ICI 164,384, a pure antagonist of estrogen-stimulated MCF-7 cell proliferation and invasiveness

E. W. Thompson, D. Katz, T. B. Shima, A. E. Wakeling, Marc E Lippman, R. B. Dickson

Research output: Contribution to journalArticle

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Abstract

Estrogen is known to stimulate the proliferation and basement membrane invasiveness of the MCF-7 human breast cancer cell line. We have compared the new steroidal antiestrogen ICI 164,384, the triphenylethylene 4-hydroxytamoxifen (OHT), and the benzothiophene LY 117018, for their effects on the proliferation and invasiveness of the MCF-7 cell line and its antiestrogen-resistant variant LY-2. While all three antiestrogens blocked the proliferative effects of 17β-estradiol on MCF-7 cells, OHT and LY 117018, but not ICI 164,384 stimulated their proliferation in the absence of estrogen. The proliferative effects of OHT and LY 117018 were blocked by ICI 164,384. Basement membrane invasiveness of MCF-7 cells was stimulated by 17β-estradiol and OHT, but not LY 117018 or ICI 164,384. Both ICI 164,384 and Ly 117018 were able to block the invasiveness induced by either 17β-estradiol or OHT. The LY-2 antiestrogen-resistant variant of the MCF-7 cell line showed increased basal proliferation, and responded only slightly to estrogen. ICI 164,384, but not OHT or LY 117018 antagonized the effects of 17β-estradiol, but did not reduce proliferation below control levels. The LY-2 line was not resistant to the antiestrogenic effects of LY 117018 or ICI 164,384 on invasiveness, and was stimulated by LY 117018 for this parameter. Thus, ICI 164,384 is a pure antiestrogen for MCF-7 cell proliferation and invasiveness, and may offer clinical advantage over nonsteroidal antiestrogens which can stimulate these activities in tumor models in vitro.

Original languageEnglish
Pages (from-to)6929-6934
Number of pages6
JournalCancer Research
Volume49
Issue number24 I
StatePublished - Dec 1 1989
Externally publishedYes

Fingerprint

LY 117018
Estrogen Antagonists
MCF-7 Cells
Estrogen Receptor Modulators
Cell Proliferation
Estradiol
Estrogens
Basement Membrane
Cell Line
ICI 164384
Breast Neoplasms

ASJC Scopus subject areas

  • Cancer Research
  • Oncology

Cite this

Thompson, E. W., Katz, D., Shima, T. B., Wakeling, A. E., Lippman, M. E., & Dickson, R. B. (1989). ICI 164,384, a pure antagonist of estrogen-stimulated MCF-7 cell proliferation and invasiveness. Cancer Research, 49(24 I), 6929-6934.

ICI 164,384, a pure antagonist of estrogen-stimulated MCF-7 cell proliferation and invasiveness. / Thompson, E. W.; Katz, D.; Shima, T. B.; Wakeling, A. E.; Lippman, Marc E; Dickson, R. B.

In: Cancer Research, Vol. 49, No. 24 I, 01.12.1989, p. 6929-6934.

Research output: Contribution to journalArticle

Thompson, EW, Katz, D, Shima, TB, Wakeling, AE, Lippman, ME & Dickson, RB 1989, 'ICI 164,384, a pure antagonist of estrogen-stimulated MCF-7 cell proliferation and invasiveness', Cancer Research, vol. 49, no. 24 I, pp. 6929-6934.
Thompson EW, Katz D, Shima TB, Wakeling AE, Lippman ME, Dickson RB. ICI 164,384, a pure antagonist of estrogen-stimulated MCF-7 cell proliferation and invasiveness. Cancer Research. 1989 Dec 1;49(24 I):6929-6934.
Thompson, E. W. ; Katz, D. ; Shima, T. B. ; Wakeling, A. E. ; Lippman, Marc E ; Dickson, R. B. / ICI 164,384, a pure antagonist of estrogen-stimulated MCF-7 cell proliferation and invasiveness. In: Cancer Research. 1989 ; Vol. 49, No. 24 I. pp. 6929-6934.
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