Skip Navigation

This Article
Right arrow Print PDF (4197K)
Right arrow A corrigendum has been published
Right arrow Alert me when this article is cited
Right arrow Alert me if a correction is posted
Services
Right arrow Email this article to a friend
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Add to My Personal Archive
Right arrow Download to citation manager
Right arrowRequest Permissions
Right arrow Commercial Re-use Guidelines
for Open Access NAR Content
Google Scholar
Right arrow Articles by Arbuckle, N. D.
Right arrow Articles by Parker, M. G.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Arbuckle, N. D.
Right arrow Articles by Parker, M. G.
Social Bookmarking
Add to CiteULike   Add to Connotea   Add to Del.icio.us  
What's this?

Nucleic Acids Research, 1992, Vol. 20, No. 15 3839-3844
© 1992

MOLECULAR BIOLOGY

Effect of antioestrogens on the DNA binding activity of oestrogen receptors in vitro

Nicola D. Arbuckle, Sophie Dauvois and Malcolm G. Parker*

Molecular Endiocironology Laboratory, Imperial Cancer Research Fund 44 Lincoln's Inn Fields, London WC2A 3PX, UK

*To whom correspondence should be addressed

Received June 3, 1992. Revised July 7, 1992. Accepted July 7, 1992.

We have investigated the effect of a series of steroidal oestrogen antagonists, related to ICI 164,384, on the DNA binding activity of mouse oestrogen receptors expressed in insect cells. The analogues possess different side chains at the 7-position of the B ring In the steroid. Inhibition was observed when the length of the side-chain was 15-16 carbon atoms but not 10 or 20 carbon atoms and only when the 7a isomer was used. The DNA binding activity of receptors expressed in COS-1 cells was also inhibited after extended periods of incubation with antioestrogens but not that of the human receptor in breast cancer cell-extracts. We have proposed that ICI 164,384 might disrupt receptor dimerisatlon, and therefore the variation in its ability to inhibit DNA binding activity may reflect differences in dimer stability. Since the DNA binding activity of in vitro translated receptors was inhibited when they were translated in the presence of the antioestrogen we suggest that ICI 164,384 might prevent the formation of receptor dimers without necessarily being able to disrupt preformed dimers.


Add to CiteULike CiteULike   Add to Connotea Connotea   Add to Del.icio.us Del.icio.us    What's this?


This article has been cited by other articles:


Home page
 Am. J. Physiol. Cell Physiol.Home page
N. Kanda and S. Watanabe
17{beta}-Estradiol enhances heparin-binding epidermal growth factor-like growth factor production in human keratinocytes
Am J Physiol Cell Physiol, April 1, 2005; 288(4): C813 - C823.
[Abstract] [Full Text] [PDF]

Home page
 J. Biol. Chem.Home page
B. J. Cheskis, S. Karathanasis, and C. R. Lyttle
Estrogen Receptor Ligands Modulate Its Interaction with DNA
J. Biol. Chem., April 25, 1997; 272(17): 11384 - 11391.
[Abstract] [Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
V. A. Dipippo and C. A. Powers
Tamoxifen and ICI 182,780 Interactions with Thyroid Hormone in the Ovariectomized-Thyroidectomized Rat
J. Pharmacol. Exp. Ther., April 1, 1997; 281(1): 142 - 148.
[Abstract] [Full Text]

Home page
 J. Biol. Chem.Home page
H. Wang, G. A. Peters, X. Zeng, M. Tang, W. Ip, and S. A. Khan
Yeast Two-hybrid System Demonstrates That Estrogen Receptor Dimerization Is Ligand-dependent in Vivo
J. Biol. Chem., October 6, 1995; 270(40): 23322 - 23329.
[Abstract] [Full Text] [PDF]

Home page
 J. Cell Sci.Home page
S Dauvois, R White, and M. Parker
The antiestrogen ICI 182780 disrupts estrogen receptor nucleocytoplasmic shuttling
J. Cell Sci., January 12, 1993; 106(4): 1377 - 1388.
[Abstract] [PDF]

Home page
 Proc. Natl. Acad. Sci. USAHome page
M. W. Dudley, C. Q. Sheeler, H. Wang, and S. Khan
Activation of the human estrogen receptor by the antiestrogens ICI 182,780 and tamoxifen in yeast genetic systems: Implications for their mechanism of action
PNAS, March 28, 2000; 97(7): 3696 - 3701.
[Abstract] [Full Text] [PDF]


Disclaimer: Please note that abstracts for content published before 1996 were created through digital scanning and may therefore not exactly replicate the text of the original print issues. All efforts have been made to ensure accuracy, but the Publisher will not be held responsible for any remaining inaccuracies. If you require any further clarification, please contact our Customer Services Department.