Modified serine protease inhibitors for use in the treatment of bleeding disorders

A serine protease and inhibitor technology, applied in protease inhibitors, blood diseases, extracellular fluid diseases, etc.
CN105992771BActive Publication Date: 2019-08-23CAMBRIDGE ENTERPRISE LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
CAMBRIDGE ENTERPRISE LTD
Publication Date
2019-08-23

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Abstract

The present invention relates to procoagulant serine protease inhibitor molecules engineered to exhibit increased specificity for anticoagulant proteases by modifying P4, P2, P1 and / or P1' residues within the reactive center loop (RCL). These modified serpin molecules can be used in therapy, for example, as coagulants for the treatment of bleeding.
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Description

technical field

[0001] The present invention relates to modified serine protease inhibitor (serpin) molecules with altered specificity, in particular modified to have anticoagulant protease (anticoagulant protease, anticoagulant protease) (such as activated protein C (activated protein C) , a serine protease inhibitor molecule of increased specificity of activated Protein C) (APC)). Background technique

[0002] Hemophilia is a bleeding disorder caused by a lack of circulating plasma fVIII (hemophilia A, HA) or fIX (hemophilia B, HB) (reviewed in Bolton-Maggs & Pasi, 2003). This reduces the activity of endogenous X enzyme (tenase) (Xase) and thereby reduces the amount of thrombin produced when tissue damage occurs. This leads to uncontrolled bleeding after injury as well as spontaneous bleeding to joints and soft tissues.

[0003] Hemophilia affects about 1 in 5,000 people. The 170,000 patients identified in the World Federation of Hemophilia Global Survey is an underesti...

Claims

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