DTI (Direct thrombin inhibitor) peptides and application thereof

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...

AI Technical Summary

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 new bifunctional fusion protein RGD-hirudin, which has dual functions of antithrombin and antiplatelet aggregation, and belongs to a class of biotechnology The new drug has now entered the phase I clinical research stage; but because the RGD-Hirudin is a protein / polypeptide drug, as a direct thrombin inhibitor, it can only be administered through intravenous injection, which obviously limits its use. clinical use range

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