Related Experiment Video

Updated: Apr 1, 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

13.2K

Biology of PXR: role in drug-hormone interactions

Jing Wang1, Shu Dai1, Yan Guo2

  • 1Beijing Key Laboratory of Gene Resource and Molecular Development and College of Life Sciences, Beijing Normal University, Beijing 100875, P.R. China.

EXCLI Journal
|September 30, 2015
PubMed

Insights

The Pregnane X receptor (PXR) regulates drug metabolism and can disrupt hormone balance. Understanding PXR

Area of Science:

  • Endocrinology
  • Pharmacology
  • Toxicology

Background:

  • Hormonal homeostasis is critical for physiological and pathological processes.
  • Xenobiotics, like drugs, can disrupt hormone balance by inducing drug-metabolizing enzymes (DMEs) and transporters.
  • The Pregnane X receptor (PXR, NR1I2) is a key regulator of xenobiotic metabolism and drug-drug interactions.

Purpose of the Study:

  • To review recent advances in understanding PXR's role in hormone homeostasis.
  • To explore PXR's function in regulating glucocorticoid, mineralocorticoid, androgen, and estrogen levels.
  • To highlight the implications of PXR-mediated drug-hormone interactions.

Main Methods:

  • Literature review of recent scientific publications.
  • Analysis of PXR's transcriptional regulation of DMEs and transporters.
  • Examination of PXR's role in endocrine disruption.

Main Results:

  • PXR plays a significant role in drug metabolism and drug-drug interactions.
  • Emerging evidence shows PXR mediates endocrine-disrupting functions.
  • PXR influences the homeostasis of key steroid hormones.

Conclusions:

  • PXR significantly impacts hormonal homeostasis, affecting glucocorticoid, mineralocorticoid, androgen, and estrogen levels.
  • PXR's role in endocrine disruption has implications for drug safety assessment.
  • Understanding PXR-mediated drug-hormone interactions may aid in managing hormone-dependent diseases.
Keywords:
PXRdrug-hormone interactionshormone homeostasisxenobiotic receptor

More Related Videos

An In Vivo Estrogen Deficiency Mouse Model for Screening Exogenous Estrogen Treatments of Cardiovascular Dysfunction After Menopause06:18

An In Vivo Estrogen Deficiency Mouse Model for Screening Exogenous Estrogen Treatments of Cardiovascular Dysfunction After Menopause

Published on: August 13, 2019

13.0K
In Silico Modeling Method for Computational Aquatic Toxicology of Endocrine Disruptors: A Software-Based Approach Using QSAR Toolbox05:47

In Silico Modeling Method for Computational Aquatic Toxicology of Endocrine Disruptors: A Software-Based Approach Using QSAR Toolbox

Published on: August 28, 2019

14.8K

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:
5.9K
Target Cell Response to Hormones01:22

Target Cell Response to Hormones

Hormones intricately bind to receptors on the surface or within target cells, initiating a cascade of cellular responses.
Notably, the cellular response can be regulated by altering the number of receptors expressed in the cell. For example, prolonged exposure to elevated hormone levels results in a gradual decline or down-regulation in the number of receptors for that specific hormone on the cell surface. Conversely, in response to low hormone levels, cells may use up-regulation, producing an...
6.3K
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....
8.3K
Pharmacogenetics of Drug Metabolism: Overview01:27

Pharmacogenetics of Drug Metabolism: Overview

Genetic polymorphism in drug metabolism is crucial to the inter-individual variability observed in drug responses. Drug metabolism primarily involves the chemical modification of drugs and other xenobiotics to enhance their elimination by increasing their polarity. Two main classes of enzymes mediate this biotransformation process: Phase I enzymes, primarily cytochrome P450s, catalyze oxidation and reduction reactions, while other enzymes, such as esterases, mediate hydrolysis, and Phase II...
117
Pharmacokinetics: Drug–Drug Interactions01:25

Pharmacokinetics: Drug–Drug Interactions

Drug interactions occur when the pharmacological effect of one drug is altered by another substance, either enhancing or diminishing its activity. The drug whose activity is altered is known as the object drug, and the substance causing the alteration is called the agent drug or the precipitant. The net effects of these interactions are mostly undesirable, leading to decreased effectiveness or increased adverse effects. In rare cases, interactions can be beneficial, such as the enhanced...
675
Secondary Messengers in Hormone Action01:26

Secondary Messengers in Hormone Action

Water-soluble hormones cannot cross the plasma membrane, so they rely on protein receptors that span the membrane to trigger intracellular signaling pathways. These pathways then activate second messengers inside the cell, including cAMP or calcium ions.
Many hormones bind to transmembrane G protein-coupled receptors that connect to regulatory G proteins. These G proteins can then activate enzymes such as adenylyl cyclase or phospholipase C. Adenylyl cyclase converts ATP to cAMP, activating...
6.2K