PMID: 2095212Mar 1, 1990Paper

Evaluation of iodovinyl antibody conjugates: comparison with a p-iodobenzoyl conjugate and direct radioiodination

Bioconjugate Chemistry
S W Hadley, D S Wilbur

Abstract

The preparations and conjugations of 2,3,5,6-tetrafluorophenyl 5-[125I/131I]iodo-4-pentenoate (7a) and 2,3,5,6-tetrafluorophenyl 3,3-dimethyl-5-[125I/131I]iodo-4-pentenoate (7b) to monoclonal antibodies are reported. Reagents 7a and 7b were prepared in high radiochemical yield by iododestannylation of their corresponding 5-tri-n-butylstannyl precursors. Radioiodinated antibody conjugates were prepared by reaction of 7a or 7b with the protein at basic pH. Evaluation of these conjugates by several in vitro procedures demonstrated that the radiolabel was attached to the antibody in a stable manner and that the conjugates maintained immunoreactivity. Comparative dual-isotope biodistribution studies of a monoclonal antibody Fab fragment conjugate of 7a and 7b with the same Fab fragment labeled with N-succinimidyl p-[131I]iodobenzoate (PIB, p-iodobenzoate, 2) or directly radioiodinated have been carried out in tumor-bearing nude mice. Coinjection of the Fab conjugate of 7a with the Fab conjugate of 2 demonstrated that the biodistributions were similar in most organs, except the neck tissue (thyroid-containing) and the stomach, which contained substantially increased levels of the 7a label. Coinjection of the Fab conjugate of 7a with ...Continue Reading

Citations

Jun 1, 2000·Nuclear Medicine and Biology·G W KabalkaM M Goodman
Jan 1, 1991·International Journal of Radiation Applications and Instrumentation. Part B, Nuclear Medicine and Biology·S C Srivastava, R C Mease
Oct 1, 1993·Nuclear Medicine and Biology·S GargM R Zalutsky
Apr 12, 2016·European Journal of Medicinal Chemistry·Tahra AyedNicolas Galland

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