Enzymatically active toxin coupled to a cell-specific ligand

Details Enzymatically active toxin coupled to a cell-specific ligand Enzymatically active toxin coupled to a cell-specific ligand

1989-02-21

1992-01-14

Naff, David M.

Drug, bio-affecting and body treating compositions

Enzyme or coenzyme containing

424 946, 424 9463, 435174, 4351723, 530807, 530810, 935 13, 935 14, A61K 3748, A61K 3754, C12N 1500, C12N 1100

Patent

active

050808982

ABSTRACT:
A cell-specific toxin molecule is prepared containing an enzymatically active toxin moiety coupled to a cell-specific binding ligand. The toxin moiety may be a diphtheria toxin, and has a non-naturally occurring cysteine residue encoded by a DNA sequence including a non-naturally occurring cysteine codon. The ligand may be a peptide hormone, proteinaceous growth factor, antibody of steroid hormone, and is derivatized with a sulfhydryl group reactive with the cysteine residue of the toxin moiety to couple the ligand to the toxin moiety via a disulfide bond. Derivatization of the ligand may be by providing the ligand with a non-naturally occurrring cysteine residue encoded by a DNA sequence including a non-naturally occurring cysteine codon. The toxin moiety exhibits cytotoxic activity but fails to exhibit generalized eukaryotic cell binding, and may be used to treat medical disorders.

REFERENCES:
patent: 4468382 (1984-08-01), Bacha et al.

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