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Related Concept Videos

Mechanically-gated Ion Channels01:12

Mechanically-gated Ion Channels

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...
Mechanically-gated Ion Channels01:12

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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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Related Experiment Video

Updated: May 26, 2026

Measurement of Vibration Detection Threshold and Tactile Spatial Acuity in Human Subjects
07:32

Measurement of Vibration Detection Threshold and Tactile Spatial Acuity in Human Subjects

Published on: September 1, 2016

Yoda molecules agonize PIEZO2.

Tharaka D Wijerathne1, Aneesh Chandrasekharan1, Aashish Bhatt2

  • 1Department of Biomedical Sciences, Western University of Health Sciences, Pomona, CA, USA.

Biorxiv : the Preprint Server for Biology
|May 25, 2026
PubMed
Summary
This summary is machine-generated.

Yoda molecules activate PIEZO1 and PIEZO2 mechanosensitive channels. This study reveals Yoda1

Keywords:
PIEZO1PIEZO2Yoda1Yoda2mechanotransduction

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Area of Science:

  • Biophysics
  • Molecular Biology
  • Cell Physiology

Background:

  • PIEZO proteins (PIEZO1 and PIEZO2) are crucial mechanosensitive ion channels.
  • Yoda molecules (Yoda1, Yoda2) are known activators of PIEZO1, but their precise interaction mechanism with PIEZO2 is unclear.

Purpose of the Study:

  • To elucidate the molecular mechanism of Yoda molecule activation on PIEZO1 and PIEZO2.
  • To investigate the selective activation of PIEZO channels by Yoda molecules.

Main Methods:

  • Electrophysiology
  • Calcium imaging
  • Site-directed mutagenesis
  • Molecular dynamics simulations

Main Results:

  • Yoda1 enhances PIEZO2 open probability and stretch sensitivity comparably to PIEZO1, but with reduced calcium influx.
  • Yoda1 and Yoda2 modulate PIEZO2 inactivation kinetics, with Yoda2 exhibiting higher potency due to specific interactions within the binding site.
  • A molecular basis for Yoda2's enhanced potency was identified through interactions between its benzoic acid group and a conserved arginine residue.

Conclusions:

  • Yoda molecules exhibit differential effects on PIEZO1 and PIEZO2, impacting their function and inactivation.
  • The findings necessitate a reevaluation of previous studies utilizing Yoda molecules to understand PIEZO channel-mediated biological processes.
  • This research provides critical insights into the structure-activity relationship of Yoda molecules and PIEZO channel modulation.