Receptor Binding in Drug Discovery

Kurt Jarnagin, Roche Bioscience, Palo Alto, California, USA

Published online: March 2004

DOI: 10.1038/npg.els.0000056

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).
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 Further Reading
    book Pratt WB and Taylor P (1990) Principles of Drug Action: The Basis of Pharmacology, 3rd edn. New York: Churchill Livingstone.
    book Alberts B, Bray D, Lewis J et al. (1994) Molecular Biology of the Cell, 3rd edn. New York: Garland Publishing.
    book Hardman JG and Limbird LE (1996) Goodmans & Gilman's: The Pharmacological Basis of Therapeutics, 9th edn. San Francisco: McGraw-Hill.
    book Devlin J (1998) High Throughput Screening: The Discovery of Bioactive Substances. New York: Marcel Dekker.

Related Sub-Topics:

Drugs and the Brain | Cell Membranes | Intracellular and Extracellular Signalling | Biochemical and Biophysical Techniques | Biomolecular Interactions | Cell Signalling | Information Flow
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Article Title: Receptor Binding in Drug Discovery
 
How to Cite close
Jarnagin, Kurt(Mar 2004) Receptor Binding in Drug Discovery. In: eLS. John Wiley & Sons Ltd, Chichester. http://www.els.net [doi: 10.1038/npg.els.0000056]