| 摘要 |
Thiol-containing peptides can be radiolabeled with fluorine-18 (F-18) by reacting a peptide comprising a free thiol group with an F-18-bound labeling reagent which also has a group that is reactive with thiols. The resulting F-18-labeled peptide s may be targeted to a tissue of interest using bispecific antibodies or bispecific antibody fragments having on arm specific for the F-18-labeled peptide or a low molecular weight hapten conjugated to the F-18-labeled peptide, and another arm specif ic to the targeted tissue. The targeted tissue is subsequently visualized by clinincal positron emission tomography. The method for radiolabeling thiol-containing peptides with fluorine-18(F-18), comprises reacting a peptide comprising a free thiol grou p with a labelling reagent having the general formula 18F-(CH2)m-CR1,R2-(CH2)n-X, wherein: n is 0, 1 or 2; m is 0, 1 or 2; and n+m is 0, 1, or 2; X is selected from the group consisting of hydroxyl, cyano, iodide, bromide, chloride, azide, tosylate, mesylate, nosylate, triflate, unsubstituted maleimide, maleimide substituted with one or two alkyl groups, and 3-sulfo-maleimide; and R1 and R2 are the same or different and are selected from the group consisting of iodide, bromide, chloride, azide, tosylate, mesylate, nosylate, triflate, hydrogen, -CONH2, carboxyl, hydroxyl, sulfonic acid, tertiary amine, quaternary ammonium, unsubstituted maleimide, maleimide substituted with on or two alkyl groups, 3-sulfo-maleimide, unsubstituted alkyl, substituted alkyl, -COOR',-CONR'2, or COR', wherein the substituents of the substituted alkyl groups are selected from the group consisting of -CONH2, carboxyl, hydroxyl, sulfonic acid, tertiary amine and quaternary ammonium and wherein R' is a C1-C6 alkyl or phenyl.
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