| 摘要 |
Methods are described for conjugating radioiodinated peptides or carbohydrate structures to proteins with improved yields and qualities of conjugates. In one method, specially designed radioiodinated bifunctional peptides containing nonmetabolizable bonds such as amide bonds are coupled to cell targeting protein. In a second method, radioiodinated nonmetabolizable bifunctional peptides, which also contain aminopolycarboxylates, are coupled to protein. In a third method, radioiodinated bifunctional aminopolycarboxylates are coupled to protein. In a fourth method, a hydrazide-appended protein is coupled to a radioiodinated carbohydrate or a thiolated protein is coupled to a hydrazide-appended and radioiodinated carbohydrate. In a fifth method a monoderivatized cyanuric chloride is used to conjugate thiolated protein. Radioiodinated residualizing protein conjugates made by these methods are particularly stable in vivo and are suitable for radioimmunodetection and radioimmunotherapy. Specifically, the invention provides a peptide of the formula: ABG-[CL]-AA-[(D)-AA]m-[(D)Tyr]n-(D)-Lys-OH wherein m and n are each integers wherein n >= 1 and m + n = 3 - to - 38, with C-terminal and N-terminal amino acids adding to 5 - to - 40 AA is an amino acid (D)-AA is a D-amino acid CL is a cross linker (D)Tyr is D-tyrosine or tyramine ABG is an antibody-binding group; wherein at least one of the AA amino acids is hydrophilic, and the AA attached to the cross-linker CL can be a D- or L-amino acid provided that if the AA attached to the cross-linker is a L-amino acid, the AA is not directly attached to a tyrosine.
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