Perspectives in Bioconjugate Chemistry

Introduction to bioconjugate chemistry. Part 1 Proteins: chemical modifications of proteins - history and applications; radiohalogenation of proteins - a overview of radionuclides, labeling methods and reagents for conjugate labeling; a brief survey of methods for preparing protein conjugates with dyes, haptens and cross-linking reagents. Part 2 Nucleic acids: a brief guide to nucleic acid chemistry; conjugates of oligonucleotides and modified oligonucleotides - a review of their synthesis and properties; sequence-selective DNA recognition by synthetic ligands; DNA recognition by intercalator-minor-groove binder hybrid molecules. Part 3 Synthetic polymers: conjugates of anticancer agents and polymers - advantages of macromolecular therapeutics in vivo. Part 4 Targeted antibodies: recent advances with monoclonal antibody drug targeting for the treatment of human cancer; the linkage of cytoxic drugs to monolonal antibodies for the treatment of cancer; radiolabeling of monoclonal antibodies and fragments with technetium and rhenium. Part 5 Antibody-enzyme conjugates: enhancements of the thrombolytic potency of plasminogen activators by conjugation with clot-specific monoclonal antibodies; conjugation of plasminogen activators and fibrin-specific antibodies to improve thrombolytic therapeutic agents; purifying antibody-plasminogen activator conjugates; generation of cytotoxic agents by targeted enzymes.