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Biotech / Medical : Ligand (LGND) Breakout!
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To: Henry Niman who wrote (3823)6/27/1997 9:30:00 AM
From: Henry Niman   of 32384
 
Here's an earlier McDonnell/O'Malley article on regulation of estrogen and progesterone receptors:

Identification of a negative regulatory
function for steroid receptors.

McDonnell DP; Vegeto E; O'Malley BW

Ligand Pharmaceuticals, Inc., San Diego, CA 92121.

Proc Natl Acad Sci U S A 89: 10563-7 (1992)

Abstract
This report describes the identification of a negative regulator of estrogen and progesterone receptor
function. Using a reconstituted estrogen-responsive transcription system in Saccharomyces
cerevisiae, we have identified a "repressor function," which when mutated, increases the
transcriptional activity of the estrogen and progesterone receptors. In the case of the estrogen
receptor this mutation increases the sensitivity of estrogen-mediated activation by at least four orders
of magnitude. Analysis of derivatives of the estrogen receptor indicated that this repressor
specifically affects the transcription activity of the TAF1 activation domain of the estrogen receptor.
The repressor was cloned by complementation and identified as SSN6, a previously described
mediator of glucose repression in yeast. Our results indicate that SSN6 is likely to be involved also
in the repression of other cellular activators. Interestingly, deletion of the SSN6 protein allows the
antiestrogens ICI 164384 and nafoxidine to behave as more potent agonists of estrogen receptor
function, while RU486 also becomes a more potent activator of progesterone receptor function.
These data suggest that in wild-type cells the role of hormone is twofold: it promotes DNA binding
of the receptor and it also induces a conformational change in the receptor which overcomes the
effects of this repressor function.
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