Serineprotease inhibitor proteins, pharmaceutical...

C - Chemistry – Metallurgy – 12 – N

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530/13, 167/103.

C12N 15/15 (2006.01) A61K 38/55 (2006.01) C07K 14/81 (2006.01) C12N 1/00 (2006.01) C12N 5/10 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2002047

Abstract The invention relates to new serineprotease inhibitor proteins, pharma-ceutical compositions containing them, DNA sequences coding for these proteins and processes for the preparation of these proteins, pharma- ceutical compositions and DNA sequences. The new proteins comprise amino acid sequences of the formula Image or parts thereof embracing at least the sequence of positions 53 to 101, wherein W is tyrosine or glutamic acid, X1 and X2 have the same or a different meaning and each represents methionine or leucine, X3 is methionine, leucine or phenylalanine, Y is proline or arginine and Z represents leucine or, in case W is tyrosine and X1, X2, X3 are leu- cine, Z may also represent isoleucine, and fusion proteins of these new serineprotease inhibitor proteins. The new proteins have excellent inhi- bitory activity especially towards human leukocyte elastase and a pro- nounced resistance against oxidative inactivation. There are described DNA sequences coding for the new serineprotease inhibitor proteins and the expression of these proteins in suitable host organisms by means of different types of vectors. There are further described methods for the preparation of these coding DNA sequences, vectors containing them and the preparation of the new proteins in pure biologically active form as well as pharmaceutical compositions containing said proteins.

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