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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:
Drug Discovery: Overview01:26

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
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...
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...
Drug-Receptor Bonds01:25

Drug-Receptor Bonds

Drug-receptor bonds are formed through various chemical forces when drugs interact with target cells. Covalent bonds, strong and irreversible, are exemplified by DNA-alkylating anticancer agents that inhibit cell division. However, such irreversible drug binding lacks selectivity and can modify the DNA of the surrounding healthy cells. Covalent binding often contributes to tissue toxicity, as seen with chloroform and paracetamol metabolites binding to the liver, causing hepatotoxicity.
In...
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: Jul 3, 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

Nuclear receptor drug discovery.

Taosheng Chen1

  • 1Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105, USA. taosheng.chen@stjude.org

Current Opinion in Chemical Biology
|July 30, 2008
PubMed
Summary
This summary is machine-generated.

Nuclear receptors (NRs) are key drug targets. Selective NR modulators offer improved therapeutic strategies by distinctively altering NR function, aiming for enhanced efficacy and reduced side effects.

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Last Updated: Jul 3, 2026

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

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06:26

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery

Published on: May 16, 2021

Area of Science:

  • Molecular biology
  • Pharmacology
  • Genetics

Background:

  • Nuclear receptors (NRs) are crucial ligand-activated transcription factors regulating gene expression.
  • The 48 human NR genes represent significant targets for therapeutic drug development.
  • Selective NR modulators are transforming drug discovery by enabling functional modulation distinct from cognate ligands.

Purpose of the Study:

  • To review current strategies in NR drug development.
  • To focus on modulators targeting the glucocorticoid receptor (GR), androgen receptor (AR), and pregnane X receptor (PXR).
  • To highlight advancements in improving NR drug function and tissue selectivity.

Main Methods:

  • Review of scientific literature on NR modulators.
  • Analysis of drug discovery strategies for NRs.
  • Focus on specific NR targets: GR, AR, and PXR.

Main Results:

  • Selective NR modulators offer a paradigm shift from mimicking natural ligands to precise functional modulation.
  • Current research prioritizes enhancing drug candidate efficacy and tissue selectivity.
  • Development aims to minimize undesirable side effects associated with NR modulation.

Conclusions:

  • Selective NR modulation represents a key advancement in drug discovery.
  • Targeting GR, AR, and PXR with selective modulators holds therapeutic promise.
  • Continued focus on selectivity is essential for effective and safe NR-based therapies.