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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:
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase01:11

Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase

Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...
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...
Drug Toxicity: Dose-Dependent Reactions01:24

Drug Toxicity: Dose-Dependent Reactions

Drug toxicities can be stratified into pharmacological, pathological, or genotoxic based on their mechanisms. The incidence and severity of these toxicities generally increase with the drug's concentration in the body and exposure time.Pharmacological toxicity is evident when the therapeutic effects of drugs overshoot into adverse reactions in a predictable, dose-dependent manner. Central nervous system (CNS) depression from barbiturates is a classic example, with effects escalating from...
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...
Mutagenicity and Carcinogenicity01:25

Mutagenicity and Carcinogenicity

Mutagenicity and carcinogenicity refer to the ability of drugs to cause genetic defects and induce cancer, respectively. The International Agency for Research on Cancer (IARC) classifies agents into four groups based on their carcinogenic potential. Group 1 agents are known human carcinogens; group 2A agents are probably carcinogenic to humans; group 3 agents lack data to support their role in carcinogenesis; and group 4 includes agents for which data support that they are not likely to be...

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Related Experiment Video

Updated: Jul 14, 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

Genomic profiling in nuclear receptor-mediated toxicity.

Courtney G Woods1, John P Vanden Heuvel, Ivan Rusyn

  • 1Department of Environmental Sciences and Engineering, University of North Carolina, Chapel Hill, North Carolina 27599-7431, USA.

Toxicologic Pathology
|June 15, 2007
PubMed
Summary

Genomics is crucial for understanding nuclear receptors (NRs) and their role in drug development and toxicity. This approach helps identify drug targets and biomarkers for chemical toxicants affecting physiological responses.

Related Experiment Videos

Last Updated: Jul 14, 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

Area of Science:

  • Pharmacology and Toxicology
  • Genomics
  • Molecular Biology

Background:

  • Nuclear receptors (NRs) regulate numerous physiological processes, making them key targets for drug development.
  • NR ligands, including pharmaceuticals and environmental chemicals, can elicit adverse health effects.
  • Understanding NR-mediated toxicity is complex due to overlapping biological pathways.

Purpose of the Study:

  • To review the application of genomics in studying nuclear receptors.
  • To highlight the role of genomics in drug discovery, toxicity assessment, and understanding NR mechanisms.
  • To focus on specific nuclear receptors: PPAR, CAR, PXR, RXR, LXR, FXR, and AHR.

Main Methods:

  • Gene expression profiling using microarrays and other genomic technologies.
  • Simultaneous analysis of thousands of genes to discern toxicological mechanisms.
  • Global approaches to comprehensively probe complex NR-regulated networks.

Main Results:

  • Genomics provides sensitive tools for identifying mechanisms of therapeutic and environmental chemical toxicity.
  • Genomic profiling is essential for identifying drug targets and biomarkers of exposure and toxicity.
  • Genomics facilitates understanding of both NR-dependent and NR-independent events.

Conclusions:

  • Genomics is indispensable for advancing drug discovery, design, optimization, and risk assessment of NR-activating toxicants.
  • Future research and development in nuclear receptor pharmacology will heavily rely on genomic profiling.
  • This review emphasizes the pivotal role of genomics in unraveling NR functions and impacts.