Abstract Antitumor protein hybrid, having a moiety consisting of the antitumor immunoglobulin and a moiety substantially consisting of the fragment A of a diphtheria toxin, which is expressed by the following formula (I): (where Ab indicates a moiety consisting of the antitumor immunoglobulin and FA indicates a moiety substantially consisting of the fragment A of a diphtheria toxin; X is an alkylene group or phenylene group which either has or does not have a branching of 1 to 5 carbon atoms. N in the amido bond is a nitrogen atom arising from the amino group in the antitumor immunoglobulin; S 1 and S 2 are both sulfur atoms, S 2 indicating a sulfur atom arising from the disulfide bond in a diphtheria toxin; n stands for an integer of 1 to 5). This antitumor protein hybrid has remarkable and specific citotoxicity against tumor cells.
Antitumor protein hybrid, having a moiety consisting of the antitumor immunoglobulin and a moiety substantially consisting of the fragment A of a diphtheria toxin, which is expressed by the following formula (I): (where Ab indicates a moiety consisting of the antitumor immunoglobulin and FA indicates a moiety substantially consisting of the fragment A of a diphtheria toxin; X is an alkylene group or phenylene group which either has or does not have a branching of 1 to 5 carbon atoms; N in the amido bond is a nitrogen atom arising from the amino group in the antitumor immunoglobulin; S1 and S 2 are both sulfur atoms, S 2 indicating a sulfur atom arising from the disulfide bond in a diphtheria toxin; n stands for an integer of 1 to 5).
Claim 2
Dependent Claim
130 words
Antitumor protein hybrid, having a moiety consisting of the antitumor immunoglobulin and a moiety substantially consisting of the fragment A of a diphtheria toxin, which is expressed by the following formula (I): (where Ab indicates a moiety consisting of the antitumor immunoglobulin and FA indicates a moiety substantially consisting of the fragment A of a diphtheria toxin; X is an alkylene group or phenylene group which either has or does not have a branching of 1 to 5 carbon atoms; N in the amido bond is a nitrogen atom arising from the amino group in the antitumor immunoglobulin; S1 and S 2 are both sulfur atoms, S 2 indicating a sulfur atom arising from the disulfide bond in a diphtheria toxin; n stands for an integer of 1 to 5).
Claim 3
Dependent Claim
13 words
Antitumor protein hybrid according to Claim 1, wherein X is an ethylene group.
Claim 4
Dependent Claim
21 words
Antitumor protein hybrid according to Claim 1, wherein FA is a moiety consisting of the fragment A of a diphtheria toxin.
Claim 5
Dependent Claim
128 words
A process for the preparation of antitumor protein hybrid expressed by the following formula (I), (where definitions of Ab, FA, X, N, S 1 , S 2 , and n are as same as those given in case of Claim 1), which comprises the reaction of 1 to 5 amino groups of the antitumor immunoglobulin with a compound which is expressed by the following formula (II), (where X is an alkylene group or phenylene group which either has or does not have a branching of 1 to 5 carbon atoms. Y indicates Both S 1 and S 0 indicate a sulfur atom,) and the reaction of thus obtained product with the substantial fragment A of a diphtheria toxin which has at least one thiol group in the fragment.
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