Polypeptide derivative for promoting cell proliferation and preparation method and application thereof

A technology of derivatives and polypeptides, applied in the field of polypeptide derivatives that promote cell proliferation and their preparation, can solve the problems of low retention rate, limited scope of application, and high cost of recombinant protein production, achieve simple synthesis, and promote blood vessels. The effect of repairing and regeneration, promoting endothelial cell proliferation

Active Publication Date: 2019-07-02
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] First of all: the production cost of existing recombinant proteins is high, the production process is difficult to strictly control, the quality between batches is difficult to guarantee, and industrialization is difficult
[0008] Secondly, the transportation and storage conditions of recombinant proteins are harsh, which further increases their production costs and limits their scope of application
[0009] Again, for the protein itself, it is ineffective to directly inject IGF-I protein into the damaged organ, mainly due to its low retention rate in the tissue (small size: about 7.5KD)
In order to solve these problems, researchers have developed many methods to encapsulate IGF-I and deliver it to designated locations through biocompatible carriers, but none of these studies have achieved clinical application

Method used

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  • Polypeptide derivative for promoting cell proliferation and preparation method and application thereof
  • Polypeptide derivative for promoting cell proliferation and preparation method and application thereof
  • Polypeptide derivative for promoting cell proliferation and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Solid Phase Synthesis of Nap-FFGGYGSSSRRAPQT

[0038] Specific steps are as follows:

[0039] 1) Weigh 0.5 mmol of 2-cl-Trt resin into a solid-phase synthesizer, add 10 mL of anhydrous dichloromethane (represented by DCM below), place it on a shaker and shake for 5 min to fully swell the 2-Cl-Trt resin ;

[0040] 2) Use ear washing balls to remove DCM from the solid-phase synthesizer equipped with 2-Cl-Trt resin;

[0041] 3) Dissolve 0.75 mmol of Fmoc-Thr in 10 mL of anhydrous DCM, add 0.75 mmol of DIPEA, then transfer to the above solid-phase synthesizer, add 0.75 mmol of DIPEA, and react at room temperature for 1 h;

[0042]4) Sealing: Remove the reaction liquid in the solid-phase synthesizer with ear washing balls, then wash with 10 mL of anhydrous DCM, 1 min each time, and wash 5 times in total. Add the prepared volume ratio of anhydrous DCM: DIPEA: methanol = 17:1:2 solution 20mL, react at room temperature for 10min;

[0043] 5) Remove the reaction solution in ...

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Abstract

The invention relates to a polypeptide derivative for promoting cell proliferation and a preparation method and an application thereof. The structure of the polypeptide derivative is Nap-FFGGYGSSRRAPQT. The present invention also provides a preparation method of the polypeptide derivative. The polypeptide derivative is synthesized by adopting a FMOC-solid phase synthesis method. The present invention also provides an application of the polypeptide derivative in medicines for promoting cell proliferation. The derivative is simple to synthesize, the active self-assembled polypeptide can be synthesized by a solid-phase synthesis method, and the used raw materials are amino acids necessary for human bodies every day; secondly, due to self-assembly, the derivative can be slowly released in vivo, thereby remarkably solving the problem of low in-vivo retention rate caused by easy degradation of IGF-I protein by various proteases in vivo after injection; and most importantly, the derivative can be combined with an IGF-I protein receptor to stimulate downstream signal pathways, to promote endothelial cell proliferation, and to promote vascular repair and angiogenesis.

Description

technical field [0001] The invention belongs to the field of biomedicine, and relates to a polypeptide derivative, in particular to a polypeptide derivative that promotes cell proliferation, and a preparation method and application thereof. Background technique [0002] Insulin-like growth factor I (IGF-I) is a growth factor protein similar to insulin in humans. It plays a vital role in growth and development, metabolism and cell survival, and has a wide range of applications in clinical and life science research. [0003] In clinical practice, there are currently two drugs based on IGF-I protein approved by the US FDA for the treatment of adolescent growth failure (Growth Failiure) and Laron syndrome (Laron syndrome), namely Mecasermin (Mecasermin) ), which is recombinant human IGF-I protein (rhIGF-I); and Mecasermin rinfabate, which is a complex of recombinant human IGF-I protein and recombinant human IGFBP-3 protein (rhIGFBP-3). [0004] In addition to being used as a c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/475C07K1/16C07K1/06C07K1/04A61K38/18A61P9/00B82Y5/00B82Y30/00B82Y40/00
CPCC07K14/475B82Y5/00B82Y30/00B82Y40/00A61K38/00Y02P20/55
Inventor 高洁杨志谋孔德领王恺商宇娜智登科
Owner NANKAI UNIV
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