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Related Concept Videos

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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Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

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G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical,...
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Types of Receptors: Internal Receptors01:07

Types of Receptors: Internal Receptors

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Many cellular signals are hydrophilic and cannot pass through the plasma membrane. However, small or hydrophobic signaling molecules can cross the hydrophobic core of the plasma membrane and bind intracellular receptors that reside within the cell cytoplasm or nucleus. Many mammalian steroid hormones and nitric oxide (NO) gas use this cell signaling mechanism.
Similar to membrane-bound receptors, the binding of a ligand to the intracellular receptor of causes a conformational change in the...
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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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G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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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...
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Internal Receptors01:31

Internal Receptors

70.3K
Many cellular signals are hydrophilic and therefore cannot pass through the plasma membrane. However, small or hydrophobic signaling molecules can cross the hydrophobic core of the plasma membrane and bind to internal, or intracellular, receptors that reside within the cell. Many mammalian steroid hormones use this mechanism of cell signaling, as does nitric oxide (NO) gas.
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Related Experiment Video

Updated: Jul 25, 2025

Biochemical Reconstitution of Steroid Receptor•Hsp90 Protein Complexes and Reactivation of Ligand Binding
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The Biologist's Guide to the Glucocorticoid Receptor's Structure.

Nick Deploey1,2,3, Laura Van Moortel1,2,3, Inez Rogatsky4,5

  • 1VIB Center for Medical Biotechnology, VIB, 9052 Ghent, Belgium.

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|June 28, 2023
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Glucocorticoid receptor alpha (GRα) is key for halting inflammation and killing cancer cells. Understanding its structure and mechanisms is vital to overcome side effects and resistance in clinical applications.

Keywords:
DNA-binding domainN-terminal domainglucocorticoid receptorglucocorticoidsligand-binding domainnuclear receptorstructure

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A Chemical Screening Procedure for Glucocorticoid Signaling with a Zebrafish Larva Luciferase Reporter System
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Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells
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Biochemical Reconstitution of Steroid Receptor•Hsp90 Protein Complexes and Reactivation of Ligand Binding
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Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells
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Area of Science:

  • Molecular Biology
  • Cell Biology
  • Biochemistry

Background:

  • The glucocorticoid receptor alpha (GRα) is a nuclear receptor superfamily member.
  • GR mediates the effects of glucocorticoids (GCs), widely used clinically for anti-inflammatory and anti-cancer effects.
  • Therapeutic limitations of GCs include side effects and resistance, necessitating a deeper understanding of GR action.

Purpose of the Study:

  • To review the various domains and mechanisms of action of GR.
  • To provide a structural perspective on GR function in different biological pathways.
  • To highlight how structural insights can close knowledge gaps in GR function.

Main Methods:

  • Literature review focusing on structural biology.
  • Analysis of published data on GR structure, conformation, and stoichiometry.
  • Synthesis of information on GR-controlled biological pathways.

Main Results:

  • Increasing understanding of GR structure, conformation, and stoichiometry.
  • Identification of key GR domains and their roles in mediating GC responses.
  • Elucidation of context-specific GR action mechanisms.

Conclusions:

  • Structural insights are crucial for understanding GR function.
  • Resolving GR's context-specific mechanisms is essential for improving GC therapy.
  • Further structural studies will aid in overcoming GC resistance and side effects.