Conjugate of 9-(2-hydroxyethoxymethyl)-guanine with lactosaminat

Details Conjugate of 9-(2-hydroxyethoxymethyl)-guanine with lactosaminat Conjugate of 9-(2-hydroxyethoxymethyl)-guanine with lactosaminat

1986-10-21

1988-02-16

Schain, Howard E.

Chemistry: natural resins or derivatives; peptides or proteins;

Proteins, i.e., more than 100 amino acid residues

Albumin

424 89, 514 8, 514 21, 530362, 530395, 530397, C07K 1514

Patent

active

047256729

ABSTRACT:
A conjugate of 9-(2-hydroxyethoxymethyl)-guanine with lactosaminated human albumin is therapeutically more efficacious than the free drug in the treatment of chronical hepatitis induced from Virus B. For the preparation of the conjugate an aqueous solution of 9-(2-hydroxyethoxymethyl)-guanine in form of a derivative, particularly monophosphate, and an aqueous solution of lactosaminated human albumin are reacted in the presence of 1-ethyl-3-(dimethylaminopropyl)-carbodiimide, by adjusting the pH to the value of 7.5 and by maintaining the reaction mixture for 24 hours under stirring and in the dark.

REFERENCES:
Analytical Biochemistry, 98, 319-328 (1979), Quinn et al.
FEBS Letters, 115, No. 2, 185-188 (1980), Feix et al.
Science, 227, 1296-1303 (1985), Dolin.
FEBS Letters, 153, No. 1 (1983), Aurialitt et al.

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