title: Radioligand binding to intact cells as a tool for extended drug screening in a representative physiological context.
abstract: 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.
authors.affiliation: Dept. of Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel, Pleinlaan 2, 1050 Brussels, Belgium. Electronic address: gvauquel@vub.ac.be.
authors.forename: Georges
authors.initials: G
authors.lastname: Vauquelin
authors.affiliation: Dept. of Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel, Pleinlaan 2, 1050 Brussels, Belgium.
authors.forename: Isabelle
authors.initials: I
authors.lastname: Van Liefde
authors.affiliation: Institute for Rare and Neglected Diseases Drug Discovery, 897 Independence Ave, Suite 2C, Mountain View, CA 94043, United States.
authors.forename: David C
authors.initials: DC
authors.lastname: Swinney
mesh_terms: D000818:Animals; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008024:Ligands; D004364:Pharmaceutical Preparations / Q000378:metabolism*; D011485:Protein Binding; D011506:Proteins / Q000378:metabolism*; D011869:Radioligand Assay
chemical_list: D008024:Ligands; D004364:Pharmaceutical Preparations; D011506:Proteins