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Related Concept Videos

Allosteric Regulation01:08

Allosteric Regulation

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Allosteric regulation of enzymes occurs when the binding of an effector molecule to a site that is different from the active site causes a change in the enzymatic activity. This alternate site is called an allosteric site, and an enzyme can contain more than one of these sites. Allosteric regulation can either be positive or negative, resulting in an increase or decrease in enzyme activity. Most enzymes that display allosteric regulation are metabolic enzymes involved in the degradation or...
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Physiology of Smell and Olfactory Pathway01:20

Physiology of Smell and Olfactory Pathway

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Humans detect odors with the help of specialized cells located in the upper part of the nasal cavity, called olfactory receptor neurons (ORNs). ORNs possess hair-like structures called cilia, which are receptive to sensations from the inhaled air. When an odorant molecule binds to a specific receptor on the cell of the cilia, it leads to a series of events that ultimately cause the ORN to send electrical signals to the olfactory bulb in the brain through the olfactory nerves.
The olfactory...
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Olfaction01:25

Olfaction

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The sense of smell is achieved through the activities of the olfactory system. It starts when an airborne odorant enters the nasal cavity and reaches olfactory epithelium (OE). The OE is protected by a thin layer of mucus, which also serves the purpose of dissolving more complex compounds into simpler chemical odorants. The size of the OE and the density of sensory neurons varies among species; in humans, the OE is only about 9-10 cm2.
The olfactory receptors are embedded in the cilia of the...
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G-Protein Gated Ion Channels01:21

G-Protein Gated Ion Channels

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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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Cooperative Allosteric Transitions01:58

Cooperative Allosteric Transitions

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Cooperative allosteric transitions can occur in multimeric proteins, where each subunit of the protein has its own ligand-binding site. When a ligand binds to any of these subunits, it triggers a conformational change that affects the binding sites in the other subunits; this can change the affinity of the other sites for their respective ligands. The ability of the protein to change the shape of its binding site is attributed to the presence of a mix of flexible and stable segments in the...
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Olfactory Receptors: Location and Structure01:03

Olfactory Receptors: Location and Structure

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The process of olfaction, also known as the sense of smell, is a sophisticated chemical response system. The specialized sensory neurons that facilitate this process, known as olfactory receptor neurons, are situated in an upper segment of the nasal cavity, known as the olfactory epithelium. Olfactory sensory neurons are bipolar, with their dendrites extending from the epithelium's apex into the mucus that lines the nasal cavity. Airborne molecules, when inhaled, traverse the olfactory...
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Related Experiment Video

Updated: Aug 5, 2025

Real-time In Vitro Monitoring of Odorant Receptor Activation by an Odorant in the Vapor Phase
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Real-time In Vitro Monitoring of Odorant Receptor Activation by an Odorant in the Vapor Phase

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Allosteric modulation of a human odorant receptor.

Casey Trimmer1, Randy Arroyave1, Christine Vuilleumier2

  • 1Firmenich Inc., 250 Plainsboro Road, Plainsboro, NJ 08536, USA.

Current Biology : CB
|March 28, 2023
PubMed
Summary

Human OR5AN1 detects musks. Specific aldehydes enhance its activity, lowering odor detection thresholds and adding complexity to olfactory coding.

Keywords:
G protein-coupled receptorGPCR pharmacologyallosteric modulationmusk perceptionodor detection thresholdodor mixturesodorant receptorolfactionolfactory enhancementperceptual synergy

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Live-cell Measurement of Odorant Receptor Activation Using a Real-time cAMP Assay
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High-throughput Analysis of Mammalian Olfactory Receptors: Measurement of Receptor Activation via Luciferase Activity
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Related Experiment Videos

Last Updated: Aug 5, 2025

Real-time In Vitro Monitoring of Odorant Receptor Activation by an Odorant in the Vapor Phase
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Real-time In Vitro Monitoring of Odorant Receptor Activation by an Odorant in the Vapor Phase

Published on: April 23, 2019

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Live-cell Measurement of Odorant Receptor Activation Using a Real-time cAMP Assay
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High-throughput Analysis of Mammalian Olfactory Receptors: Measurement of Receptor Activation via Luciferase Activity
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Area of Science:

  • Olfactory neuroscience
  • Chemosensation research

Background:

  • Odor perception relies on detecting environmental volatiles via olfactory receptors.
  • Combinatorial activation of odorant receptors enables discrimination of numerous odorants.
  • Odorant receptors exhibit inhibitory modulation with odorant mixtures, aiding discrimination and code sparsity.

Purpose of the Study:

  • To establish the role of human OR5AN1 in musk detection.
  • To identify odorants that enhance OR5AN1 activity in binary mixtures.
  • To investigate the perceptual relevance of allosteric modulation in olfactory receptors.

Main Methods:

  • Chemical and pharmacological characterization of OR5AN1 activity.
  • Identification of positive allosteric modulators using binary odorant mixtures.
  • Sensory experiments to assess odor detection thresholds in humans.

Main Results:

  • Human OR5AN1 was identified as a key receptor for musk odorants.
  • Specific α-β unsaturated aliphatic aldehydes were found to enhance OR5AN1 activity.
  • Allosteric modulation by these aldehydes led to a decreased odor detection threshold.

Conclusions:

  • Allosteric modulation of olfactory receptors is perceptually relevant.
  • This modulation adds complexity to the peripheral olfactory system's odor encoding.
  • OR5AN1 and its modulators offer insights into the mechanisms of odor discrimination.