Repression of glucocorticoid receptor function by the anti-rheumatic gold compound aurothiomalate

We describe functional interaction between the anti-rheumatic water-soluble gold compound aurothiomalate and glucocorticoid receptors. Aurothiomalate contains gold in the Au(I) state, and Au(I) alone, not thiomalate or malate, reduced the ligand-binding activity of the glucocorticoid receptor. Au(I) also interfered with the productive interaction between the glucocorticoid receptor and the cognate target DNA sequences and repressed the transactivation function of the receptor. Thus, Au(I) variably modulates glucocorticoid receptor-mediated intracellular signals.