Use of Bifunctional Chelating Agents for Radiolabeling Antibodies
A remarkably large number of metallic ions form “stable” chelate complexes with certain organic molecules (chelators, or ligands). For example, diligent — but probably incomplete — searching of the literature reveals references to the preparation and/or thermodynamic stability constants of the chelates of about 70 different elements with the chelator EDTA (1,2). These elements (Figure 1) have a great range of properties; included are radionuclides suitable for medical diagnosis and therapy, as well as paramagnetic, chemically reactive, or luminescent metals appropriate to other applications. Since many of these elements have only moderate stability as EDTA chelates, there are good reasons to search for new chelators that will permit particular metals to be used in vivo as probes or cell-killing agents.
KeywordsHydrolysis Albumin EDTA Glycine Radionuclide
Unable to display preview. Download preview PDF.
- 1.“Stability Constants of Metal Ion Complexes,” L. G. Sillen and A. E. Martell, eds., Chemical Society, London (1964) .Google Scholar
- 2.“Critical Stability Constants,” A. E. Martell and R. M. Smith, eds., Plenum, New York (1974).Google Scholar
- 3.A. Ringbom, “Complexation in Analytical Chemistry,” Interscience, New York (1963).Google Scholar
- 5.A. White, P. Handler, and E. L. Smith, “Principles of Biochemistry,” 4th ed., p. 711, McGraw-Hill, New York (1968).Google Scholar
- 6.Reference 2, pp. 204–225.Google Scholar
- 10.D. W. Margerum, G. R. Cayley, D. C. Weatherburn, and G. K. Pagenkopf, Kinetics and Mechanisms of Complex Formation and Ligand Exchange, in “Coordination Chemistry,” Vol 2, A. E. Martell, ed., American Chemical Society, Washington, D. C. (1978).Google Scholar
- 12.M. J. Welch, and T. J. Welch, Solution chemistry of carrierfree indium, in “Radiopharmaceuticals,” pp. 73–79, G. Subramanian, B. A. Rhodes, J. F. Cooper, and V. J. Sodd, eds., Soc. Nuclear. Med., New York (1975)Google Scholar
- 14.Reference 2, pp. 281–285.Google Scholar
- 15.Reference 5, p. 711.Google Scholar
- 23.C. F. Meares, M. J. McCall, D. T. Reardan, D. A. Goodwin, C. I. Diamanti, and M. McTigue, Conjugation of Antibodies with Bifunctional Chelating Agents: Isothiocyanate and Bromoacetamide Reagents, Methods of Analysis, and Subsequent Addition of Metal Ions, Analyt. Biochem. 142: 68 (1984).PubMedCrossRefGoogle Scholar