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Erythropoietin mimic peptide derivative, and preparation method and application thereof

A technology of erythropoietin and peptide mimics, applied in the field of biomedicine, can solve the problems of low and limited EC50, and achieve the effect of prolonging the half-life

Active Publication Date: 2016-08-10
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • 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

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  • Erythropoietin mimic peptide derivative, and preparation method and application thereof
  • Erythropoietin mimic peptide derivative, and preparation method and application thereof
  • Erythropoietin mimic peptide derivative, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Example 1 Synthesis of Erythropoietin Mimetic Peptide Derivatives

[0057] The present invention will be described in further detail below in conjunction with specific examples.

[0058] The erythropoietin mimetic peptide derivatives of the present invention are multimers, wherein the monomers are prepared using the Fmoc solid-phase peptide synthesis method, and the CS 336X instrument produced by CSBio Company is used to synthesize the peptides 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. ...

Embodiment 2

[0082] Example 2. Effects of Erythropoietin Mimetic Peptide Derivatives on Mice

[0083] Using mice to evaluate and compare the effects of erythropoietin mimetic peptide derivatives and erythropoietin protein on mouse erythropoiesis.

[0084] Among them, EPO drugs were purchased from Shenyang Sansheng Pharmaceutical Co., Ltd.;

[0085] 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 12 groups.

[0086] Among them, 10 groups of mice were injected with erythropoietin mimetic peptide derivatives 1-10, 1 group of mice were injected with erythropoietin protein, 1 group of mice were blank controls, injected with PBS buffer solution, the dose was 4.5mg / kg, for three consecutive days, and then the mice were sacrificed, and the whole blood was collected for peripheral blood cell and reticulocyte count, and the blood cell cou...

Embodiment 3

[0090] Example 3: Effects of Erythropoietin Mimetic Peptide Derivatives on Rhesus Monkeys

[0091] Rhesus monkeys were used to evaluate the effect of erythropoietin-mimetic peptide derivatives 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. One group received derivative 3, intravenously injected once a week, 4.5 mg / kg each time, and the other group received EPO, three times / week, 240 μ / kg each time, administered for five consecutive weeks, and measured hematological indicators once a week

[0092] It was found that a single intravenous injection of the derivative 3 led to an increase in the hemoglobin content (33%) and hematocrit in the peripheral blood of rhesus monkeys, indicating that the derivative 3 stimulated the production of hemoglobin. The positive control erythropoietin also in...

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Abstract

The invention relates to an erythropoietin mimic peptide derivative having a long-acting function of promoting erythropoiesis and pharmaceutically-acceptable salt of the derivative. The invention further provides a preparation method of the erythropoietin mimic peptide derivative, and an application of the derivative to prepare a medicine for treating diseases characterized by lacking erythrogenin, or lacking or having defects in erythrocyte groups. The provided erythropoietin mimic peptide derivative is a monomer peptide shown in SEQ ID NO:1 or a multimer formed from lysine (K) located at the end of the monomer peptide through side-chain free amino groups. In the multimer, two cysteines of each monomer peptide form a disulfide bond, and the number of monomer peptide is 2-10.

Description

technical field [0001] The invention belongs to the field of biomedicine, and relates to an erythropoietin mimic peptide derivative. Erythropoietin mimetic peptide derivatives with agonistic effect of poietin and preparation method thereof, the present invention also relates to the use of said mimetic peptide derivatives in the preparation and treatment of diseases characterized by the lack of erythropoietin or by the absence or deficiency of red blood cell populations Uses in medicine. Background technique [0002] Erythropoietin (EPO) is a glycoprotein hormone with a molecular weight of about 34kD. The erythropoietin present in the plasma is composed of 165 amino acids, with a high degree of glycosylation, and the main sugar component is sialic acid. According to different carbohydrate content, naturally occurring erythropoietin is divided into two types, α-type and β-type, among which, α-type contains 34% carbohydrates, and β-type contains 26% carbohydrates. The two ty...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/505C07K19/00C07K1/06C07K1/04A61K38/18A61P7/06A61P37/06A61P35/00
Inventor 龚珉郑学敏于冰孔维苓黄长江吴疆徐为人
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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