A two-state model for the kinetics of competitive radioligand binding.

ABSTRACT:

Background and purpose

Ligand-receptor binding kinetics is receiving increasing attention in the drug research community. The Motulsky and Mahan model, a one-state model, offers a method for measuring the binding kinetics of an unlabelled ligand, with the assumption that the labelled ligand has no preference while binding to distinct states or conformations of a drug target. As such, the one-state model is not applicable if the radioligand displays biphasic binding kinetics to the receptor.

Experimental approach

We extended the Motulsky and Mahan model to a two-state model, in which the kinetics of the unlabelled competitor binding to different receptor states (R₁ and R₂ ) can be measured. With this extended model, we determined the binding kinetics of

SUBMITTER: Guo D 

PROVIDER: S-EPMC5913406 | biostudies-literature | 2018 May

REPOSITORIES: biostudies-literature