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Related Concept Videos

Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

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:
Intracellular Hormone Receptors01:08

Intracellular Hormone Receptors

Lipid-soluble hormones diffuse across the plasma and nuclear membrane of target cells to bind to their specific intracellular receptors. These receptors act as transcription factors that regulate gene expression and protein synthesis in the target cell
Receptor Downregulation in MVBs01:15

Receptor Downregulation in MVBs

Multivesicular bodies (MVBs) are mature endosomes that sort ubiquitinated proteins and then fuse with lysosomes to degrade the sorted proteins. Epidermal growth factor (EGF) and its receptor (EGFR) form a complex that can be internalized through endocytosis, sorted into an MVB, and later degraded.
The EGFR can initiate signaling pathways that  lead to cell proliferation, migration, and differentiation. Overexpression of EGFR  stimulates cells to proliferate. Excessive  EGFR activation may...
The Two-State Receptor Model01:29

The Two-State Receptor Model

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 one...
Secondary Messengers in Hormone Action01:26

Secondary Messengers in Hormone Action

Water-soluble hormones cannot cross the plasma membrane, so they rely on protein receptors that span the membrane to trigger intracellular signaling pathways. These pathways then activate second messengers inside the cell, including cAMP or calcium ions.
Many hormones bind to transmembrane G protein-coupled receptors that connect to regulatory G proteins. These G proteins can then activate enzymes such as adenylyl cyclase or phospholipase C. Adenylyl cyclase converts ATP to cAMP, activating...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:

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Updated: Jul 7, 2026

Systems Biology of Metabolic Regulation by Estrogen Receptor Signaling in Breast Cancer
10:36

Systems Biology of Metabolic Regulation by Estrogen Receptor Signaling in Breast Cancer

Published on: March 17, 2016

Estrogen receptor beta: an overview and update.

Chunyan Zhao1, Karin Dahlman-Wright, Jan-Ake Gustafsson

  • 1Department of Biosciences and Nutrition, Novum, Karolinska Institutet, Huddinge, Sweden. chunyan.zhao@cnt.ki.se

Nuclear Receptor Signaling
|February 28, 2008
PubMed
Summary

The discovery of estrogen receptor beta (ERbeta) reveals distinct biological functions and gene targets compared to ERalpha. This finding opens new therapeutic avenues for ERbeta-targeted drugs.

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Systems Biology of Metabolic Regulation by Estrogen Receptor Signaling in Breast Cancer
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Area of Science:

  • Endocrinology
  • Molecular Biology
  • Genetics

Background:

  • Estrogen signaling is crucial for various physiological processes.
  • The identification of estrogen receptor beta (ERbeta) alongside ERalpha has expanded the understanding of estrogen action.
  • Tissue-specific effects of estrogens suggest differential roles for ER subtypes.

Purpose of the Study:

  • To elucidate the distinct biological functions and downstream targets of ERalpha and ERbeta.
  • To explore the implications of ERbeta's unique roles in estrogen-responsive tissues.
  • To identify potential therapeutic strategies targeting ERbeta.

Main Methods:

  • Comparative analysis of ERalpha and ERbeta expression patterns.
  • Phenotypic assessment of ERalpha and ERbeta knockout (alphaERKO and betaERKO) mice.
  • Microarray experiments to identify downstream target genes.

Main Results:

  • ERalpha and ERbeta exhibit distinct expression patterns and biological functions.
  • ERalpha and ERbeta regulate overlapping yet unique sets of downstream target genes.
  • Differential transcriptional activities of ERalpha and ERbeta were observed across various contexts.

Conclusions:

  • ERalpha and ERbeta possess unique and partially overlapping functions, contributing to tissue-specific estrogen effects.
  • The distinct roles of ERbeta suggest its potential as a therapeutic target.
  • Development of ERbeta-selective ligands shows promise for clinical applications in various indications.