help button home button Endocrine Society Endocrinology
HOME HELP FEEDBACK SUBSCRIPTIONS ARCHIVE SEARCH TABLE OF CONTENTS
This Article
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 Download to citation manager
Right arrow Request Copyright Permission
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Scholl, S. M.
Right arrow Articles by Lippman, M. E.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Scholl, S. M.
Right arrow Articles by Lippman, M. E.

Endocrinology, Vol 113, 611-617, Copyright © 1983 by Endocrine Society

ARTICLES

Antiestrogenic effects of LY 117018 in MCF-7 cells

SM Scholl, KK Huff and ME Lippman

LY 117018 is a nonsteroidal compound which has been shown to antagonize more effectively than tamoxifen the effects of estradiol in rats and mice. We have further defined the properties of this compound on cell growth and progesterone receptor (PR) induction and have compared inhibitory effects to relative binding affinity in a human breast cancer cell line. In MCF-7 cells, LY 117018 [( 6-hydroxy-2-(p- hydroxyphenyl)-benzo(b) thien-3-yl-p-(2-(pyrrolidinyl)ethoxy phenyl ketone] is devoid of estrogenic effects, has a greater affinity for the estrogen receptor (ER) than tamoxifen at 4 C, and is 100-1000 times more potent than tamoxifen at inhibiting cell growth. While tamoxifen has been reported to induce PR, a purported estrogen effect, the LY 117018 compound failed to induce PR using a broad range of concentrations. The direct antagonistic effect of LY 117018 was demonstrated by the use of varying concentrations of LY 117018 and estradiol concomitantly. We conclude that LY 117018 is a very effective antiestrogen devoid of any stimulatory effects among these parameters tested.


This article has been cited by other articles:


Home page
 Cancer Res.Home page
N. Suh, A. L. Glasebrook, A. D. Palkowitz, H. U. Bryant, L. L. Burris, J. J. Starling, H. L. Pearce, C. Williams, C. Peer, Y. Wang, et al.
Arzoxifene, a New Selective Estrogen Receptor Modulator for Chemoprevention of Experimental Breast Cancer
Cancer Res., December 1, 2001; 61(23): 8412 - 8415.
[Abstract] [Full Text] [PDF]

Home page
 Pharmacol. Rev.Home page
J. I. Macgregor and V. C. Jordan
Basic Guide to the Mechanisms of Antiestrogen Action
Pharmacol. Rev., June 1, 1998; 50(2): 151 - 196.
[Abstract] [Full Text] [PDF]

Home page
 ScienceHome page
A Kasid, M. Lippman, A. Papageorge, D. Lowy, and E. Gelmann
Transfection of v-rasH DNA into MCF-7 human breast cancer cells bypasses dependence on estrogen for tumorigenicity
Science, May 10, 1985; 228(4700): 725 - 728.
[Abstract] [PDF]


HOME HELP FEEDBACK SUBSCRIPTIONS ARCHIVE SEARCH TABLE OF CONTENTS
Endocrinology Endocrine Reviews J. Clin. End. & Metab.
Molecular Endocrinology Recent Prog. Horm. Res. All Endocrine Journals
Copyright © 1983 by The Endocrine Society