Polypeptide inhibitor modified with polyethylene glycol for inhibiting vascular endothelial growth factor receptors 2 tyrosine kinase and application thereof.

A growth factor receptor and tyrosine kinase technology, applied in the direction of peptides, anti-inflammatory agents, non-central analgesics, etc., to achieve less side effects, significant rheumatoid arthritis, and polyethylene glycol-modified vascular endothelial growth Effects of Science on Factor Receptor 2 Tyrosine Kinase Peptide Inhibitors

Inactive Publication Date: 2014-05-07
NANTONG CHENGXIN AMINO ACID
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The research on PEG modification of synthetic small molecule peptides started late, but it has attracted the attention of many researchers

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Immunoprotective effect of polyethylene glycol-modified vascular endothelial growth factor receptor 2 tyrosine kinase polypeptide inhibitor in collagen-induced mouse arthritis animal model

[0018] To construct collagen-type mouse arthritis animal model, and to study the therapeutic effect of polyethylene glycol-modified vascular endothelial growth factor receptor 2 tyrosine kinase polypeptide inhibitor on collagen-induced arthritis (CIA) in mice. Mice were used as experimental animals, 90 SPF grade DBA / 1 mice (provided by Sino-British SIPPR Lab. Animal Ltd, animal production license number: SCXK (Shanghai )2008-0016), male, 7-8 weeks old, body weight 18-22 g, were randomly divided into 6 groups, namely normal control group, model control group, peptide inhibitor 1 low, middle and high dosage groups (5, 10 , 20 mg / kg) and positive drug control group (methotrexate 2 mg / kg). In addition to the normal group, the mouse CIA model was established in each experimental group o...

Embodiment 2

[0023] In vivo immunoprotective effect of polyethylene glycol-modified vascular endothelial growth factor receptor 2 tyrosine kinase polypeptide inhibitor on adjuvanted rat arthritis animal model

[0024]To construct an adjuvant rat arthritis animal model, and to study the therapeutic effect of polyethylene glycol-modified vascular endothelial growth factor receptor 2 tyrosine kinase polypeptide inhibitor on adjuvant arthritis (AA) rats. Rats were used as experimental animals, 90 SPF grade SD rats (provided by Sino-British SIPPR Lab. Animal Ltd, animal production license number: SCXK (Shanghai) 2008 -0016), male, weighing 140 g-160 g, were randomly divided into 6 groups, which were normal control group, model control group, polyethylene glycol-modified vascular endothelial growth factor receptor 2 tyrosine kinase polypeptide inhibitor low There were 3 medium and high dose groups (5, 10, 20 mg / kg) and positive drug control group (methotrexate 1 mg / kg). In addition to the norma...

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Abstract

The invention relates to the field of medicines and particularly relates to polypeptide for inhibiting vascular endothelial growth factor receptors 2 tyrosine kinase and preventing and treating the rheumatoid arthritis. After the polypeptide is modified with polyethylene glycol and the sequence of the polypeptide is Mpeg-SC10k-Val-Cys-CyS-Ser-Thr-Arg-Glu which is an entirely-new sequence. The polypeptide can be used for treating the rheumatoid arthritis and has potential new-medicine development value.

Description

Technical field: [0001] The invention relates to the field of medicine, in particular to a vascular endothelial growth factor receptor 2 tyrosine kinase polypeptide inhibitor for preventing and treating rheumatoid arthritis. Background technique: [0002] Rheumatoid arthritis (RA) is the most common clinical inflammatory joint disease and one of the main disabling factors. It is about 0.5%-1.0% in the world, and the incidence of RA is about 0.4% in my country. RA can occur at any age, and the incidence rate increases with age. The high-incidence age of women is 45-55 years old, and gender is closely related to the incidence of RA, with a male-to-female ratio of about 1:3. [0003] Neovascularization, under normal physiological conditions, is highly regulated and is an essential process in reproduction, embryonic development, tissue repair and wound healing. Angiogenesis also occurs in various pathological conditions, such as RA. In the pathological process of RA, angio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06A61K38/08A61P19/02A61P29/00
Inventor 邢将军许刘华彭立军任世阔华俊国曹铭刘加根刘明明汪士金施新华刘伟峰严明
Owner NANTONG CHENGXIN AMINO ACID
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