Direct thrombin inhibitor polypeptides and uses thereof

Abstract

The invention belongs to the field of biotechnology, and relates to direct thrombin inhibitor polypeptide and application thereof. On the basis of an RGD-Hirudin structure, the molecule of RGD-Hirudin is shortened to obtain direct thrombin inhibitor micro-molecule polypeptides Peptide 1 and Peptide 2; results of tests and animal experiments show that the polypeptides Peptide 1 and Peptide 2 are direct thrombin inhibitors, have anti-thrombin activity, and are clear in drug action target and of no effect on other blood coagulation factors; the direct thrombin inhibitors can be further used for preparing oral or subcutaneous controlled-release anticoagulant drugs, and is especially suitable for preventing thrombotic diseases; the polypeptides disclosed by the invention can additionally undergo deep study as a candidate drug of the direct thrombin inhibitors, so as to lay a foundation for developing novel direct thrombin inhibitors.

Description

[0001] This application is the name of the invention: direct thrombin inhibitor polypeptide and its use, [0002] Application number: 201310127718.2, application date: divisional case on April 14, 2013. technical field [0003] The invention belongs to the field of biological technology, and relates to an anticoagulant polypeptide and its application, especially a direct thrombin inhibitor polypeptide and its application. Background technique [0004] The prior art discloses that the research and development of direct thrombin inhibitors (DTIs) play a role in the prevention and treatment of cardiovascular and cerebrovascular diseases such as venous and arterial thrombosis, heparin-induced thrombocytopenia (HIT) and acute coronary ischemic syndrome. played a huge role. Compared with traditional anticoagulants (heparin (heparin) and vitamin K (VKAs)), the DTIs have obvious advantages; currently known, DTIs for injection and oral DTI have been used in clinical treatment. Howe...

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 therein is only for a specific disease, and the treatment cost is expensive; Promising potential for preventing thromboembolic disease

[0005] The inventors of the present application have previously developed a novel bifunctional fusion protein RGD-hirudin, which has dual functions of antithrombin and antiplatelet aggregation. RGD-Hirudin is a protein / polypeptide drug. As a direct thrombin inhibitor, it can only be administered through intravenous injection, which obviously limits its clinical application.

Images