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Updated: Jun 26, 2026

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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
Nuclear receptors: one big family
1School of Medical Sciences, University of Aberdeen, Aberdeen, UK, Scotland.
Methods in Molecular Biology (Clifton, N.J.)
|January 2, 2009
Summary
Nuclear receptors, a superfamily of transcription factors, are activated by lipophilic molecules like hormones and vitamins. Research has significantly advanced our understanding of their structure, function, and biological roles.
Area of Science:
- Molecular Biology
- Endocrinology
- Genetics
Background:
- The cloning of steroid receptor cDNAs over 20 years ago established the nuclear receptor superfamily.
- Nuclear receptors are ligand-activated transcription factors.
- Natural ligands are lipophilic molecules including hormones, vitamins, and fatty acids.
Purpose of the Study:
- To review the progress in understanding nuclear receptors since their initial cDNA cloning.
- To highlight the crucial roles of nuclear receptors in various physiological processes.
Main Methods:
- Literature review of studies on nuclear receptor structure, function, and biology.
- Analysis of the roles of nuclear receptors as sensors of the cellular environment.
Main Results:
- Significant advancements have been made in understanding nuclear receptor structure and mechanisms of action.
- Nuclear receptors are vital for controlling development, differentiation, metabolic homeostasis, and reproduction.
Conclusions:
- The nuclear receptor superfamily plays a critical role in integrating environmental signals to regulate gene expression.
- Continued research is essential for a comprehensive understanding of these proteins and their therapeutic potential.
Related Concept Videos
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:
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
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...
Typically, signal transduction involves three...
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
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...
Similar to membrane-bound receptors, the binding of a ligand to the intracellular receptor of causes a conformational change in the...
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 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.
