Isohirudins

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – 25 or more amino acid residues in defined sequence

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Details

A61K 3700, A61K 3702, C07K 500, C07K 700

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active

053229266

ABSTRACT:
Thrombin inhibitors from the hirudin family which differ from the previously known hirudins by mutation in the protein chain, and a process for their preparation are described. The novel hirudins are distinguished by a high specific activity, high stability and good pharmacokinetics.

REFERENCES:
patent: 4668662 (1987-05-01), Tripier
patent: 4791100 (1988-12-01), Kramer et al.
Smith et al., Principles of Biochemistry, 7th Ed., McGraw-Hill, New York, 1983.
Dodt et al., FEBS Letters, vol. 165, No. 2, pp. 180-184, Jan. 1984.
Dodt et al., FEBS Letters, vol. 229, No. 1, pp. 87-90, Feb. 1988.
Geiger et al., "Deamidation, Isomerization, and Racemization at Asparaginyl and Aspartyl Residues in Peptides," Journal of Biological Chemistry, vol. 262, No. 2, 1987, pp. 785-794.
Stephenson et al., "Succinimide Formation from Aspartyl and Asparaginyl Peptides as a Model for the Spontaneous Degradation of Proteins," Journal of Biological Chemistry, vol. 264, No. 11, 1989, pp. 6164-6170.
Bowie et al., "Deciphering the Message in Protein Sequences: Tolerance to Amino Acid Substitutions," Science, vol. 247, Mar. 16, 1990, pp. 1306-1310.
Baskova et al., "Hirudin From Leech Heads and Whole Leaches and `Pseudo-Hirudin` From Leech Bodies," Thrombosis Research, vol. 30, 1983, pp. 459-467.
Harvey et al., "Cloning and Expression of a cDNA Coding for the Anticoagulant Hirudin From the Bloodsucking Leech, Hirudo medicinalis," Proc. Natl. Acad. Sci. USA, vol. 83, Feb. 1986, pp. 1084-1088.

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