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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.
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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.
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Related Experiment Video

Updated: May 13, 2026

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

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 and their selective pharmacologic modulators.

Thomas P Burris¹, Laura A Solt, Yongjun Wang

¹The Scripps Research Institute, 130 Scripps Way 2A1, Jupiter, FL 33458, USA. tburris@scripps.edu

Pharmacological Reviews

|March 5, 2013

Summary

Selective nuclear receptor modulators offer precise therapeutic control by targeting specific tissues or genes. This review explores the development and pharmacology of these advanced receptor modulators.

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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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Published on: November 15, 2013

In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues

In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues

Published on: March 21, 2017

Area of Science:

Molecular Biology
Pharmacology
Endocrinology

Background:

Nuclear receptors are crucial ligand-activated transcription factors regulating diverse physiological processes.
They are key targets for drug development across various disorders.
Traditional ligands (agonists/antagonists) modulate receptor activity broadly.

Purpose of the Study:

To review the development of selective nuclear receptor modulators.
To explore the distinct pharmacology of these selective modulators.

Main Methods:

Review of scientific literature on nuclear receptors and selective modulators.
Analysis of ligand-receptor interactions and their functional outcomes.

Main Results:

Selective modulators exhibit tissue- and gene-specific agonist/antagonist functions.
These ligands offer a distinct pharmacological profile compared to traditional modulators.

Conclusions:

Selective nuclear receptor modulators represent a sophisticated class of therapeutic agents.
Their development and understanding are critical for targeted drug discovery.