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Related Concept Videos

Non-gated Ion Channels01:24

Non-gated Ion Channels

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Ion channels are specialized proteins on the plasma membrane that allow charged ions to pass down their electrochemical gradient. Their main function is to maintain the membrane potential which is critical for cell viability. These channels are either gated or non-gated and can transport more than a thousand ions within milliseconds for the cellular event to occur.
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Mechanically-gated ion channels are proteins found in eukaryotic and prokaryotic cell membranes that open in response to mechanical stress. Tension, compression, swelling, and shear stress can alter the conformation of the protein, opening a transmembrane channel that allows the passage of ions for signal transmission. In eukaryotes, mechanically-gated channels are distributed in several regions like the neurons, lungs, skin, bladder, and heart, where they play critical roles in numerous...
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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.
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G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
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GPCRs are primarily responsible for our sense of smell, taste, and vision.  The binding of a sensory stimulus activates GPCR to stimulate effector proteins, many of which are ion channels in the sensory organs. GPCRs modulate the opening and closing of the target ion channels either directly by binding them, or by releasing second messengers that activate these channels. As ions move across the membrane, the membrane potential is altered, which induces an appropriate response.
Sensory...
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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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Epithelial P2X purinergic receptor channel expression and function.

A L Taylor1, L M Schwiebert, J J Smith

  • 1Department of Cell Biology, Gregory Fleming James Cystic Fibrosis Research Center, University of Alabama-Birmingham, Birmingham, Alabama 35294, USA.

The Journal of Clinical Investigation
|October 8, 1999
PubMed
Summary
This summary is machine-generated.

P2X purinergic receptors (P2XRs) are present in epithelial cells and activate chloride transport. This suggests P2XRs could be a therapeutic target for cystic fibrosis (CF) by modulating extracellular nucleotide signaling.

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Area of Science:

  • Epithelial physiology
  • Purinergic signaling
  • Ion channel function

Background:

  • P2X purinergic receptors (P2XRs) are ATP-gated ion channels.
  • P2XRs mediate calcium influx, influencing cellular processes.
  • Epithelial ion transport is crucial for various physiological functions.

Purpose of the Study:

  • To investigate the expression and function of P2XRs in epithelial tissues.
  • To determine if P2XRs transduce extracellular ATP signals to stimulate chloride transport.
  • To explore P2XRs as potential therapeutic targets for cystic fibrosis (CF).

Main Methods:

  • Electrophysiological recordings of epithelial cells.
  • Messenger RNA (mRNA) analysis to detect P2XR expression.
  • Utilizing P2X-selective agonists to study receptor activation.

Main Results:

  • Multiple P2XRs are broadly expressed in human and mouse pulmonary epithelia and other epithelial cells.
  • P2XRs are active on both apical and basolateral epithelial surfaces.
  • P2X agonists stimulate chloride transport in both CF and non-CF nasal mucosa.

Conclusions:

  • Epithelial cells express functional P2XRs on both apical and basolateral membranes.
  • P2XRs are involved in transducing extracellular ATP signals to regulate chloride transport.
  • Targeting P2XRs offers a potential novel therapeutic strategy for cystic fibrosis (CF).