Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Experiment Videos

Structure and function of the estrogen receptor

M G Parker1, N Arbuckle, S Dauvois

  • 1Imperial Cancer Research Fund, Molecular Endocrinology Laboratory, London, United Kingdom.

Annals of the New York Academy of Sciences
|June 11, 1993
PubMed
Summary
This summary is machine-generated.

Related Concept Videos

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Uterine Hemorrhage.

The North-Western medical and surgical journal·2023
Same author

Influence of reverse Trendelenburg position on aortocaval compression in obese pregnant women.

International journal of obstetric anesthesia·2015
Same author

Educational level and use of osteoporosis drugs in elderly men and women: a Swedish nationwide register-based study.

Osteoporosis international : a journal established as result of cooperation between the European Foundation for Osteoporosis and the National Osteoporosis Foundation of the USA·2012
Same author

Cognitive impairments in adult mice with constitutive inactivation of RIP140 gene expression.

Genes, brain, and behavior·2011
Same author

Kidney allograft biopsy: timing to complications.

Clinical nephrology·2010
Same author

Conditionally immortalized white preadipocytes: a novel adipocyte model.

Journal of lipid research·2007
Same journal

Multiomics Profiling During Autoimmune Demyelination Highlights a Complex Regulatory Role for Ataxin-1 in B Cells.

Annals of the New York Academy of Sciences·2026
Same journal

Global Trends in Light Pollution and Their Relationship With Socioeconomic Factors.

Annals of the New York Academy of Sciences·2026
Same journal

Wired for Corruption: Inter-Brain Synchrony Encodes Bribery-Related Value Information and Predicts Bribery Agreement.

Annals of the New York Academy of Sciences·2026
Same journal

LM-YOLO: A Lightweight Multi-Scale Enhanced Model for Forest Smoke Detection Using Unmanned Aerial Vehicles.

Annals of the New York Academy of Sciences·2026
Same journal

Polyrhythm Perception and Production: A Scoping Review.

Annals of the New York Academy of Sciences·2026
Same journal

DARTS-CNN-BiLSTM: Intelligent Fault Diagnosis for Computer Numerical Control Machine Tool Feed System.

Annals of the New York Academy of Sciences·2026
See all related articles

Pure antiestrogens like ICI 164384 and ICI 182780 disrupt estrogen receptor dimerization and promote its degradation. This occurs because their unique structure interferes with the receptor

Area of Science:

  • Molecular Endocrinology
  • Nuclear Receptor Signaling

Background:

  • The estrogen receptor (ER) hormone-binding domain is crucial for estradiol binding, homodimerization, and transcriptional activation.
  • Estrogen binding residues are implicated in dimerization, suggesting the hormone-binding pocket is near the dimer interface.
  • Specific hydrophobic and charged residues are vital for hormone-dependent transcriptional activation, conserved across nuclear receptors.

Purpose of the Study:

  • To investigate the mechanism by which pure antiestrogens ICI 164384 and ICI 182780 affect estrogen receptor turnover and function.
  • To explore the role of the antiestrogen's 7 alpha alkyl-amide extension in inhibiting receptor dimerization.

Main Methods:

  • Comparative analysis of estrogen receptor turnover in the presence of estradiol versus pure antiestrogens (ICI 164384, ICI 182780).

Related Experiment Videos

  • Hypothesizing antiestrogen binding to the ER hormone-binding pocket based on structural similarities.

    • Main Results:

    • Pure antiestrogens ICI 164384 and ICI 182780 significantly increase estrogen receptor turnover compared to estradiol.
    • Antiestrogens are proposed to inhibit receptor dimerization via their 7 alpha alkyl-amide extension.
    • Inhibition of dimerization leads to reduced nuclear uptake and accelerated cytoplasmic degradation of the estrogen receptor.

    Conclusions:

    • The 7 alpha alkyl-amide extension of pure antiestrogens is critical for disrupting estrogen receptor dimerization.
    • Antiestrogen-induced inhibition of dimerization results in decreased nuclear localization and enhanced receptor degradation.
    • This mechanism explains how pure antiestrogens function as antagonists by destabilizing the estrogen receptor complex.