The analysis of hormone-receptor interaction. Theoretical and practical aspects
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Abstract
Detailed description of modern methodological approaches for the analysis of the hormone-receptor interaction is presented. Concise and comprehensive theoretical bases for such investigations as well as definitie practical recommendations for experimental design and performance are given. We cover here questions concerning methodology for the determination of basic characteristics of the interaction between low-molecular weight ligands and their receptors: specific (nonspecific) binding, type of interaction, affinity constants, receptor quantity, and ligand specificity. Numerous examples of theoretical relationships and experimental results are clearly illustrated by a number of graphics. The lecture is intended not only for the experts directly engaged in the research of molecular aspects of hormone perception and signaling, but also for a wide range of readers interested in the topic of hormonal regulation in eukaryotes.
Key words
hormone ligand receptor hormone-receptor interaction affinity constants ligand specificity radioligand methodAbbreviations and designations
- L (U, F)
unbound (free) ligand (hormone)
- L*
labeled ligand
- R
receptor
- [LT], [RT]
total concentrations of ligand and of receptor-binding sites
- LR (B)
ligand-receptor complex (bound hormone)
- BS
specific binding
- BT
total binding
- BNS
nonspecific binding
- IC50
concentration of unlabeled ligand suppressing binding of labeled ligand by 50%
- KD
equilibrium dissociation constant
- KA
equilibrium association constant
- K1
equilibrium constant of inhibition
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