Receptor Binding in Drug Discovery


Receptors have formed one of the most successful classes of drug targets, with receptor‐binding analysis being a central component of drug discovery for such targets. Receptor assays are easily established in robust formats, and the advent of high‐throughput screening equipment using robotics and fast, reliable assay technology has made receptor binding one of the most reliable drug discovery technologies available.

Keywords: receptor binding; high‐throughput screening

Figure 1.

Schematic drawing illustrating some structural features found in several different membrane‐embedded receptors. These features include catalytic domains, domains common to large families of molecules (e.g. Cys‐rich, immunoglobulin, type I cytokine and ion channel domains), transmembrane regions, and serine/threonine‐rich domains used for receptor regulation by phosphorylation.

Figure 2.

Typical binding results obtained in a ligand saturation experiment. (a) A complete saturation binding experiment: square, total apparent binding; triangle, nonspecific binding; circle, specific binding derived by subtracting the nonspecific binding from the total binding. (b) A Scatchard replot of the specific binding data.

Figure 3.

Displacement binding curves illustrating three frequent situations: circle, a drug that is competitive with the labelled ligand (red curve); triangle, a drug that binds competitively to two receptor forms (sites) both of which bind the labelled ligand identically (yellow curve); square, a drug that displaces the labelled ligand but exhibits a low Hill slope (blue curve).


Further Reading

Pratt WB and Taylor P (1990) Principles of Drug Action: The Basis of Pharmacology, 3rd edn. New York: Churchill Livingstone.

Alberts B, Bray D, Lewis J et al. (1994) Molecular Biology of the Cell, 3rd edn. New York: Garland Publishing.

Hardman JG and Limbird LE (1996) Goodmans & Gilman's: The Pharmacological Basis of Therapeutics, 9th edn. San Francisco: McGraw‐Hill.

Devlin J (1998) High Throughput Screening: The Discovery of Bioactive Substances. New York: Marcel Dekker.

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Jarnagin, Kurt(Mar 2004) Receptor Binding in Drug Discovery. In: eLS. John Wiley & Sons Ltd, Chichester. [doi: 10.1038/npg.els.0000056]