The energetics of ligand binding at catecholamine receptors.
One of the key events in the actions of agonists and antagonists is their binding to receptors. Understanding this event is of interest in terms of understanding receptor function but it also has immense practical relevance for the design of drugs. If the ligand-binding process could be understood in detail, including the nature of the interactions made between ligand and receptor, then this could help in the design of more-selective drugs. The interaction of a ligand with its receptor is clearly of importance in determining the specificity of ligand action but ligand-receptor interaction also initiates the processes of signalling that are exhibited in the efficacy of ligand action. Here Philip Strange considers these events for catecholamine receptors, concentrating mostly on dopamine receptors; where necessary the discussion is widened to include other receptor systems.
Strange
P G
PG
Department of Biosciences, The University, Canterbury, UK.
D015195:Drug Design; D006860:Hydrogen Bonding; D008024:Ligands; D009154:Mutation / Q000235:genetics; D017983:Receptors, Catecholamine / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D017447:Receptors, Dopamine D1 / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D017448:Receptors, Dopamine D2 / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*
D008024:Ligands; D017983:Receptors, Catecholamine; D017447:Receptors, Dopamine D1; D017448:Receptors, Dopamine D2