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Related Concept Videos

Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

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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.
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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
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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...
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Effect of Hepatic Disease on Pharmacokinetics: Drug Dosing and Hepatic Blood Flow01:26

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Chronic liver disease significantly impacts drug metabolism due to alterations in hepatic blood flow and enzyme accessibility. This disruption affects the body's pharmacokinetics—the movement and processing of drugs within the system. Key enzymes crucial for metabolizing medications become less accessible, changing how drugs are processed and utilized. Furthermore, liver disease influences the synthesis of plasma proteins, such as albumin and globulins, which play critical roles in drug...
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Liver Regeneration01:24

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The liver is an important organ in vertebrates that plays an essential role in metabolism. It is also responsible for storing and redistributing nutrients such as carbohydrates, fats, and vitamins in the body. Additionally, the liver releases bile salts which are critical for digesting food and eliminating toxic metabolites from the body.
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Updated: Apr 7, 2026

Inducing and Characterizing Vesicular Steatosis in Differentiated HepaRG Cells
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Nuclear Receptor-Targeted Therapy for Metabolic Dysfunction-Associated Steatotic Liver Disease.

Yachao Zhou1, Zhaojian Liu2, Donghai Cui2

  • 1Department of Medical Genetics and Molecular Biochemistry, Lewis Katz School of Medicine, Temple University, Philadelphia, PA 19140, USA.

International Journal of Drug Discovery and Pharmacology
|April 6, 2026
PubMed
Summary
This summary is machine-generated.

Metabolic dysfunction-associated steatotic liver disease (MASLD) affects over 25% of the population. Nuclear receptors (NRs) are key targets for new MASLD and MASH treatments, with several drugs in development.

Keywords:
farnesoid X receptor (FXR)metabolic dysfunction-associated steatotic liver disease (MASLD)nuclear receptor targeted therapynuclear receptors (NRs)peroxisome proliferator-activated receptors (PPARs)thyroid hormone receptor-β (THR-β)

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Area of Science:

  • Hepatology
  • Endocrinology
  • Molecular Biology

Background:

  • Metabolic dysfunction-associated steatotic liver disease (MASLD) is a global health issue affecting over 25% of the population.
  • Metabolic dysfunction-associated steatohepatitis (MASH), an advanced form of MASLD, involves liver inflammation, injury, and fibrosis.
  • Current MASLD and MASH treatments are limited due to complex, not fully understood pathophysiological mechanisms.

Purpose of the Study:

  • To review recent advancements in understanding nuclear receptor (NR) mechanisms in MASLD pathogenesis.
  • To discuss the progress of NR-targeted therapies for MASLD and MASH.
  • To highlight the therapeutic potential of targeting thyroid hormone receptor-β (THR-β), peroxisome proliferator-activated receptors (PPARs), and farnesoid X receptor (FXR).

Main Methods:

  • Literature review of recent research on nuclear receptors and MASLD.
  • Analysis of the role of specific NRs (THR-β, PPARs, FXR) in liver disease.
  • Summary of current and emerging NR-targeted therapeutic strategies.

Main Results:

  • Nuclear receptors significantly regulate lipid metabolism, glucose homeostasis, inflammation, and fibrosis, all critical to MASLD progression.
  • Several NR-targeted drugs, including THR-β agonist resmetirom and dual PPAR-α/γ agonist saroglitazar, have been approved.
  • Numerous NR-targeted therapies are currently undergoing clinical trials for MASLD and MASH.

Conclusions:

  • Nuclear receptors represent promising therapeutic targets for MASLD and MASH.
  • Targeting specific NRs like THR-β, PPARs, and FXR offers potential for effective treatment strategies.
  • Continued research into NR mechanisms and targeted therapies is crucial for combating the growing burden of MASLD and MASH.