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Related Concept Videos

Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

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Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
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Target Cell Response to Hormones01:22

Target Cell Response to Hormones

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Hormones intricately bind to receptors on the surface or within target cells, initiating a cascade of cellular responses.
Notably, the cellular response can be regulated by altering the number of receptors expressed in the cell. For example, prolonged exposure to elevated hormone levels results in a gradual decline or down-regulation in the number of receptors for that specific hormone on the cell surface. Conversely, in response to low hormone levels, cells may use up-regulation, producing an...
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Internal Receptors01:31

Internal Receptors

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Many cellular signals are hydrophilic and therefore cannot pass through the plasma membrane. However, small or hydrophobic signaling molecules can cross the hydrophobic core of the plasma membrane and bind to internal, or intracellular, receptors that reside within the cell. Many mammalian steroid hormones use this mechanism of cell signaling, as does nitric oxide (NO) gas.
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Types of Receptors: Internal Receptors01:07

Types of Receptors: Internal Receptors

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Many cellular signals are hydrophilic and cannot pass through the plasma membrane. However, small or hydrophobic signaling molecules can cross the hydrophobic core of the plasma membrane and bind intracellular receptors that reside within the cell cytoplasm or nucleus. Many mammalian steroid hormones and nitric oxide (NO) gas use this cell signaling mechanism.
Similar to membrane-bound receptors, the binding of a ligand to the intracellular receptor of causes a conformational change in the...
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Signal Transduction: Overview01:26

Signal Transduction: Overview

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Cells respond to many types of information, often through receptor proteins positioned on the membrane. They respond to chemical signals, such as hormones, neurotransmitters, and other signaling molecules, initiating a series of molecular reactions to produce an appropriate response. This is called signal transduction. Cells also coordinate different responses elicited by the same signaling molecule via mediators, allowing molecular cross-talk.
Typically, signal transduction involves three...
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The Two-State Receptor Model01:29

The Two-State Receptor Model

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The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
The binding affinity of a drug determines its interaction with...
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Related Experiment Video

Updated: Sep 5, 2025

Screening for Phytoestrogens using a Cell-based Estrogen Receptor &#946; Reporter Assay
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Screening for Phytoestrogens using a Cell-based Estrogen Receptor β Reporter Assay

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Estrogens: Two nuclear receptors, multiple possibilities.

Anna Biason-Lauber1, Mariarosaria Lang-Muritano2

  • 1University of Fribourg, Division of Endocrinology, Chemin du Musée 5, 1700, Fribourg, Switzerland.

Molecular and Cellular Endocrinology
|July 5, 2022
PubMed
Summary

Estrogen receptors alpha and beta are crucial for human health and development. This review details their roles, mechanisms, and the clinical impact of estrogen resistance, particularly highlighting new findings on beta-receptor defects.

Keywords:
ESR2)Estrogen receptor genes (ESR1Estrogen resistanceEstrogen α-receptorEstrogen β-receptorGonadal development

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Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay

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Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
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Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists

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Related Experiment Videos

Last Updated: Sep 5, 2025

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Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay
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Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay

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Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
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Area of Science:

  • Endocrinology
  • Molecular Biology
  • Genetics

Background:

  • Estrogen signaling is vital in both animal models and human physiology.
  • Estrogen exerts its effects through two main receptors: estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ).
  • Dysregulation of estrogen signaling is implicated in various human pathologies, including osteoporosis.

Purpose of the Study:

  • To review the structure, mechanisms of action, and tissue-specific roles of ERα and ERβ.
  • To explore the clinical manifestations of estrogen resistance arising from estrogen receptor gene variants.
  • To present novel findings on ERβ defects and their impact on human development and health.

Main Methods:

  • Literature review of estrogen action in animal models and humans.
  • Analysis of clinical data pertaining to estrogen receptor gene variants.
  • Case study focusing on long-term follow-up of women with ERα and ERβ resistance.

Main Results:

  • Estrogen receptors α and β exhibit distinct structures and mechanisms of action across various tissues.
  • Estrogen resistance, caused by ER gene variants, presents diverse clinical pictures in both men and women.
  • A novel case of a woman with a β-receptor defect expands the known spectrum of estrogen resistance.

Conclusions:

  • ERβ plays an essential role in gonad development.
  • Understanding estrogen resistance is critical for managing associated pathologies.
  • Further research is needed to elucidate the complex interactions between ERα and ERβ in bone metabolism and the hypothalamic-pituitary-gonadal axis.