Fibrinolytic composition and method of its preparation
AssigneeCouncil of Scientific and Industrial Research
InventorsNavneet Kaur, Prakash Kumar, Girish Sahni
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Abstract
The present invention discloses modified forms of plasmin with advantageous properties. As compared to their natural unmodified form, these variants exhibit significantly modulated kinetics in terms of delayed inhibition characteristics in the presence of specific inhibitors, such as α2-antiplasmin (α2-AP). These include PEG-conjugated thiol derivatives of truncated plasmin with potential clinical applications in various regimens of thrombolytic therapies.
Claims12
A fibrinolytic composition comprising:
- (a) a thiol derivative of plasminogen comprising a substitution of one to eight amino acid residues in a catalytic domain of SEQ ID NO:
- 2 with a cysteine residue, wherein the thiol derivative of plasminogen comprises an amino acid sequence selected from SEQ ID NOs:
- 3-23 and a polyethylene glycol (PEG) moiety covalently-bound to the cysteine residue;
- and
- (b) a pharmaceutically acceptable diluent, carrier, or adjuvant.
A plasminogen variant polypeptide, comprising a substitution of one to eight amino acid residues in a catalytic domain of SEQ ID NO:
- 2 with a cysteine residue, wherein the plasminogen variant polypeptide comprises an amino acid sequence selected from SEQ ID NOs:
- 3-23, and a polyethylene glycol (PEG) moiety covalently-bound to the cysteine residue.
Dependencies are inferred from the claim text.