Ligand-screening assays

A similar idea involves the modification of screening assays for the detection of special ligands. For example,... 

Screening of chemokine receptors has focused mostly on ligand displacement assays. These assays use a radiolabeled ligand and cells or membranes... 

Powell, K.D., Fitzgerald, M.C. High-throughput screening assay for the tunable selection of protein ligands. 

Drmota T, Greasley P, Groblewski T, Screening assays for cannabinoid ligand-GPR55 receptor binding modulators, WO 2004/074844, p. 49, 2004. 

FIGURE 6.6. Schematic depiction of the screening assay for monitoring ligand-receptor interactions on a supported fluid lipid bilayer in the presence of a library of soluble inhibitors. Surface specific observation is achieved using TIRFM. 

So far, lanthanide-based sensors have been successfully used for drug screening, assays and diagnostics as reviewed in Hemmila and Webb (1997). Sensors for pH, pC>2 and some anions (Cl-, CO32-,...) have been tested as examplified in Parker et al. (1998), Bazzicalupi et al. (2001). In the case where protonation/deprotonation of part of the ligand (in its excited state) is the sensor basis, the pKa of interest is that of the excited state, which may differ from that of the ground-state, as explained in sect. 5 (Parker et al., 1998 Blair et al., 2001). 

The products of combinatorial chemistry, namely, drug leads, instrumentation software for library data analysis, affinity ligands, etc., are all valuable and useful, because they are geared toward specific applications. For example, entire libraries have value as starting points for drug-lead screening purposes, and leads themselves are very valuable if they show desired effects in screening assays. 

Parker, G.J. et al. 2000. Development of high-throughput screening assays using fluorescence polarization nuclear receptor-ligand-binding and kinase/phosphatase assays. J. Biomol. Screen. 5, 77-88. 

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