The antagonists RU486 and ZK98299 stimulate progesterone receptor binding to deoxyribonucleic acid in vitro and in vivo, but have distinct effects on receptor conformation.
作者： Elizabeth K. Gass , Susan A. Leonhardt , Steven K. Nordeen , Dean P. Edwards
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摘要: Three types of transfection experiments were used to detect the abilities different classes antagonists stimulate binding progesterone receptor (PR) response elements (PRE) in intact mammalian cells. These included a promoter interference assay, which PR PREs positioned between TATA box and start transcription is detected as reduction expression constitutively active reporter gene, competition antagonist glucocorticoid agonist for common element/PRE-controlled construct, activation chimeric (PR-VP16) containing constitutive trans-activation domain derived from VP16 protein herpes simplex virus. By each approach, all tested equally effective stimulating cell. This previously designated type I (ZK98299) II (RU486, ZK98734, ZK112993) 11β-aryl substituted steroid analogs. Stimulation t...
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