Novel hirudine variant, process for producing the same, and...

Details Novel hirudine variant, process for producing the same, and... Novel hirudine variant, process for producing the same, and...

C - Chemistry, Metallurgy

12

N

C12N 15/15 (2006.01) A61K 38/58 (2006.01) C07K 14/815 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2124330

Abstract of the disclosure Novel hirudin analogs, method of manufacture thereof and anticoagulant compositions having these as active ingredients. Hirudin analogs of which sequences are shown in the general formula I. DNAs coding the amino acid sequence of these hirudin analogs, expression vectors, recombinant microorganisms, and method of manufacturing the hirudin analogs using these recombinant microorganisms. Anticoagulants containing these hirudin analogs as their active ingredient. Sequences Asp33-Gly34- or Asp62-Ala63- of conventional hirudins or their analogs were substituted to suppress the formation of succinimide form or .beta. form, which resulted in hirudins with high stability, high antithrombin activity and useful as anticoagulants. Furthermore, the hirudin analogs having Val1-Val2- of the conventional hirudin analogs substituted by Ile1-Ile2- show particularly preferrable and extremely high antithrombin activity when used as an anticoagulant. 57

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