Adhesion G-protein-coupled receptors (GPCRs) are a major family of GPCRs, but limited knowledge their ligand regulation or structure is available1–3. Here we report that glucocorticoid stress hormones activate adhesion receptor G3 (ADGRG3; also known as GPR97)4–6, prototypical GPCR. The cryo-electron microscopy structures GPR97–Go complexes bound to the anti-inflammatory drug beclomethasone ste...

Adverse early experience impairs adult learning and memory. Previously, we showed that neonatal maternal separation impaired eyeblink conditioning in adult male rats. This impairment was correlated with increases in glucocorticoid receptor expression in the posterior region of the cerebellar interpositus nucleus, a key structure in the neural circuitry controlling eyeblink conditioning. To begi...

Measurement of glucocorticoid receptors appears to be useful for selecting which patients with leukemia and lymphoma should receive glucocorticoid therapy. To determine the effect of recent or concurrent glucocorticoid therapy on the number of measured tumor glucocorticoid receptor sites, 18 patients with leukemia and lymphoma were studied. Baseline determinations of numbers of glucocorticoid r...

OBJECTIVES To characterize glucocorticoid receptor expression in peripheral WBCs of critically ill children using flow cytometry. DESIGN Prospective observational cohort. SETTING A university-affiliated, tertiary PICU. PATIENTS Fifty-two critically ill children. INTERVENTIONS Samples collected for measurement of glucocorticoid receptor expression and parallel cortisol levels. MEASUREM...

Cortisol-activated glucocorticoid receptors modulate cellular responses to stress by translocating from the cytosol to the nucleus and enhancing or repressing the transcription of target genes. The functional capacity of mononuclear leukocytes is inhibited in parturient dairy cows at a time when blood cortisol concentrations are high. Because the glucocorticoid receptor is autoregulatory in man...

Steroid hormones exert their glucocorticoid activity by binding reversibly to a receptor protein in the cytoplasm of target cells [ 1,2]. We have shown [3] that Ca2+ inhibit the rate of association of dexamethasone, a semi-synthetic glucocorticoid, with the glucocorticoid receptor. The half-maximum effect was seen at 0.3 PM free Ca2+, a concentration within the range (0. l1 PM) of fluctuations ...

Glucocorticoid-resistant P1798 cell lines have been found to contain levels of glucocorticoid receptor comparable to receptor levels in glucocorticoid-sensitive P1798 cells. Previously, most of the P1798 resistant cells examined were found to contain low levels of glucocorticoid receptor, and this was thought to account for the resistance of these cells to glucocorticoid treatment. Resistant ce...