Inoue A, Higashi Y, Yukioka M, Morisawa S
Department of Biochemistry, Osaka City University Medical School.
J Biochem. 1987 Dec;102(6):1365-70. doi: 10.1093/oxfordjournals.jbchem.a122182.
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.
利福霉素AF/013是核酸聚合酶和某些激素受体的强效抑制剂，能强烈抑制甲状腺激素与分离出的核受体的结合。在AF/013浓度低至8微克/毫升时即可达到50%的抑制率。然而，AF/013仅能微弱地促进结合的激素从受体上解离。AF/013的抑制作用具有竞争性，降低了受体对激素的亲和力。
