Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

A kind of erythropoietin mimetic peptide and its preparation method and application

An erythropoietin and peptide-mimicking technology, applied in the field of Ming Dynasty, can solve the problems of low EC50 and limitation, and achieve the effect of prolonging the half-life

Active Publication Date: 2019-06-28
TIANJIN INSTITUTE OF PHARMA RESEARCH
View PDF6 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the EC50 of peptides that can stimulate erythrocyte proliferation and differentiation is very low, between 20nM and 250nM, so the clinical application of these peptides is greatly limited

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A kind of erythropoietin mimetic peptide and its preparation method and application
  • A kind of erythropoietin mimetic peptide and its preparation method and application
  • A kind of erythropoietin mimetic peptide and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1 Synthesis of Erythropoietin Mimetic Peptide Dimer

[0049] The erythropoietin mimetic peptide of the present invention is a polypeptide, which can be prepared using the Fmoc solid-phase polypeptide synthesis method, and the CS 336X instrument produced by CSBio Company to synthesize the polypeptide of the present invention. The method of synthesis was carried out according to the manufacturer's instruction manual. The Fmoc solid-phase polypeptide synthesis method described herein refers to a synthetic method in which a polymer resin is used as a solid-phase reaction matrix to sequentially condense amino-terminal Fmoc-protected amino acids in the presence of a coupling reagent to synthesize a polypeptide. For its specific method, see Fmoc solid phase peptide synthesis: a practical approach, 2000, Oxford University Press. And form the intramolecular disulfide bond of the simulated peptide by oxidation methods, such as 20% DMSO oxidation method and iodine oxidat...

Embodiment 2

[0050] Example 2 Effect of erythropoietin mimetic peptide dimer on mice

[0051] Using mice to evaluate and compare the effects of p-xylene-conjugated erythropoietin mimetic peptide dimer and erythropoietin protein on mouse erythropoiesis.

[0052] Among them, EPO drugs were purchased from Shenyang Sansheng Pharmaceutical Co., Ltd.;

[0053] Kunming mice, purchased from Shanghai Experimental Animal Center of Chinese Academy of Sciences, weighing 25-30 g, are all female mice. The number of animals in each group in the experiment: 10, divided into 4 groups.

[0054] Among them, the mice in group 1 were injected with p-xylene-coupled erythropoietin mimetic peptide dimer at a dose of 4.5 mg / kg, and the mice in group 1 were injected with erythropoietin protein at a dose of 4.5 mg / kg. The mice in group 1 were the blank control, injected with PBS buffer solution for seven consecutive days, then sacrificed the mice, and collected whole blood for counting peripheral blood cells and ...

Embodiment 3

[0058] Example 3: Effects of Erythropoietin Mimetic Peptides on Rhesus Monkeys

[0059] The EPO drug used in the present invention was purchased from Shenyang Sansheng Pharmaceutical Co., Ltd.

[0060] Rhesus monkeys were used to evaluate the effect of erythropoietin-mimetic peptides on erythropoiesis. Rhesus monkeys, weighing 5.5-8.5 kg, male or female, were purchased from Hainan Experimental Animal Center. The macaques were divided into two groups according to the basic hemoglobin, with three monkeys in each group. The experimental group used the mimetic peptide dimer of the present invention, administered intravenously once a week, 4.5 mg / kg each time; the positive control group used EPO, three times / week, 1.5 mg / kg each time, continuously administered for five weeks, weekly Hematological indicators were measured once.

[0061] As a result, it was found that a single intravenous injection of the mimic peptide of the present invention led to an increase in the hemoglobin...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to erythropoietin mimetic peptide and a dimer thereof. The mimic peptide is the mimic peptide with sequence as shown in the SEQ ID NO:1: SEQ ID NO: 1GGLYAC6HMGPITX1VC15QPLRX2KC, wherein X1 is 3-(1-naphthyl)-L-alanine(Nal); X2 is sarcosine (Sar); cysteine (C) at 6th and 15th sites forms intramolecular disulfide bond; and N-terminal is acetylated. The dimer is formed after the mimic peptide is coupled with p-xylylene. The invention also provides a preparation method of the mimic peptide and the dimer and pharmaceutical salt thereof. The invention also further provides a pharmaceutical composition containing the above mimic peptide or dimer or pharmaceutical salt. The erythropoietin mimetic peptide, the dimer and pharmaceutical salt can stimulate erythropoiesis and remarkably prolong half-life period of a medicine in body.

Description

technical field [0001] The invention belongs to the field of biomedicine, and relates to an erythropoietin mimetic peptide coupled with p-xylene, in particular, the invention relates to an erythropoietin receptor capable of binding to and activating the erythropoietin receptor Or a p-xylene-coupled erythropoietin mimetic peptide capable of agonizing erythropoietin and a preparation method thereof. The present invention also relates to the use of the mimetic peptide in the preparation and treatment of erythropoietin deficiency or red blood cell population deficiency or deficiency Use in medicine for a characteristic disease. Background technique [0002] Erythropoietin (EPO) is a glycoprotein hormone, the earliest clinically used cytokine, and the most single, safe and reliable hemoglobin-raising preparation known so far. It has a certain curative effect on renal anemia, aplastic anemia, multiple myeloma and paroxysmal nocturnal hematuria; in addition, the application of ery...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/505C07K1/14C07K1/10A61K38/18A61P13/12A61P7/06A61P37/02A61P35/00
CPCA61K38/00C07K14/505
Inventor 魏群超郑学敏龚珉周植星徐为人汤立达
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com