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                                                   Bioconjugate Chemistry






              Claude F. Meares
              University of California, Davis



               I. Chemical Principles
              II. Multiple Sites of Chemical Conjugation:
                 Mathematics of Random Labeling
              III. Molecular Cloning: Modern Preparative
                 Methodology
              IV. Analysis of Bioconjugates
              V. Nomenclature
             VI. Examples








              GLOSSARY                                            molecule. For example, biotin binds strongly to the
                                                                  proteins avidin and streptavidin. Biotin may be con-
              Antibody A large protein molecule that binds reversibly  jugated  to  other  molecules  (see  Fig.1),  which  can
                and with high specificity to a small molecule or a spe-  then be trapped by binding to immobilized avidin or
                cific region (epitope) of a macromolecule.         streptavidin.
              Bioconjugate Generally, a synthetic substance in which  Liposome  A particle composed of multiple phospholipid
                a functional biological molecule is conjugated (linked)  molecules, arranged in a bilayer structure to enclose a
                to another substance with useful properties. The latter  small aqueous space (see Fig. 2).
                may be another biological molecule, a synthetic poly-  ODN  An oligodeoxynucleotide, a short, synthetic frag-
                mer, a small molecule, or even a macroscopic particle  ment of deoxyribonucleic acid (DNA).
                or a surface.                                   PEG Poly(ethylene glycol), also called PEO, poly(ethy-
              Enzyme Aprotein(ornucleicacid)thatcatalyzesachem-   lene oxide) (see Fig. 3). The degree of polymerization
                ical reaction, such as hydrolysis of a peptide bond.  n is usually specified according to the average number
              Epitope A molecular group, part of a larger molecule,  of CH 2 CH 2 units in a polymer molecule.
                recognized by an antibody or other binding macro-
                molecule. Typically, a small number of amino acid
                residues in a particular geometric arrangement on the  BIOCONJUGATE CHEMISTRY involves the joining of
                surface of a protein.                           two molecular functions by chemical or biological means.
              Hapten A small molecule recognized by an antibody or  This includes, among other topics, the conjugation of
                other binding macromolecule. Sometimes referred to  antibodies, nucleic acids, lipids, carbohydrates, or other
                as a ligand. A hapten may be conjugated to another  biologically active molecules with each other or with other



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