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

1994-09-08

1997-03-25

Nucker, Christine M.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 2, 514 13, 530300, 530324, 530325, 530326, A61K 3800, C02K 14745

Patent

active

056144946

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 residues 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 cationic charge on the polycationic peptide to the range of about [+14] to [+18], preferably [+16] to [+18]. In specific embodiments, there are sequences of 29 and 32 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. Another modification, specifically use of .alpha.-helix forming amino acids, such as glutamic acid, further promotes anticoagulation reversal.

REFERENCES:
DeLucia III, A. et al. (1993) Efficacy and toxicity of differently charged olycationic protamine-like peptides for heparin anticoagulation reversal. J. Vasc. Surg. 18, 49-60. See entire document. Published Jul. 9, 1993.
McKay, D. et al. (1986) Amino acid sequences of six distinct proteins from a single testis. Eur. J. Biochem. 158, 361-366. See Fig. 6 on p. 365.
Merck Index, Ninth Ed., Merck & Co., Rahway, NJ (1976). See p. 7675, entry No. 7669.

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