[HTML][HTML] Mutations in the estrogen receptor ligand binding domain discriminate between hormone-dependent transactivation and transrepression

JE Valentine, E Kalkhoven, R White, S Hoare… - Journal of Biological …, 2000 - ASBMB
The estrogen receptor (ER) suppresses transcriptional activity of the RelA subunit of nuclear
factor-κB in a hormone-dependent manner by a mechanism involving both the receptor DNA
binding domain and ligand binding domain (LBD). In this study we examine the role of the
ER LBD in mediating ligand-dependent RelA transrepression. Both ERα and ERβ inhibit
RelA in response to 17β-estradiol but not in the presence of antihormones. We have
identified residues within the ERα LBD that are responsible for receptor dimerization and …