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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.
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
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Glucagon-like Receptor Agonists01:24

Glucagon-like Receptor Agonists

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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...
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Insulin: The Receptor and Signaling Pathways01:28

Insulin: The Receptor and Signaling Pathways

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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...
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Intracellular Hormone Receptors01:08

Intracellular Hormone Receptors

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Lipid-soluble hormones diffuse across the plasma and nuclear membrane of target cells to bind to their specific intracellular receptors. These receptors act as transcription factors that regulate gene expression and protein synthesis in the target cell
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GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

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Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
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Hormones Regulating Blood Glucose01:16

Hormones Regulating Blood Glucose

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Insulin is released by beta cells of the pancreas when blood glucose levels are high. It facilitates glucose absorption and utilization in insulin-dependent cells with insulin receptors on their plasma membranes. Insulin promotes glucose uptake by increasing the number of glucose transport proteins in the cell membrane, allowing glucose to enter the cell. As a result, glucose utilization and ATP production are enhanced.
In addition to accelerating glucose uptake and utilization, insulin has...
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Related Experiment Video

Updated: Mar 6, 2026

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

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Glucocorticoid receptors: finding the middle ground.

Sofie J Desmet, Karolien De Bosscher

    The Journal of Clinical Investigation
    |March 21, 2017
    PubMed
    Summary

    Glucocorticoids (GCs) have dual roles in inflammation, acting both to reduce and promote it. Understanding the GC receptor (GR) mechanisms is key to developing safer GC-based therapies for inflammation and cancer.

    Area of Science:

    • Immunology
    • Pharmacology
    • Molecular Biology

    Background:

    • Glucocorticoids (GCs) are crucial steroid hormones with significant anti-inflammatory and immune-modulating effects.
    • GCs can also exhibit pro-inflammatory activities, priming the immune system depending on the context.
    • The GC receptor (GR) is a transcription factor with complex, context-dependent functions.

    Purpose of the Study:

    • To investigate the intricate mechanisms underlying GC receptor (GR) functions.
    • To identify strategies for improving the safety profile of glucocorticoid therapies.
    • To reconcile the paradoxical pro- and anti-inflammatory roles of GR.

    Main Methods:

    • Review of recent studies on GR mechanisms.
    • Analysis of GR's dual role in inflammation.

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    Primary Culture of Rat Adrenocortical Cells and Assays of Steroidogenic Functions
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    A Chemical Screening Procedure for Glucocorticoid Signaling with a Zebrafish Larva Luciferase Reporter System
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  • Exploration of GR as a drug target.

    • Main Results:

    • GR exhibits both pro-inflammatory and anti-inflammatory activities.
    • Understanding these paradoxical roles is crucial for therapeutic development.
    • GR's net effect can shift towards anti-inflammation.

    Conclusions:

    • GR is a vital drug target for treating inflammation and cancer.
    • Future therapies may involve refined GCs or novel nonsteroidal GR-targeting molecules.
    • Further research is needed to fully elucidate GR's complex functions and therapeutic potential.