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Antithrombotic medicine RWR for specifically identifying platelet alpha<IIb>beta3

A technology for thrombotic diseases and small molecule peptides, applied in the field of protein peptides, can solve the problems of large side effects and low specificity, and achieve the effects of small side effects, reduced immunogenicity, broad market and clinical application prospects

Inactive Publication Date: 2012-02-15
SHANXI MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The purpose of the present invention is to provide a polypeptide that can specifically recognize and inhibit thrombosis, so as to overcome the problems of large side effects and low specificity of existing thrombosis inhibitors and some thrombolytic drugs, in order to play a role in clinical treatment. Efficient and specific inhibition of thrombus formation
A specific recognition platelet α described in the present invention IIb beta 3 The antithrombotic drug RWR has not been reported at home and abroad so far

Method used

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  • Antithrombotic medicine RWR for specifically identifying platelet alpha&lt;IIb&gt;beta3
  • Antithrombotic medicine RWR for specifically identifying platelet alpha&lt;IIb&gt;beta3

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Synthesis, purification and identification of Arg-Gly-Asp-Trp-Arg

[0018] Applying the 9-fluorenylmethoxycarbonyl (Fmoc) method, using Wang Resin (Wang Resin) peptide to synthesize the carrier, first link the carboxyl group of Arg with wang-Resin through an amide bond, and then extend the peptide from the C-terminus to the N-terminus according to the pentapeptide sequence Chain, adding condensing agents such as benzotriazole-N,N,N,N-tetramethyluronium hexafluorophosphate (HBTU), 1-hydroxy-benzo-triazole (HOBt) for each condensation step, After condensation, the Fmoc protecting group was removed with 20% DMF (dimethylformamide) solution. After the synthesis of the peptide chain, TFA (trifluoroacetic acid) was used to stir at room temperature, oscillate, and filter to dissociate the peptide chain from the resin while removing the side chain protecting group. The completeness of deprotection and condensation was checked using ninhydrin reagent. The synthesized RWR was ...

Embodiment 2

[0019] : Activity experiment and dose-effect relationship research of antithrombotic effect in vitro

[0020] Blood was collected through the cubital vein on an empty stomach in the early morning, anticoagulated with 3.8% sodium citrate (the volume ratio of blood to anticoagulant was 9:1), centrifuged at 1000r / min for 8min at room temperature, and the upper plasma was taken as platelet-rich Plasma (PRP platelet-rich plasma), isolated PRP. The remaining blood was centrifuged at 3000r / min for 10min, and the upper layer of plasma was collected to obtain platelet-poor plasma (PPP platelet-poor plasma). PRP was adjusted with PPP so that the platelet count was about 250,000 / μL. Take 400 μL of PRP, add NS (negative control) and different concentrations of Tirofiban (Tirofiban) (200, 100, 50, 25, 12.5 μM positive control) / small peptide RWR (100, 50, 20, 12.5, 6.25 μM Final concentration) 50 μl, the platelet aggregation rate was determined by turbidimetry (the measuring instrument i...

Embodiment 3

[0025] : Stability experiment and aging relationship research of antithrombotic effect in vivo

[0026] In order to measure the change of blood drug concentration in the body, this study used the platelet aggregation rate to observe the relationship between the pharmacological effect and time after RWR rabbit ear vein injection.

[0027] In order to observe the action time and intensity of the drug, that is, the stability in plasma, NS, small peptide RWR, and PRP (in the same amount as above) were incubated for 3 hours at 37°C, and platelet aggregation was induced with a concentration of 50 μM ADP, and the maximum platelet aggregation rate was measured. , The measurement time is 2h.

[0028] The results show that after intravenous injection of RWR, it can quickly produce a strong anti-platelet aggregation effect, which can significantly prolong the platelet aggregation rate compared with the control group, and the strong anti-platelet pharmacological effect can be maintained f...

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Abstract

The invention provides a small molecular polypeptide for reforming RGD tripeptide. According to the characteristic that the RGD is specifically combined with alpha<IIb>beta3, a hydrophobic amino acid and a basic amino acid are added at the N end of the RGD, a hydrophobic amino acid W is added in the fourth site, a basic amino acid R is added in the fifth site, the small peptide sequence is Arg-Gly-Asp-Trp-Arg, the protein primary structure is RGDWR, the capability for specifically being combined with the alpha<IIb>beta3 can be improved, the immunogenicity can also be reduced by smaller molecular weight, and the defects of the existing antithrombotic preparations are overcome.

Description

Technical field: [0001] The present invention relates to the field of protein polypeptides, in particular to a protein that can specifically recognize platelet surface integrin α IIb beta 3 Polypeptides and their preparation and application. Background technique: [0002] Cardiovascular and cerebrovascular diseases such as myocardial infarction and cerebral infarction are major diseases that seriously threaten human health. The number of people who die from cardiovascular and cerebrovascular diseases in the world is as high as 15 million every year, ranking first among various causes of death. Cardiovascular and cerebrovascular diseases have the characteristics of high morbidity, high disability rate, high mortality rate, high recurrence rate, and many complications, that is, "four highs and one many". It has become the number one killer with the highest cause of human death. Even if the most advanced and perfect treatment methods are applied, more than 50% of survivors of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C07K1/20C07K1/06C07K1/04A61K38/08A61P7/02
CPCY02P20/55
Inventor 杨利军杨涛孙海飚刘海桃赵海霞常冰梅王惠珍
Owner SHANXI MEDICAL UNIV
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