Related Experiment Video

Updated: Nov 25, 2025

High-resolution Respirometry to Measure Mitochondrial Function of Intact Beta Cells in the Presence of Natural Compounds
12:32

High-resolution Respirometry to Measure Mitochondrial Function of Intact Beta Cells in the Presence of Natural Compounds

Published on: January 23, 2018

12.6K

Targeting Orphan Nuclear Receptors NR4As for Energy Homeostasis and Diabetes

Chenyang Zhang1,2,3,4, Bin Zhang1,2,3,4, Xuelian Zhang1,2,3,4

  • 1Beijing Key Laboratory of Innovative Drug Discovery of Traditional Chinese Medicine (Natural Medicine) and Translational Medicine, Institute of Medicinal Plant Development, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing, China.

Frontiers in Pharmacology
|December 17, 2020
PubMed

Insights

Nuclear receptor subfamily 4, group A (NR4As) are crucial for energy balance and diabetes regulation. Understanding NR4As offers new therapeutic targets for obesity and metabolic syndrome.

Area of Science:

  • Endocrinology
  • Metabolic Research
  • Molecular Biology

Background:

  • Orphan nuclear receptors, particularly NR4As, influence key metabolic processes like cell proliferation and energy homeostasis.
  • Obesity is a major driver of metabolic diseases, including diabetes, yet its precise mechanisms remain incompletely understood.
  • NR4As are implicated in regulating energy balance and are potential drug targets for metabolic syndrome.

Purpose of the Study:

  • To review the structure, regulation, and critical roles of NR4As in energy homeostasis and diabetes.
  • To explore small molecules that can modulate NR4A activity.
  • To provide a foundation for developing NR4A-targeted therapies for obesity and related metabolic disorders.

Main Methods:

  • Literature review of studies on NR4A structure, regulation, and function.
  • Analysis of research linking NR4A dysregulation to metabolic diseases.
  • Examination of small molecules affecting NR4A activity.

Main Results:

  • NR4As play significant roles in regulating carbohydrate and lipid metabolism.
  • Altered NR4A levels are associated with chronic inflammation, tumorigenesis, diabetes complications, and cardiovascular diseases.
  • Existing research highlights NR4As' potential in managing metabolic health.

Conclusions:

  • NR4As are vital regulators of energy homeostasis and are implicated in diabetes pathogenesis.
  • Targeting NR4As presents a promising strategy for treating obesity and associated metabolic diseases.
  • Further research into NR4A modulators could lead to novel therapeutic interventions.
Keywords:
NR4Asdiabetesenergy homeostasismetabolismorphan nuclear receptors

More Related Videos

Live Images of GLUT4 Protein Trafficking in Mouse Primary Hypothalamic Neurons Using Deconvolution Microscopy08:47

Live Images of GLUT4 Protein Trafficking in Mouse Primary Hypothalamic Neurons Using Deconvolution Microscopy

Published on: December 7, 2017

10.0K
Mechanism of Regulation of Adipocyte Numbers in Adult Organisms Through Differentiation and Apoptosis Homeostasis08:34

Mechanism of Regulation of Adipocyte Numbers in Adult Organisms Through Differentiation and Apoptosis Homeostasis

Published on: June 3, 2016

15.5K

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:
2.1K
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
3.5K
Insulin: The Receptor and Signaling Pathways01:28

Insulin: The Receptor and Signaling Pathways

Insulin action is mediated through a receptor tyrosine kinase, akin to the IGF-1 receptor. The number of receptors per cell varies significantly, from 40 on erythrocytes to 300,000 on adipocytes and hepatocytes. The insulin receptor consists of linked α/β subunit dimers, forming a heterotetramer glycoprotein with two extracellular α subunits and two β subunits spanning the membrane. The α subunits inhibit the inherent tyrosine kinase activity of the β subunits, but...
2.1K
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...
10.6K
Spare Receptors01:30

Spare Receptors

Some receptors remain unoccupied even when an agonist produces a maximal response. Such empty ones are called spare receptors. In presence of spare receptors the maximum effect of an agonist drug is achieved with fewer than 100% of the receptors being occupied. To determine the presence of spare receptors, scientists often compare the concentration of the drug needed to produce 50% of the maximum effect (EC50) with the concentration of the drug needed to occupy 50% of the receptors (Kd). If the...
4.3K
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
15.3K