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Function
Disease
Relevance
Structural highlights
The specific conformation of this tight loop creates part of the activation signal that will stimulate normal growth, as estradiol is a normal ligand for ER.
Tamoxifen is a drug created to bind ER and inhibit the transcription factor activity of ER. Tamoxifen is larger than the normal hormone ER binds (estradiol); for this reason the activation loop is pushed into an inactive conformation. This blocks ER from giving the signal to grow.
ER binds to DNA
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