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Differential SERM activation of the estrogen receptors (ERα and ERβ) at AP-1 sites by Ross V Weatherman; Nicola J Clegg; Thomas S Scanlan is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is Differential SERM activation of the estrogen receptors (ERα and ERβ) at AP-1 sites about?

Background : The selective estrogen receptor modulators (SERMs) raloxifene and tamoxifen are triphenylethylene derivatives that affect transcriptional regulation by the estrogen receptors (ERK and ERL) but show different effects in different tissues. A third triphenylethylene derivative, GW-5638, displays tissue selectivity in rats identical to that of raloxifene, suggesting that GW-5638 and raloxifene share a mechanism of action that is different from that of tamoxifen. Results: Both GW-5638 and its hydroxylated analog GW-7604 were tested for their ability to bind to ERK and ERL and their ability to affect transcription of ERK and ERL at a consensus estrogen response element and an ER/AP-1 response element. The drugs were found to have the same affinity for ERK and ERL, although they were also found to activate transcription from an AP-1 promoter element more potently with ERL than with ERK. Derivatives of GW-5638 with alterations at the carboxylic acid still showed increased ERL potency compared to ERK, but the magnitude of the activation with ERK was much higher than with ERL. Conclusions: Despite similar binding affinities to isolated ERK and ERL, GW-5638 and GW-7604 show marke

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Author

Ross V Weatherman; Nicola J Clegg; Thomas S Scanlan

Publisher

Elsevier Science; Elsevier ; Cell Press; Elsevier BV (ISSN 1074-5521)

Published

2001

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)