Nuclear Receptor Interaction

Nuclear receptor interaction is the binding and functional communication between nuclear receptors, their ligands, DNA response elements, and regulatory proteins that control gene expression. In many cases, a small molecule binds the receptor’s ligand-binding domain, changing its shape and influencing recruitment of coactivators or corepressors; the receptor complex can then bind specific DNA sequences and alter transcription. These interactions help regulate development, metabolism, reproduction, and immune responses in biology. Studying them clarifies hormone signaling and supports research into receptor-targeted drugs for conditions such as cancer, metabolic disease, and inflammation, while also helping evaluate endocrine-disrupting chemicals.

Nuclear Receptor Interaction - Related Videos

Research

JoVE Journal - Biology

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

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Cited by 6 •

2013

Ketoconazole binds to and antagonizes Pregnane X Receptor (PXR) activation. Yeast high throughput screens of PXR mutants define a unique region for ketoconazole binding. This yeast-based genetic method discovers novel nuclear receptor interactions with ligands that associate with surface binding sites.

Education

JoVE Core - Pharmacology
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Transducer Mechanism: Nuclear Receptors

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2023

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:

Drug-Receptor Interactions

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2025

Drug-receptor interaction describes the binding of receptors by drugs, but not all drug-receptor interactions result in activation and tissue response. For instance, the binding of agonists activates the receptor to generate a cellular reaction, while antagonists bind to receptors without causing their activation. Several parameters, such as the drug's affinity for its receptor and its efficacy, which is its ability to activate the receptor, determine the drug's effect on the tissue.

A Protein Preparation Method for the High-throughput Identification of Proteins Interacting with a Nuclear Cofactor Using LC-MS/MS Analysis

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Cited by 1 •

2017

We have established a method for the purification of coregulatory interaction proteins using the LC-MS/MS system.

Biomembrane Force Probe to Quantitate Receptor-Ligand Interactions

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2025

In this video, biomembrane force probes (BFPs) are used to measure the forces between receptors and ligands. This technique can detect interactions by monitoring the pressure needed to break the bonds between the pMHC conjugated on the probe beads and the TCRs on the target cells.

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