Libraries receptor-ligand interactions

Nestler HP, Wennemers H, Sherlock R, Dong DLY, Microautoradiographic identification of receptor-ligand interactions in bead-supported combinatorial libraries, Bioorg. Med. Chem. Lett., 6 1327-1330, 1996. 

Template-directed synthesis has also been exploited for combinatorial purposes in which a reversible reaction and the use of thermodynamic templates have been used. Two different processes have been envisaged and validated, both of which consider the dynamic optimization of a receptor-ligand interaction where one of the partners is the template that drives the self-assembly of a reversible library of other partners from which the best binder for the template is selected (Fig. 8.53). If the receptor is a template, a library made using a reversible reaction is incubated with the receptor and... 

Array-Based Techniques for Glycans Development and Applications Peptide Combinatorial Libraries Transcript Profiling Receptor-Ligand Interactions... 

The use of on-hne affinity CE-MS is an early example of a direct detection approach [33]. The receptor is present in the electrophoresis bnffer and the library of ligands is injected as the sample. Ligands that show relatively strong binding to the receptor are retained and can thrrs be separated from compotmds that do not interact. The on-line MS detection allows direct characterization of the interacting ligands. 

Another technique of single-bead, direct deconvolution is based on on-bead screening. When the biological assay can be run in this format, each library component is tested as resin bound in an assay medium where a soluble receptor is present and the receptor/ligand, or inhibitor, interaction takes place at the surface of the bead. After the biological assay a few positive beads are identified, usually through colorimetric, fluorescent, or radiolabeled detection. They are removed from the assay medium and characterized analytically after washing off the receptor. This technique was first described by Lam et al. [78], has since been... 

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