ArticleBritish journal of pharmacology2019
Structural mechanisms underlying activation of TRPV1 channels by pungent compounds in gingers.
Article in British journal of pharmacology, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 63 citations in OpenAlex.
- Pharmacological evaluation of physcion as a TRPV1 inhibitor with multimodal analgesic efficacy in experimental pain models.Biological research · 2025Article
- Recent Preclinical Evidence on Phytocannabinoids in Neurodegenerative Disorders: A Focus on Parkinson's and Alzheimer's Disease.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Advances in the Study for Modulators of Transient Receptor Potential Vanilloid (TRPV) Channel Family.Current topics in medicinal chemistry · 2025Review
- Modulating TRPV1 and TRPA1 channels: a viable strategy for treating asthma using Chinese herbal medicines.Frontiers in pharmacology · 2025Review
- New options for targeting TRPV1 receptors for cancer treatment: odorous Chinese herbal medicine.Frontiers in oncology · 2025Review
- How much does TRPV1 deviate from an ideal MWC-type protein?Biophysical journal · 2024Article
- Zingiber Officinale Roscoe: The Antiarthritic Potential of a Popular Spice-Preclinical and Clinical Evidence.Nutrients · 2024Review
- The "root" causes behind the anti-inflammatory actions of ginger compounds in immune cells.Frontiers in immunology · 2024Review
- Integrated virtual screening andFrontiers in pharmacology · 2024Article
- Opening of capsaicin receptor TRPV1 is stabilized equally by its four subunits.The Journal of biological chemistry · 2023Article
- Application of a Magnetic Platform in α6 Integrin-Positive iPSC-TM Purification.Bioengineering (Basel, Switzerland) · 2023Article
- Natural Active Ingredients and TRPV1 Modulation: Focus on Key Chemical Moieties Involved in Ligand-Target Interaction.Plants (Basel, Switzerland) · 2023Review
- A journey from molecule to physiology andFrontiers in pharmacology · 2023Review
- Regulation of transient receptor potential channels by traditional Chinese medicines and their active ingredients.Frontiers in pharmacology · 2022Review
- Gallic Acid Inhibits Mesaconitine-Activated TRPV1-Channel-Induced Cardiotoxicity.Evidence-based complementary and alternative medicine : eCAM · 2022Article
- Lipid-dependent sequential allosteric activation of heat-sensing TRPV1 channels by anchor-stereoselective "hot" vanilloid compounds and analogs.Biochemistry and biophysics reports · 2021Review
- Ginger facilitates cell migration and heat tolerance in mouse fibroblast cells.Molecular medicine reports · 2021Article
- Transient Receptor Potential Vanilloid Subtype 1: Potential Role in Infection, Susceptibility, Symptoms and Treatment of COVID-19.Frontiers in medicine · 2021Review
- Therapeutic Effects of Traditional Chinese Medicine on Cardiovascular Diseases: the Central Role of Calcium Signaling.Frontiers in pharmacology · 2021Review
- Potential Interplay between Nrf2, TRPA1, and TRPV1 in Nutrients for the Control of COVID-19.International archives of allergy and immunology · 2021Review
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
Abstract
background and purposeLike chili peppers, gingers produce pungent stimuli by a group of vanilloid compounds that activate the nociceptive transient receptor potential vanilloid 1 (TRPV1) ion channel. How these compounds interact with TRPV1 remains unclear. EXPERIMENTAL APPROACH: We used computational structural modelling, functional tests (electrophysiology and calcium imaging), and mutagenesis to investigate the structural mechanisms underlying ligand-channel interactions. KEY
resultsThe potency of three principal pungent compounds from ginger -shogaol, gingerol, and zingerone-depends on the same two residues in the TRPV1 channel that form a hydrogen bond with the chili pepper pungent compound, capsaicin. Computational modelling revealed binding poses of these ginger compounds similar to those of capsaicin, including a "head-down tail-up" orientation, two specific hydrogen bonds, and important contributions of van der Waals interactions by the aliphatic tail. Our study also identified a novel horizontal binding pose of zingerone that allows it to directly interact with the channel pore when bound inside the ligand-binding pocket. These observations offer a molecular level explanation for how unique structures in the ginger compounds affect their channel activation potency. CONCLUSIONS AND IMPLICATIONS: Mechanistic insights into the interactions of ginger compounds and the TRPV1 cation channel should help guide drug discovery efforts to modulate nociception.
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