ZIRCONIUM-RADIOLABELED, CYSTEINE ENGINEERED ANTIBODY CONJUGATES
First Claim
1. A zirconium-labelled, cysteine-engineered antibody comprising a cysteine engineered antibody (Ab) conjugated through a free cysteine amino acid to a linker (L) and a zirconium complex (Z), having Formula I:
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Ab-(L-Z)p
Iwhere p is 1 to 4;
wherein Z comprises zirconium complexed to desferrioxamine B (Df); and
wherein L-Df is selected from;
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Abstract
Antibodies are engineered by replacing one or more amino acids of a parent antibody with non cross-linked, highly reactive cysteine amino acids. Antibody fragments may also be engineered with one or more cysteine amino acids to form cysteine engineered antibody fragments (ThioFab). Methods of design, preparation, screening, and selection of the cysteine engineered antibodies are provided. Cysteine engineered antibodies (Ab) are conjugated with one or more zirconium complex (Z) labels through a linker (L) to form cysteine engineered zirconium-labeled antibody conjugates having Formula I:
Ab-(L-Z)p I
where p is 1 to 4. Imaging methods and diagnostic uses for zirconium-radiolabeled, cysteine engineered antibody conjugate compositions are disclosed.
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Citations
23 Claims
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1. A zirconium-labelled, cysteine-engineered antibody comprising a cysteine engineered antibody (Ab) conjugated through a free cysteine amino acid to a linker (L) and a zirconium complex (Z), having Formula I:
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Ab-(L-Z)p
Iwhere p is 1 to 4;
wherein Z comprises zirconium complexed to desferrioxamine B (Df); and
wherein L-Df is selected from; - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 11, 18, 20, 21, 22, 23)
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10. (canceled)
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12. (canceled)
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13. A desferrioxamine-labelled, cysteine-engineered antibody comprising a cysteine engineered antibody (Ab) conjugated through a free cysteine amino acid to a linker (L) and a desferrioxamine moiety (Df), having Formula II:
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Ab-(L-Df)p
IIwherein L-Df is selected from;
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14. (canceled)
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15. A method of making a desferrioxamine-labelled, cysteine-engineered antibody comprising comprising a cysteine engineered antibody (Ab) conjugated through a free cysteine amino acid to a linker (L) and a desferrioxamine moiety (Df), having Formula II:
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Ab-(L-Df)p
IIwherein L-Df is selected from;
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16. A method of making a zirconium-labelled, cysteine-engineered antibody comprising a cysteine engineered antibody (Ab) conjugated through a free cysteine amino acid to a linker (L) and a zirconium complex (Z), having Formula I:
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Ab-(L-Z)p
Iwhere p is 1 to 4; the method comprising complexing a zirconium reagent with a desferrioxamine-labelled, cysteine-engineered antibody comprising a cysteine engineered antibody (Ab) conjugated through a free cysteine amino acid to a linker (L) and a desferrioxamine moiety (Df), having Formula II;
Ab-(L-Df)p
IIwherein L-Df is selected from; - View Dependent Claims (17)
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19. (canceled)
Specification