Early Detection of Growth Hormone Secretagogue Receptor Antagonists Exploiting Their Atypical Behavior in Competitive Assays | Zendy

George-Mădălin Dănilă | Zendy; Mihaela Puiu | Zendy; Lucian-Gabriel Zamfir | Zendy; Camelia Bala | Zendy

Open Access

Early Detection of Growth Hormone Secretagogue Receptor Antagonists Exploiting Their Atypical Behavior in Competitive Assays

Author(s) -

George-Mădălin Dănilă,

Mihaela Puiu,

Lucian-Gabriel Zamfir,

Camelia Bala

Publication year - 2019

Publication title -

analytical chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.117

H-Index - 332

eISSN - 1520-6882

pISSN - 0003-2700

DOI - 10.1021/acs.analchem.9b03845

Subject(s) - chemistry , ghrelin , antagonist , receptor , secretagogue , growth hormone secretagogue receptor , growth hormone receptor , competitive antagonist , g protein coupled receptor , biophysics , hormone , biochemistry , growth hormone , biology

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 labeled ghrelin (GHR), namely, the strong promoting effect on the GHR/GHS-R1a interaction at low molar ratios GHR/antagonist. The antagonists 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.

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