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Related Concept Videos

Drugs for Treatment of Crohn's Disease in IBD Using Glucocorticoids01:21

Drugs for Treatment of Crohn's Disease in IBD Using Glucocorticoids

Glucocorticoids, a class of anti-inflammatory drugs, are pivotal in treating moderate to severe Crohn's disease by inducing remission. They exhibit their anti-inflammatory action by inhibiting the production of inflammatory cytokines such as tumor necrosis factor (TNF)-α, interleukin (IL)-1, and chemokines like IL-8. In addition, they reduce the expression of inflammatory cell adhesion molecules and inhibit gene transcription of nitric oxide synthase, phospholipase A2, cyclooxygenase-2 (COX-2),...
Antiasthma Drugs: Inhaled Corticosteroids and Glucocorticoids01:25

Antiasthma Drugs: Inhaled Corticosteroids and Glucocorticoids

Inhaled corticosteroids (ICS) are anti-inflammatory drugs used primarily in treating persistent asthma and providing long-term maintenance. They target the bronchial mucosa, the lining of the airways, to control inflammation, a critical factor in asthma progression and exacerbation.
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Glucagon-like Receptor Agonists01:24

Glucagon-like Receptor Agonists

Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by the...
Dose-Response Relationship: Selectivity and Specificity01:25

Dose-Response Relationship: Selectivity and Specificity

Drugs exert their therapeutic effects by interacting with receptors, enzymes, or ion channels that are present throughout the human body. The strength and duration of the interaction between a drug and its target receptor are characterized by the selectivity and specificity of the drug. Selectivity refers to a drug's strong preference for its intended target over other targets. For instance, isoprenaline, a non-selective β-adrenergic agonist, interacts with both β1- and β2-adrenergic receptors...
Antiasthma Drugs: Leukotriene Modifiers01:19

Antiasthma Drugs: Leukotriene Modifiers

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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:

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Updated: Jun 15, 2026

Biochemical Reconstitution of Steroid Receptor&#x2022;Hsp90 Protein Complexes and Reactivation of Ligand Binding
11:07

Biochemical Reconstitution of Steroid Receptor•Hsp90 Protein Complexes and Reactivation of Ligand Binding

Published on: September 21, 2011

Selective Glucocorticoid Receptor modulators.

Karolien De Bosscher1

  • 1Department of Physiology, Ghent University, Belgium. Karolien.DeBosscher@ugent.be <Karolien.DeBosscher@ugent.be>

The Journal of Steroid Biochemistry and Molecular Biology
|March 9, 2010
PubMed
Summary
This summary is machine-generated.

The Glucocorticoid Receptor (NR3C1) has multiple functions, complicating the development of anti-inflammatory drugs. New research focuses on selective modulators for safer, targeted therapies.

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A Chemical Screening Procedure for Glucocorticoid Signaling with a Zebrafish Larva Luciferase Reporter System
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Biochemical Reconstitution of Steroid Receptor&#x2022;Hsp90 Protein Complexes and Reactivation of Ligand Binding
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A Chemical Screening Procedure for Glucocorticoid Signaling with a Zebrafish Larva Luciferase Reporter System
13:22

A Chemical Screening Procedure for Glucocorticoid Signaling with a Zebrafish Larva Luciferase Reporter System

Published on: September 10, 2013

Area of Science:

  • Pharmacology
  • Molecular Biology
  • Immunology

Background:

  • The Glucocorticoid Receptor (NR3C1) exhibits dual actions, mediating anti-inflammatory effects and causing adverse outcomes.
  • Its diverse functionalities are influenced by tissue type, ligand, receptor variants, cofactors, and gene promoters.
  • Developing selective ligands targeting specific gene expression programs remains a significant challenge.

Purpose of the Study:

  • To review recent advances in understanding the multifaceted nature of the Glucocorticoid Receptor (NR3C1).
  • To highlight the development of novel selective Glucocorticoid Receptor modulators (SGRMs).
  • To discuss the application of SGRMs in anti-inflammatory strategies.

Main Methods:

  • Literature review of recent studies on Glucocorticoid Receptor (NR3C1) function and modulation.
  • Analysis of emerging data on selective Glucocorticoid Receptor modulators (SGRMs).
  • Focus on research related to anti-inflammatory applications.

Main Results:

  • Characterization of Glucocorticoid Receptor (NR3C1) complexity beyond its dual nature.
  • Identification of factors influencing Glucocorticoid Receptor (NR3C1) functionality.
  • Progress in designing selective ligands for targeted therapeutic effects.

Conclusions:

  • Fundamental research is crucial for designing effective and safe Glucocorticoid Receptor (NR3C1) modulators.
  • Selective Glucocorticoid Receptor modulators (SGRMs) show promise for targeted anti-inflammatory therapies.
  • Further development of SGRMs is needed to translate research into clinical applications.