Does a radiolabelled ligand bind to a homogeneous population of non-interacting receptor sites?
Receptor subtypes of pharmacological interest are often characterized by studies in which a particular radiolabelled ligand is competitively displaced from its binding sites, either by its unlabelled analogue (homologous displacement), or by different, unlabelled, ligands (heterologous displacement). In this article, Stéphane Swillens, Magali Waelbroeck and Philippe Champeil emphasize the fact that a single homologous displacement curve is generally unable to reveal that the radioligand binds to a heterogeneous receptor population. Overlooking this heterogeneity may, in turn, dramatically affect interpretation of heterologous displacement curves displaying more than one receptor type for the unlabelled ligand: neither the binding affinities of the ligands for the different receptors, nor the proportion of these receptors, can be estimated reliably.
Swillens
S
S
Laboratoire de Chimie Biologique et de la Nutrition, Université Libre de Bruxelles, Belgium.
Waelbroeck
M
M
Champeil
P
P
D001665:Binding Sites; D001667:Binding, Competitive; D007700:Kinetics; D008024:Ligands; D008962:Models, Theoretical; D011869:Radioligand Assay; D011956:Receptors, Cell Surface / Q000378:metabolism*
D008024:Ligands; D011956:Receptors, Cell Surface