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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.
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...
Regulation of Nuclear Protein Sorting01:45

Regulation of Nuclear Protein Sorting

Nuclear protein sorting regulates nucleus composition and gene expression, crucial for determining the fate of a eukaryotic cell. Hence, the entry and exit of molecules across the nuclear envelope is a tightly controlled process. Nuclear protein sorting can be inhibited by one of the following ways: 1) masking cargo signal sequences, 2) modifying the nuclear receptor's affinity for cargo, 3) controlling the nuclear pore size, 4) retaining the cargo during its transit to the cytosol or the...

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Related Experiment Video

Updated: Jun 11, 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

What are nuclear receptor ligands?

Frances M Sladek1

  • 1Department of Cell Biology and Neuroscience, University of California, 2115 Biological Sciences Building, Riverside, CA 92521, United States. frances.sladek@ucr.edu

Molecular and Cellular Endocrinology
|July 10, 2010
PubMed
Summary

Nuclear receptors (NRs) are crucial transcription factors regulating gene expression. This review explores the definition and evolution of NR ligands, considering historical, biological, and environmental factors.

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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

Published on: November 15, 2013

Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay
09:07

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

Published on: December 19, 2018

Area of Science:

  • Molecular Biology
  • Evolutionary Biology
  • Biochemistry

Background:

  • Nuclear receptors (NRs) are conserved transcription factors regulating gene expression in response to lipophilic compounds.
  • NRs are vital in human development, physiology, and disease, and their presence across the animal kingdom suggests evolutionary significance.
  • Emerging evidence indicates early NRs may have functioned as environmental sensors, binding external ligands.

Purpose of the Study:

  • To provide a comprehensive overview of nuclear receptor (NR) ligands.
  • To examine the definition of an NR ligand from historical, biological, and evolutionary viewpoints.
  • To establish a foundation for further research and identify new avenues for investigation into NR-ligand interactions.

Main Methods:

  • Literature review and synthesis of existing research on nuclear receptors and their ligands.
  • Analysis of historical, biological, and evolutionary data pertaining to NR ligand interactions.
  • Comparative analysis of NR ligand binding across different species and environmental contexts.

Main Results:

  • The definition of a nuclear receptor ligand has evolved from classical endocrine signaling to include environmental sensing.
  • Early nuclear receptors likely evolved to detect external environmental cues, influencing their function and specificity.
  • Understanding the diverse nature of NR ligands is critical for comprehending their roles in evolution and physiology.

Conclusions:

  • The concept of nuclear receptor ligands is multifaceted, encompassing both endogenous and exogenous compounds.
  • Evolutionary perspectives highlight the ancient role of NRs as environmental sensors, predating their classical endocrine functions.
  • Further research is needed to fully elucidate the complex interplay between nuclear receptors, their ligands, and biological systems.