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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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Transducer Mechanism: G Protein–Coupled Receptors01:30

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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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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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Intracellular Hormone Receptors01:08

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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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Types of Receptors: Internal Receptors01:07

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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.
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Internal Receptors01:31

Internal Receptors

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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 16, 2025

Biochemical Reconstitution of Steroid Receptor•Hsp90 Protein Complexes and Reactivation of Ligand Binding
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The human glucocorticoid receptor.

Nicolas C Nicolaides1, George P Chrousos1

  • 1Division of Endocrinology, Metabolism and Diabetes, First Department of Pediatrics, National and Kapodistrian University of Athens Medical School, 'Aghia Sophia' Children's Hospital, Athens, Greece; Division of Endocrinology and Metabolism, Center of Clinical, Experimental Surgery and Translational Research, Biomedical Research Foundation of the Academy of Athens, Athens, Greece; University Research Institute of Maternal and Child Health and Precision Medicine and UNESCO Chair on Adolescent Health Care, National and Kapodistrian University of Athens Medical School, Athens, Greece.

Vitamins and Hormones
|September 17, 2023
PubMed
Summary
This summary is machine-generated.

Glucocorticoids, regulated by the hypothalamic-pituitary-adrenal (HPA) axis and circadian rhythms, are crucial steroid hormones. This review details the human glucocorticoid receptor (GR), its structure, function, and signaling in health and disease.

Keywords:
Chrousos syndromeGlucocorticoid receptor isoformsGlucocorticoidsHuman glucocorticoid receptorNR3C1 gene mutationsNR3C1 gene polymorphisms

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Area of Science:

  • Endocrinology
  • Molecular Biology
  • Genetics

Background:

  • Glucocorticoids are steroid hormones produced by the adrenal cortex.
  • They are key regulators of physiological functions, controlled by the hypothalamic-pituitary-adrenal (HPA) axis and circadian rhythms.
  • Glucocorticoids exert their effects by binding to the glucocorticoid receptor (GR).

Purpose of the Study:

  • To summarize current knowledge on the human glucocorticoid receptor (GR).
  • To provide insights into GR structure, expression, function, and signaling.
  • To discuss GR's role in both normal physiology and pathological conditions.

Main Methods:

  • Review of current scientific literature.
  • Integration of findings from cellular, molecular, and computational-structural biology.
  • Consideration of epigenetic mechanisms.

Main Results:

  • The glucocorticoid receptor (GR) is a ubiquitous transcription factor influencing up to 20% of the mammalian genome.
  • Understanding of GR's molecular mechanisms has advanced significantly.
  • GR's involvement in various physiological and pathological states is increasingly recognized.

Conclusions:

  • The human glucocorticoid receptor (GR) plays a central role in regulating gene transcription and physiological processes.
  • Advances in biology and epigenetics enhance our comprehension of GR signaling.
  • This knowledge is vital for understanding and managing conditions related to glucocorticoid function.