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Trends Pharmacol Sci. 1996 Aug;17(8):280-3.

Two-point kinetic experiments to quantify allosteric effects on radioligand dissociation.

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1
Laboratory of Bioorganic Chemistry, National Institutes of Health, Bethesda, MD 20892, USA.

Abstract

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.

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PMID:
8810873
DOI:
10.1016/0165-6147(96)10034-1
[Indexed for MEDLINE]

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