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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:
Transducer Mechanism: Enzyme-Linked Receptors01:27

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Adrenergic Receptors: β Subtype01:26

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Adrenergic Receptors (Adrenoceptors): Classification01:27

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Receptor Autoradiography Protocol for the Localized Visualization of Angiotensin II Receptors
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Nuclear membrane receptors for ET-1 in cardiovascular function.

Ghassan Bkaily1, Levon Avedanian, Johny Al-Khoury

  • 1Dept. of Anatomy and Cell Biology, Faculty of Medicine, Université de Sherbrooke, 3001- 12 Ave. North, Sherbrooke, Quebec, Canada J1H 5N4. ghassan.bkaily@usherbrooke.ca

American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
|November 19, 2010
PubMed
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Endothelin receptors (ET(A) and ET(B)) are found on both cell and nuclear membranes in cardiovascular cells. Nuclear ET-1 receptors may be crucial for ET-1

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Area of Science:

  • Cardiovascular Biology
  • Cellular Signaling
  • Molecular Pharmacology

Background:

  • Endothelin receptors (ET(A) and ET(B)) are known to regulate cardiovascular functions.
  • Recent research indicates G protein-coupled receptors (GPCRs) and ion transporters are functional at nuclear membranes.
  • The presence and role of ET receptors at nuclear membranes remain largely unexplored.

Purpose of the Study:

  • To investigate the presence and function of ET(A) and ET(B) receptors at both plasma and nuclear membranes in cardiovascular cells.
  • To determine the role of these receptors in mediating calcium (Ca2+) and reactive oxygen species (ROS) signaling.
  • To explore the potential of nuclear ET-1 receptors as therapeutic targets.

Main Methods:

  • Immunohistochemistry and Western blotting to detect ET(A) and ET(B) receptor localization in various cardiovascular cell types.
  • Measurement of intracellular calcium ([Ca](c) and [Ca](n)) and ROS levels using fluorescent indicators.
  • Stimulation with endothelin-1 (ET-1) to assess receptor-mediated signaling pathways.

Main Results:

  • ET(A) and ET(B) receptors are present at both plasma and nuclear membranes in human cardiac, vascular smooth muscle, and endothelial cells.
  • ET-1 stimulation increases cytosolic and nuclear calcium and ROS levels, with cell-type specific variations.
  • Extracellular ET-1 effects on nuclear calcium depend on receptor type and cell type, while cytosolic ET-1 effects on nuclear calcium are cell-type independent.

Conclusions:

  • Nuclear membrane ET-1 receptors play a significant role in overall ET-1 action.
  • The localization and signaling of ET receptors at the nuclear membrane offer novel insights into cardiovascular regulation.
  • Nuclear ET-1 receptors represent a potential new target for therapeutic interventions.