Radioligand binding to intact cells as a tool for extended drug screening in a representative physiological context

Publication date: October 2015 Source:Drug Discovery Today: Technologies, Volume 17 Author(s): Georges Vauquelin, Isabelle Van Liefde, David C. Swinney Radioligand binding assays on intact cells offer distinct advantages to those on membrane suspensions. Major pharmacological properties like drug affinity and binding kinetics are more physiologically relevant. Complex mechanisms can be studied with a wider choice of experimental approaches and so provide insights into induced-fit type binding, receptor internalisation and even into pharmacomicrokinetic phenomena like drug rebinding and partitioning into the membrane. Hence, intact cell binding constitutes a valuable addition to the pharmacologist's toolbox.
Source: Drug Discovery Today: Technologies - Category: Drugs & Pharmacology Source Type: research