ArticleJournal of the American Chemical Society2015
Conserved Residues Control Activation of Mammalian G Protein-Coupled Odorant Receptors.
Article in Journal of the American Chemical Society, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 papers.
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Who cites it
40 citing papers in PubMed.
- Molecular simulation-based 3D structural construction of olfactory receptor with agonist binding.Journal of computer-aided molecular design · 2025Article
- Decoding the Molecular Mechanisms of Menthol Isomer Perception Based on Computational Simulations.Foods (Basel, Switzerland) · 2025Article
- Chemosensory Receptors in Vertebrates: Structure and Computational Modeling Insights.International journal of molecular sciences · 2025Review
- Article
- Engineered odorant receptors illuminate structural principles of odor discrimination.bioRxiv : the preprint server for biology · 2023Article
- Antagonistic interactions between odorants alter human odor perception.Current biology : CB · 2023Article
- Machine Learning-Based Modeling of Olfactory Receptors in Their Inactive State: Human OR51E2 as a Case Study.Journal of chemical information and modeling · 2023Article
- Modeling the Orthosteric Binding Site of the G Protein-Coupled Odorant Receptor OR5K1.Journal of chemical information and modeling · 2023Article
- Article
- Two odorant receptors regulate 1-octen-3-ol induced oviposition behavior in the oriental fruit fly.Communications biology · 2023Article
- Odor Discrimination by Lipid Membranes.Membranes · 2023Article
- Article
- The Third Extracellular Loop of Mammalian Odorant Receptors Is Involved in Ligand Binding.International journal of molecular sciences · 2022Article
- Interactions among key residues regulate mammalian odorant receptor trafficking.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2022Article
- Selectively Fluorinated Citronellol Analogues Support a Hydrogen Bonding Donor Interaction with the Human OR1A1 Olfactory Receptor.Organic letters · 2022Article
- Large-Scale G Protein-Coupled Olfactory Receptor-Ligand Pairing.ACS central science · 2022Article
- Functional molecular switches of mammalian G protein-coupled bitter-taste receptors.Cellular and molecular life sciences : CMLS · 2021Article
- Machine Learning Assisted Approach for Finding Novel High Activity Agonists of Human Ectopic Olfactory Receptors.International journal of molecular sciences · 2021Article
- Copper-mediated thiol potentiation and mutagenesis-guided modeling suggest a highly conserved copper-binding motif in human OR2M3.Cellular and molecular life sciences : CMLS · 2020Article
- A two-stage computational approach to predict novel ligands for a chemosensory receptor.Current research in structural biology · 2020Article
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Authors and funding
7 authors.
Funding
Abstract
Odorant receptor (OR) genes and proteins represent more than 2% of our genome and 4% of our proteome and constitute the largest subgroup of G protein-coupled receptors (GPCRs). The mechanism underlying OR activation remains poorly understood, as they do not share some of the highly conserved motifs critical for activation of non-olfactory GPCRs. By combining site-directed mutagenesis, heterologous expression, and molecular dynamics simulations that capture the conformational change of constitutively active mutants, we tentatively identified crucial residues for the function of these receptors using the mouse MOR256-3 (Olfr124) as a model. The toggle switch for sensing agonists involves a highly conserved tyrosine residue in helix VI. The ionic lock is located between the "DRY" motif in helix III and a positively charged "R/K" residue in helix VI. This study provides an unprecedented model that captures the main mechanisms of odorant receptor activation.
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