Two-point kinetic experiments to quantify allosteric effects on radioligand dissociation.
Allosteric modulation of a receptor may be proved experimentally by demonstrating an altered radioligand dissociation in the presence of the allosteric modulator. Two-point kinetic experiments provide a screening-type approach to determine the delay of radioligand dissociation caused by allosteric modulation. In this article, Evi Kostenis and Klaus Mohr describe a pitfall in the data analysis that may lead to a suboptimum determination of the allosteric potency in the case of monophasic dissociations, and suggest how this problem may be resolved.
Kostenis
E
E
Laboratory of Bioorganic Chemistry, National Institutes of Health, Bethesda, MD 20892, USA.
Mohr
K
K
D000494:Allosteric Regulation; D006801:Humans; D007700:Kinetics; D008432:Mathematical Computing; D011869:Radioligand Assay; D011955:Receptors, Drug / Q000187:drug effects / Q000378:metabolism*
D011955:Receptors, Drug