Inhibition by rifamycin AF/013 of thyroid hormone binding to the nuclear receptor.

Rifamycin AF/013, a potent inhibitor of nucleic acid polymerizing enzymes and of some hormone receptors, strongly inhibited thyroid hormone-binding to the isolated nuclear receptor. Fifty percent inhibition was obtained at AF/013 concentration of as low as 8 micrograms/ml. AF/013, however, only weakly promoted dissociation of the bound hormone from the receptor. The inhibitory action of AF/013 was competitive with respect to and reduced the receptor's affinity for the hormone.