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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:
Signal Transduction: Overview01:26

Signal Transduction: Overview

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...
Internal Receptors01:31

Internal Receptors

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.
Types of Receptors: Internal Receptors01:07

Types of Receptors: Internal Receptors

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...
Ligand Binding Sites02:40

Ligand Binding Sites

Proteins are dynamic macromolecules that carry out a wide variety of essential processes; however, the activities of most proteins depend on their interactions with other molecules or ions, known as ligands.
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...
Ligand Binding Sites02:40

Ligand Binding Sites

Proteins are dynamic macromolecules that carry out a wide variety of essential processes; however, the activities of most proteins depend on their interactions with other molecules or ions, known as ligands.
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...

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Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
10:51

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

Published on: November 15, 2013

Endogenous ligands for nuclear receptors: digging deeper.

Michael Schupp1, Mitchell A Lazar

  • 1Department of Endocrinology, Diabetes, and Nutrition and Center for Cardiovascular Research, Institute of Pharmacology, Charité-University Medicine Berlin, 10115 Berlin, Germany. michael.schupp@charite.de

The Journal of Biological Chemistry
|October 20, 2010
PubMed
Summary

Identifying endogenous ligands for nuclear receptors (NRs) is crucial for understanding their biology. This review updates progress on ligands for peroxisome proliferator-activated receptors and Rev-erbα, potentially aiding therapeutic drug development.

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Detection of Ligand-activated G Protein-coupled Receptor Internalization by Confocal Microscopy

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Last Updated: Jun 7, 2026

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
10:51

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

Published on: November 15, 2013

Detection of Ligand-activated G Protein-coupled Receptor Internalization by Confocal Microscopy
10:24

Detection of Ligand-activated G Protein-coupled Receptor Internalization by Confocal Microscopy

Published on: April 9, 2017

Area of Science:

  • Molecular Biology
  • Endocrinology
  • Pharmacology

Background:

  • Nuclear receptors (NRs) are critical transcription factors that mediate cellular responses to hormones and dietary signals.
  • Understanding the endogenous ligands for orphan NRs is essential for elucidating their biological functions.
  • A specific cluster of NRs, including peroxisome proliferator-activated receptors (PPARs) and Rev-erbα, share high sequence homology.

Purpose of the Study:

  • To provide an updated overview of recent advancements in identifying endogenous ligands for PPARs (α and γ) and Rev-erbα.
  • To highlight the physiological relevance of these identified ligands.
  • To explore the potential for developing new therapeutic strategies based on this knowledge.

Main Methods:

  • Literature review of recent research on nuclear receptor ligand identification.
  • Focus on studies concerning peroxisome proliferator-activated receptors α and γ, and Rev-erbα.
  • Analysis of the physiological roles and implications of identified endogenous ligands.

Main Results:

  • Significant progress has been made in identifying endogenous ligands for PPARs and Rev-erbα.
  • The nature and physiological actions of these ligands are becoming increasingly understood.
  • This growing knowledge base offers new avenues for therapeutic interventions.

Conclusions:

  • The identification and characterization of endogenous ligands for NRs like PPARs and Rev-erbα are advancing our understanding of their roles.
  • This research holds promise for the development of novel drugs targeting these nuclear receptors.
  • Further investigation into NR-ligand interactions can unlock new therapeutic opportunities.