Bispecific antibodies are unique macromolecular heterobifunctional cross-linkers with two different binding specificities within a single molecule. As ideal bioconjugates, they can specifically glue any two different molecules together without the need for chemical conjugation. With this unique feature, they have immense potential in biological and immunological fields. Their applications range from immunohistochemistry, immunoassays, radioimmunodiagnosis, radioimmunotherapy, and immunotherapy. Recently, a new second generation of bispecific molecules, bispecific single chain Fv and diabodies, has been produced by DNA recombinant technology. They can be considered as the ultimate magic bullets for in vivo applications. They may theoretically improve tumor or pathogen targeting and minimize side effects, eventually replacing the full-length bispecific antibodies. Emphasizing on developmental methodology and clinical applications of bispecific antibodies, this review gives a bird's-eye view of these unique bioconjugates.
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