|
KMID : 0377619980630030268
|
|
Korean Jungang Medical Journal
1998 Volume.63 No. 3 p.268 ~ p.280
|
|
|
The Estrogen Receptor : Changing Concepts-Clinical Lessons from Molecular Biology-
|
|
Leon Speroff
|
|
|
Abstract
|
|
|
Instructional Objectives :
1. Explain the mechanism of action for estrogen and Progesterone receptors.
2. Describe how the mechanism of action differs comparing estrogen and
antiestrogens.
3. Understand how tamoxifen Protects against recurrent breast cancer and how
resistance to tamoxifen emerges.
4. Explain how specific estrogens can have different effects in diverse cells and
tissues.
The Molecular Structure and Function of Steroid Hormone Receptors
The history of estrogen is a modem story. The estrogen receptor was discovered
about 1960 But even before the estrogen receptor was discovered, chemists had
developed an antiestrogen. This compound, called MER-25, was evaluated for the
treatment of breast cancer, but caused neurological toxicity. Tamoxifen is a member of
this class of compounds(as is clomiphene) called triphenylethylenes.
Tamoxifen was originally discovered as part of a fertility control Program at Imperial
Chemical Industries(ICI) In England. The first tamoxifen report, in 1967, indicated an
antiestrogen effect on rat uterus. The initial excitement over a potential contraceptive
rapidly gave way to disappointment when it was discovered that tamoxifen induced
ovulation in anovulatory women. The sequence of the estrogen receptor(ER) was report
in 1986.
Estrogens Produce cellular responses by regulating gene activity. This action is
mediated by an intracellular receptor that primarily affects gene transcription, but also
regulates post-transcriptional events and non-genomic events. The estrogen receptor
belongs to a superfamily of receptors. This family now includes about 50 proteins, many
of which are called orphan receptors because a specific ligand for these proteins has not
been identified.
|
|
|
KEYWORD
|
|
|
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
|
|
|