The selective oestrogen receptor modulators idoxifene and raloxifene have fundamentally different cell-specific oestrogen-response element (ERE)-dependent/independent mechanisms in vitro.
Academic Article
Overview
Research
Identity
Additional Document Info
Other
View All
Overview
abstract
Idoxifene and raloxifene are selective oestrogen receptor modulators (SERMs) that by definition exhibit tissue-specific agonist or antagonist properties via interactions with the oestrogen receptor (ER). Idoxifene acts as an oestrogen agonist in osteoblastic cells via an ER/ERE-mediated mechanism. In contrast, raloxifene is an antagonist via the ERE in osteoblastic cells. Like the pure antagonist ICI 182,780, raloxifene inhibited the potent agonist activity of both 17beta-oestradiol and idoxifene through the ERE whereas idoxifene had no effect on the agonist activity of 17beta-oestradiol via the ERE. In breast cancer cells, both raloxifene and idoxifene were potent antagonists of ERE-mediated 17beta-oestradiol action suggesting an ERE-dependent mechanism of action for both ligands in these cells. Therefore, these SERMs exhibit cell-specific ERE-dependent and -independent mechanisms of action.
