DTI (Direct thrombin inhibitor) peptides and application thereof

A thrombin inhibitor and anti-thrombin technology, which is applied in the direction of protease inhibitors, leech inhibitors, specific peptides, etc., can solve the problems of limited clinical application range, single indication, high treatment cost, etc.

Inactive Publication Date: 2013-12-04
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, practice shows that the indications of the above-mentioned injection DTIs and oral DTI drugs are still single, and each DTI is only for a specific disease, and the treatment cost is expensive; therefore, the development of new injection and oral DTIs is important in the treatment and Promising potential for preventing thromboembolic disease
[0003]The inventor of this application has previously developed a ...

Method used

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  • DTI (Direct thrombin inhibitor) peptides and application thereof
  • DTI (Direct thrombin inhibitor) peptides and application thereof
  • DTI (Direct thrombin inhibitor) peptides and application thereof

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Experimental program
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Effect test

Embodiment 1

[0043] 1. Materials and methods

[0044] (1) Strains and plasmids

[0045] GS115 Pichia strain, DH5α Escherichia coli, and pPIC9K plasmids are preserved and frozen by our laboratory;

[0046] (2) Reagents and instruments

[0047] Antibiotic G 418 Purchased from Promega Corporation;

[0048] Acrylamide, methylenebisacrylamide, YNB, and human thrombin were purchased from Sigma Aldrich;

[0049] Yeast extract and tryptone were purchased from OXIOID company;

[0050] Plasma was purchased from Shanghai Blood Center;

[0051] Plasmid extraction kit was purchased from Invitrogen;

[0052] Sephacryl S-100 HR, Sephadex-G50 and Q-Sepharose-FF were purchased from GE;

[0053] Molecular simulation software Discovery Studio 3.1 was purchased from Chuangteng Company;

[0054] Electroporation instrument and electroporation cup were purchased from Bio-Rad;

[0055] The rest of the reagents are imported or domestic analytical reagents;

[0056] (3) Solution and medium preparation

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Abstract

The invention belongs to the field of biotechnology and relates to DTI (Direct thrombin inhibitor) peptides and the application thereof. According to the invention, the molecule of RGD-Hirudin is truncated on the basis of the structure of the RGD-Hirudin, so as to obtain micro-molecule DTI Peptide 1 and micro-molecule DTI Peptide 2. A test and an animal experiment show that the Peptide 1 and the Peptide 2 are DTIs, have antithrombin activity, have definite action target points, have no impact on other blood coagulation factors, can be further used for preparing oral anticoagulant drugs or subcutaneous sustained-release anticoagulant drugs, and particularly suitable for thrombotic disease prevention. The DTI peptides can be taken as candidate drugs for DTIs to be studied intensively, and lay the foundation for developing novel DTIs.

Description

Technical field [0001] The invention is a biotechnology field, involving a anticoagulant polypeptide and its purpose, especially the polypeptide and its use of direct coagulanticase inhibitors. Background technique [0002] Existing technology has disclosed the development and development of direct coagulant inhibitors (DTIS) in preventing and treating veins and arterial thrombosis, heparin -induced platelet reduction (HIT) and acute coronary ischemic syndrome and other cardiovascular and cerebrovascular diseases.It has a huge role.Compared with traditional anticoagulants (heparin and vitamin K (VKAS)), DTIS has obvious advantages; it is currently known that DTIS and oral DTI are used for clinical treatment.However, practice shows that the adaptation of DTIS and oral DTI drugs in the above injection is still single. Each DTI is only for specific diseases and expensive treatment costs. Therefore, the development of new injection and oral DTIS is developed.It has a broad prospect f...

Claims

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Application Information

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IPC IPC(8): C07K14/815A61K38/58A61P7/02
Inventor 莫炜黄一农于敏张艳玲
Owner FUDAN UNIV
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