Related Experiment Video
Updated: Jun 27, 2026
09:53
Real-time In Vitro Monitoring of Odorant Receptor Activation by an Odorant in the Vapor Phase
Published on: April 23, 2019
High-potency olfactory receptor agonists discovered by virtual high-throughput screening: molecular probes for
Nicolas Triballeau1, Eric Van Name, Guillaume Laslier
1Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques, CNRS UMR-8601, Université Paris Descartes, 45 rue des Saints Pères, 75270 Paris Cedex 06, France.
Neuron
|December 17, 2008
Summary
Researchers discovered new potent odorant molecules using computational screening to target olfactory receptors. These findings enhance our understanding of smell and could lead to new ways to detect environmental signals like bacteria.
Area of Science:
- Olfactory receptor research
- Computational chemistry
- Biochemistry
Background:
- Vertebrate olfactory systems detect diverse chemicals via ligand-receptor interactions.
- Olfactory G protein-coupled receptors (GPCRs) are crucial for odorant recognition.
- Amino acid receptors represent a key class of olfactory GPCRs.
Purpose of the Study:
- To identify novel high-affinity agonists for an amino acid-recognizing olfactory GPCR.
- To explore the molecular basis of ligand binding through computational modeling.
- To validate the in vivo olfactory activity of identified compounds.
Main Methods:
- Virtual screening of chemical libraries to predict ligand-receptor interactions.
- Functional assays to test the potency of candidate agonists.
- Molecular modeling to visualize ligand-receptor binding interfaces.
Main Results:
- Several novel agonists were identified with potencies exceeding natural ligands.
- Computational models revealed conserved binding interactions across divergent receptors.
- Top compounds demonstrated significant in vivo odorant activity, including a natural product.
Conclusions:
- Virtual screening is effective for discovering potent olfactory receptor agonists.
- Identified compounds offer insights into conserved ligand-binding mechanisms.
- The approach can be applied to discover bioactive molecules for chemosensory research.
Related Concept Videos
01:03Olfactory Receptors: Location and Structure
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...
01:25Olfaction
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...
The olfactory receptors are embedded in the cilia of the...
01:20Physiology of Smell and Olfactory Pathway
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...
The olfactory...
01:15G Protein-coupled Receptors
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.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
01:25Drug-Receptor Interaction: Agonist
Agonists are drugs that interact with specific receptors in the body to produce a biological response. When an agonist binds to a receptor, it activates or enhances the receptor's function, leading to physiological effects. The interaction between agonist drugs and receptors is crucial for their therapeutic action in various medical treatments.
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.
01:26Drug Discovery: Overview
Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...