Boron-Rich Oligophosphates — Novel Molecules for Use in BNCT
For some time we1,2 and others3,4 have been interested in the use of immunoproteins for the selective localization of boron-10 in tumors. A significant challenge inherent in this approach is the requirement that each immunoprotein must be conjugated to (or otherwise associated with) approximately 103 boron-10 atoms in order to attain the necessary tumor concentrations of boron-10. Early work suggested that the development of methods for the facile synthesis of macromolecules containing large numbers of boron atoms, which we call ‘trailer’ molecules, would be necessary for the successful application of this approach to BNCT.5,6 Our research in this area has been focused upon the design of boron-rich trailers that are simple and economical to synthesize, water soluble, and homogeneous.
KeywordsBoron Atom Boron Neutron Capture Therapy Anionic Phosphate Automate Synthesis Tumor Concentration
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- 2.Goldenberg, D.M., Sharkey, R.M., Primus, F.J., Mizusawa, E.A., Hawthorne, M.F., Neutron-Capture Therapy of Human Cancer: In Vivo Results on Tumor Localization of Boron-10-Labeled Antibodies to Carcinoembryonic Antigen in the GW-39 Tumor Model System, Proc. Natl. Acad. Sci. 81: 560–565, 1984.PubMedCrossRefGoogle Scholar
- 3.Barth, R.F., Alam, F., Soloway, A.H., Adams, D.H., Steplewski, Z., Boronated Monoclonal Antibody 17–1A for Potential Neutron Capture Therapy of Colorectal Cancer, Hybridoma 5, Suppl. 1: S43, 1986.Google Scholar
- 4.Barth, R.F., Mafune, N., Alam, F., Adams, D.H., Soloway, A.H., Makroglou, G.E., Oredipe, O.A., Blue, T.E., Steplewski, Z., Conjucation, Purification and Characterization of Boronated Monoclonal Antibodies for Use in Neutron Capture Therapy, Strahlenther. Oncol. 165: 142, 1989.Google Scholar
- 6.Hawthorne, M.F., Biochemical Applications of Boron Cluster Chemistry, Pure Appl. Chem. 63(3):327330, 1991.Google Scholar
- 7.Varadarajan, A., Hawthorne, M.F., Novel Carboranyl Amino Acids and Peptides: Reagents for Antibody Modification and Subsequent Neutron Capture Studies, Bioconjugate Chemistry 2: 242–253, 1991.Google Scholar
- 12.Gait, M. J., ed. “Oligonucleotide Synthesis: A Practical Approach,” IRL, Ltd., Oxford, 1984.Google Scholar
- 14.Kane, R.R., Kim, Y.-S., unpublished results. Google Scholar