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We report the proof-of-concept of a bioaffinity format designed for the early detection of growth hormone secretagogue receptor (GHS-R1a) antagonists in urine samples. We exploit here their atypical behavior in competitive experiments with labelled ghrelin (GHR), namely the strong promoting effect on the GHR/ GHS-R1a interaction at low molar ratios GHR/antagonist. The antago-nists potentiate the GHR/GHS-R1a interaction and they display the same effect on the interaction of GHS-R1a with other agonists listed as doping agents. The developed assay allows the estimation of affinity constants of ligand/receptor and antagonist/receptor binding and is amenable to optical, electrochemical and mass-sensitive detection. The estimated affinity constants for GHR/GHS-R1a and antagonist/GHS-R1a in the absence of G proteins are in good agreement with recently reported data.
This article was published in the following journal.
Name: Analytical chemistry
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