Polyvalent ligand

G. Thoma, A. G. Katopodis, N. Voelcker, R. O. Duthaler, and M. B. Streiff, Novel glycodendrimers self-assemble to nanoparticles which function as polyvalent ligands in vitro and in vivo, Angew. Chem. Int. Ed., 41 (2002) 3195-3198. 

Self-assembly of such dendrimers is a dynamic equilibrium process (Fig. 8.9). Conceivably, the non-covalent polyvalent ligands can be optimised with regard to their size and shape in the presence of natural multivalent receptors, as a kind of template for their own multivalent inhibitor, and thus open up a range of physiologically relevant polyvalent interactions [40 a]. 

Figure 9.1 The variation in cation species (as % of the total cation concentration) with the pK of formation of a 1 1 complex in the absence of competing anions. Curve set (a) pH 4, total cation to monovalent ligand ratio = 1 1000 (b) pH 4, total cation to polyvalent ligand ratio = 1 1000 (c) pH 4, total cation to monovalent ligand ratio =1 1.

G4. Gibbons, I., Hanlon, T. M., Skold, C. N., Russell, M. E., and Ullman, E. F., Enzyme-enhancement immunoassay A homogeneous assay for polyvalent ligands and antibodies. Clin. Chem. 27, 1602-1606 (1981). 

The simultaneous interaction of multiple saccharide epitopes of polyvalent ligands with oligomeric receptors can lead to interactions of high functional affinity when the orientation of the saccharide recognition elements corresponds to that of the receptor (O Fig. 8). The mechanism of affinity increase is often described as the chelate effect [52,53]. This idea is... 

PS-supported l,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD) was used as a polyvalent ligand for the Cu-catalyzed Huisgen reactions (Coelho et al., 2010) (Scheme 4.18). The three-component synthesis of 1,2,3-triazoles was successfully achieved under the same conditions. However, the catalytic system was less active, maybe due to its low catalyst loading. 

Coelho, A., Diz, R, Caamano, O., and Sotelo, E. 2010. Polymer-supported 1,5,7-tiiazabicy-clo[4.4.0]dec-5-ene as polyvalent ligands in the copper-catalyzed Huisgen J,3-dipolar cycloaddition. A(iv. Synth. Catal. 352(7) 1179-1192. 

Polyvalent Ligands Polymeric Drugs for the Sequestration of Macromolecular Pathogens... 

Polyvalent Ligands as Antiviral Agents. The use of polyvalent ligands to inhibit viral infection is the most extensively studied of all polyvalent interactions. This platform has in fact served as the protot5 ical system to validate the fundamental concept of polyvalent ligands as a new class of polymeric pharmaceutical agents. 

Although a wealth of information is available through in vitro studies, in vivo assays exhibiting the success of these polyvalent ligands in protecting animals against influenza infection has yet to be demonstrated. The success of this approach to develop antiviral agents for influenza would also depend on their favorable toxicity and activity profile in vivo. 

Here, n is the valency number, F is statistical factor defined by the system, and s = 30/(interreceptor distance (A)). An application is illustrated by a monovalent P trisaccharide ligand, which binds to pentavalent Shiga toxin (AB5) with a Ka of 10 M . If this monovalent ligand is converted to a polyvalent ligand through conjugation to polyacrylamide, a binding constant can be estimated for the multivalent interaction with the toxin pentamer as follows in (8). 

Fig. 8 Schematic representation of the sequestration of C. difficile toxin hy the polyvalent ligand...

Table 4 Representative examples of polyvalent ligands as influenza virus inhibitors...

Schengrund, C.-L., and Ringler, N. J., 1989, Binding of Vibrio cholerae toxin and the heat-labile enterotoxin of Escherichia coli to G, derivatives of G, and nonlipid oligosaccharide polyvalent ligands, J. Biol. Chem. 264 13233-13237. 

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