Peptides for heparin and low molecular weight heparin anticoagul

Details Peptides for heparin and low molecular weight heparin anticoagul Peptides for heparin and low molecular weight heparin anticoagul

1996-07-09

1998-02-24

Hutzell, Paula K.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530324, A61K 3800, C07K 1400

Patent

active

057212120

ABSTRACT:
Less toxic agents for reversal of heparin or low molecular weight heparin anticoagulation which are synthetic protamine-like polycationic peptides having a total cationic charge which is less than that of n-protamine. In preferred embodiments, arginine resides of n-protamine are replaced with lysine residues for ease of manufacture. Selective positively charged arginine residues have been replaced with an uncharged amino acid residue or its analog, such as glycine or glutamine, in order to reduce the total 29 amino acid residues wherein 4 to 5 clusters of 2 to 4 positively charged amino acids are separated by 2 to 6 neutral amino acids. The C-terminus and the N-terminus can be modified to mitigate against in vivo degradation by carboxypeptidases and aminopeptidases.

REFERENCES:
patent: 4792525 (1988-12-01), Ruoslahti et al.
patent: 5272261 (1993-12-01), Cardin et al.
patent: 5358934 (1994-10-01), Borovsky et al.

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