20K Reaction with AP-25

[0116] Weigh 2g mPEG-SC respectively 20K Put 168.33mg AP-25 (molar ratio is 1.5:1) in 40ml-100ml prepared PBS buffer solution with pH5-8.5, overnight at 4°C, make it react, the PEG modification site is N-terminal Alanine, PEG reacts with free amino groups on alanine. PEG-SC500-20000 can be linked according to Example 2 to synthesize modified polypeptides.

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Abstract

The invention relates to the medicine field, and more specifically relates to an integrin blocking agent capable of inhibiting tumor vessel generation, having integrin element endophilicity and combination capability, the blocking agent is a polypeptide, and the polypeptide is modified by polyethylene glycol, after modifying, the half-life period of the polypeptide is prolonged, immunogenicity is reduced, and the blocking agent enables fusion expression with bovine serum albumin, heat shock protein, chaperonin, glutathione transferase (GST), signal peptide and immunoglobulin, and is in favor of correct formation of disulfide bond, the half life period can be prolonged, a certain special function of fusion protein is simultaneously increased. The integrin blocking agent polypeptide after modification and fusion expression can be used in treatment of solid tumor. The designed integrin blocking agent polypeptide has the advantages of scientific, reasonable, feasible and effective performances, and can be a treatment medicine for treating solid tumor of human, the treatment spectrum of the integrin blocking agent can be greatly developed, and the integrin blocking agent has obviously social value and market value.

Description

technical field [0001] The present invention relates to the field of medicines, in particular to a class of integrin blocking agents capable of inhibiting tumor angiogenesis, and having integrin affinity and binding ability. The blocking agent is a polyethylene glycol modified or fusion polypeptide, and the integrated The peptide blocker polyethylene glycol modification or fusion polypeptide can be used in the preparation of vascular diseases, including rheumatoid, eye disease and tumor drugs. Background technique [0002] Neovascularization, under normal physiological conditions, is highly regulated, and is an essential process in reproduction, embryonic development, tissue repair and wound healing. At the same time, neovascularization is also closely related to many diseases, such as rheumatoid arthritis Inflammation, eye diseases such as age-related macular degeneration (AMD), tumors, etc. [0003] Rheumatoid arthritis (RA) is the most common clinical inflammatory joint ...

Claims

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Application Information

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IPC IPC(8): C07K14/00C07K19/00A61K38/16A61K47/48A61P35/00A61P19/02A61P29/00A61P27/02
Inventor 徐寒梅王祥
Owner CHINA PHARM UNIV
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