Correlation between glucocorticoid receptor binding parameters, blood pressure, and body mass index in a healthy human population

Abstract

Correlation between the glucocorticoid receptor (GR) number and affinity for the ligand, as well as the relationship between these equilibrium binding parameters and body mass index, blood pressure, and age were examined in peripheral blood mononuclear cells (PBMC) of healthy human subjects. It was found that the only statistically significant correlation was that between the GR number per cell and equilibrium dissociation constant, K-d (r = 0.84, p < 0.0001). This observation implies the existence of a compensatory mechanism providing for lower GR affinity in individuals that have more receptor sites in circulating mononuclear cells and vice versa. This compensatory phenomenon together with considerable interindividual variation (GR number per cell ranging from 1391 to 15133, CV = 58.62%; and K-d from 2.5 to 98.6 nM, CV = 80.87%), reflects plasticity of the glucocorticoid system. The results pose the question of whether this compensatory mechanism observed in healthy human subjects persists in pathophysiological states associated with glucocorticoid hormone actions and suggest that tissue sensitivity to glucocorticoids could be better predicted by the sign and magnitude of the correlation between the two receptor equilibrium binding parameters than by each of them separately. Copyright (C) 2006 John Wiley & Sons, Ltd.