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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:
The Two-State Receptor Model01:29

The Two-State Receptor Model

The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
The binding affinity of a drug determines its interaction with one...
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...
Structure-Activity Relationships and Drug Design01:28

Structure-Activity Relationships and Drug Design

Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...
Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
Drug-Receptor Interactions01:29

Drug-Receptor Interactions

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.

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Related Experiment Video

Updated: Jun 2, 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

Modulation of RXR function through ligand design.

Efrén Pérez1, William Bourguet, Hinrich Gronemeyer

  • 1Departamento de Química Orgánica, Facultade de Química, Universidade de Vigo, Spain.

Biochimica Et Biophysica Acta
|April 26, 2011
PubMed
Summary

Retinoid X receptors (RXRs) are crucial nuclear receptors targeted for drug discovery. While RXR modulators show promise for cancer and metabolic diseases, side effects complicate their development, necessitating selective rexinoids.

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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

Prediction and Validation of Gene Regulatory Elements Activated During Retinoic Acid Induced Embryonic Stem Cell Differentiation
09:07

Prediction and Validation of Gene Regulatory Elements Activated During Retinoic Acid Induced Embryonic Stem Cell Differentiation

Published on: June 21, 2016

Area of Science:

  • Nuclear Receptor Superfamily
  • Endocrinology
  • Molecular Biology

Background:

  • Retinoid X receptors (RXRs) are promiscuous partners in nuclear receptor heterodimers, crucial for transcriptional regulation.
  • Heterodimers can be permissive (activated by rexinoids or partner ligands) or non-permissive (requiring both).
  • RXR modulators are explored for cancer and metabolic diseases, with a rexinoid already in clinical use.

Purpose of the Study:

  • To review the modulation of PPARγ/RXR and LXR/RXR heterodimer activities by rexinoids.
  • To discuss the therapeutic potential and limitations of RXR modulators in metabolic diseases.
  • To highlight the need for selective rexinoids to overcome adverse effects.

Main Methods:

  • Review of genetic and pharmacological data from animal models of metabolic diseases.
  • Analysis of RXR heterodimer function and ligand-receptor interactions.
  • Focus on PPARγ/RXR and LXR/RXR heterodimer modulation by rexinoids.

Main Results:

  • RXR agonists and antagonists show potential as anti-obesity agents.
  • RXR modulation can lead to adverse effects like elevated triglycerides, suppressed thyroid axis, and hepatomegaly.
  • Selective PPARγ/RXR and LXR/RXR rexinoids may offer improved therapeutic profiles.

Conclusions:

  • RXR modulators hold therapeutic promise but face development challenges due to side effects.
  • Development of heterodimer-selective rexinoids is crucial for overcoming limitations.
  • Targeting specific RXR heterodimers could lead to safer and more effective treatments for metabolic diseases.