Cited by 522Estrogen and related hormone effectsNuclear Structure and FunctionProstate Cancer Treatment and Research

The antiestrogen ICI 182780 disrupts estrogen receptor nucleocytoplasmic shuttling

Dauvois, Sophie, White, Roger, Parker, Malcolm G.·1993·Journal of Cell Science

Abstract

The mouse estrogen receptor was shown to be constantly shuttling between the nucleus and cytoplasm although under steady-state conditions it is detected predomi-nantly in the cell nucleus in both the absence and pres-ence of estradiol. Shuttling was demonstrated by moni-toring the transfer of protein between nuclei in heterokaryons and by examining the subcellular distri-bution of mutant receptors. In the presence of the par-tial antiestrogen 4-hydroxytamoxifen the receptor was retained in the nucleus whereas it accumulated in the cytoplasm when cells were treated with the pure antie-strogen ICI 182780. The effect of the pure antiestrogen was to inhibit nucleocytoplasmic shuttling of the recep-tor by blocking its nuclear uptake. Thus although ligand binding is not required by the estrogen receptor to undergo nucleocytoplasmic shuttling, this process can be disrupted by the binding of a pure antiestrogen.

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Crossref · 10.1242/jcs.106.4.1377

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45 of 45 references verified0 citation errors · 0 not checkable

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  • ICI 182,780 is a pure anti-estrogen.

    “we treated mice with either the anti-estrogen ICI 182,780 (ICI), a “pure” anti-estrogen [17], 4,4′,4″-(4-Propyl-[1H]-pyrazole-1,3,5-triyl)trisphenol (PPT), a potent ERα agonist [18], or ditolylguanidine (DTG), a sigma-1 and −2 receptor agonist.”

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Authors
Dauvois, S., White, R., & Parker, M. G.
Affiliations
Molecular Endocrinology Laboratory, Imperial Cancer Research Fund, 44 Lincoln’s Inn Fields, London WC2A 3PX, UK
Venue
Journal of Cell Science
Published
1993-12-01
Volume
106
Issue
4
Pages
1377-1388
ISSN
  • 0021-9533 (ISSN-L)
  • 1477-9137
OpenAlex
W2147673480
Cited by
522
References
45
Citations by year
2026: 2 · 2025: 4 · 2024: 2 · 2023: 6 · 2022: 8 · 2021: 11 · 2020: 10 · 2019: 4 · 2018: 7 · 2017: 9 · 2016: 14 · 2015: 15 · 2014: 17 · 2013: 19 · 2012: 15
FWCI
7.50
Type
journal article
Language
en
Open access
closed
Locations
  • Journal of Cell Science (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nuclear Structure and Function
  • Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Prostate Cancer Treatment and Research
Keywords
estrogen receptor, fulvestrant, tamoxifen, antiestrogens, nucleocytoplasmic shuttling, nuclear uptake, subcellular localization, heterokaryons, estradiol, ligand binding, nuclear export
MeSH terms
Fulvestrant, Amino Acid Sequence, Animals, Biological Transport, Cell Compartmentation, Cell Nucleus, Cells, Cultured, Chlorocebus aethiops, Cytoplasm, Estradiol, Estrogen Antagonists, Hybrid Cells, Molecular Sequence Data, Oligomycins, Receptors, Estrogen, Recombinant Proteins, Tamoxifen, Transfection, Sequence Homology, Amino Acid, Mice, Polyunsaturated Alkamides

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