Receptor-ligand binding assays: Technologies and applications

LAA de Jong*, DRA Uges, JP Franke, R Bischoff, Lutea A.A. de Jong, Rainer Piet Franke

*Corresponding author for this work

Research output: Contribution to journalReview articleAcademicpeer-review

151 Citations (Scopus)

Abstract

Receptor-ligand interactions play a crucial role in biological systems and their measurement forms an important part of modem pharmaceutical development. Numerous assay formats are available that can be used to screen and quantify receptor ligands. In this review, we give an overview over both radioactive and non-radioactive assay technologies with emphasis on the latter. While radioreceptor assays are fast, easy to use and reproducible, their major disadvantage is that they are hazardous to human health, produce radioactive waste, require special laboratory conditions and are thus rather expensive on a large scale. This has led to the development of non-radioactive assays based on optical methods like fluorescence polarization, fluorescence resonance energy transfer or surface plasmon resonance. In light of their application in high-throughput screening environments, there has been an emphasis on so called "mix-and-measure" assays that do not require separation of bound from free ligand. The advent of recombinant production of receptors has contributed to the increased availability of specific assays and some aspects of the expression of recombinant receptors will be reviewed. Applications of receptor-ligand binding assays described in this review will relate to screening and the quantification of pharmaceuticals in biological matrices. (c) 2005 Elsevier B.V. All rights reserved.

Original languageEnglish
Pages (from-to)1-25
Number of pages25
JournalJournal of Chromatography B-Analytical Technologies in the Biomedical and Life Sciences
Volume829
Issue number1-2
DOIs
Publication statusPublished - 27-Dec-2005

Keywords

  • receptor-ligand binding
  • assay technologies
  • high-throughput screening
  • quantitative receptor assay
  • recombinant receptor expression
  • PROTEIN-COUPLED RECEPTORS
  • FLUORESCENCE CORRELATION SPECTROSCOPY
  • SCINTILLATION PROXIMITY ASSAY
  • SURFACE-PLASMON RESONANCE
  • BIOMOLECULAR INTERACTION ANALYSIS
  • NICOTINIC ACETYLCHOLINE-RECEPTOR
  • LIQUID-CHROMATOGRAPHIC DETERMINATION
  • ULTRAFILTRATION-MASS-SPECTROMETRY
  • INTERNAL-REFLECTION FLUORESCENCE
  • BIOSPECIFIC INTERACTION ANALYSIS

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