ArticleProceedings of the National Academy of Sciences of the United States of America2016
Understanding TRPV1 activation by ligands: Insights from the binding modes of capsaicin and resiniferatoxin.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 91 papers, 2 of them syntheses that pooled it.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
91 citing papers in PubMed, 2 syntheses or guidelines pooled it, 165 citations in OpenAlex.
- Modulation of transient receptor potential (TRP) channels by plant derived substances used in over-the-counter cough and cold remedies.Respiratory research · 2023Pooled it
- Antinociceptive Activity of Chemical Components of Essential Oils That Involves Docking Studies: A Review.Frontiers in pharmacology · 2020Pooled it
- Cholesterol inhibits capsaicin activation of the TRPV1 channel.Channels (Austin, Tex.) · 2026Article
- Modulation of nociceptive nerve activity as a novel therapeutic strategy in acute myeloid leukemia.Fundamental research · 2026Article
- Article
- Review
- TRPV1 in Cardiovascular Disease: A Molecular Nexus of Treatment.Biomolecules · 2026Review
- Review
- Article
- Capsaicinoid Glucoside Attenuates Lipid Accumulation in HepG2 Cells Through TRPV1/AMPK-Dependent Signaling Pathway.Food science & nutrition · 2025Article
- Neurotoxins Acting on TRPV1-Building a Molecular Template for the Study of Pain and Thermal Dysfunctions.Toxins · 2025Review
- Spinal Involvement of TRPV1 and PI3K/AKT/mTOR Pathway During Chronic Postoperative Pain in Mice.Brain sciences · 2025Article
- Role of homovanillic acid esters in the regulation of skin inflammatory pathways and their effect on tight junction protein expression.Frontiers in pharmacology · 2025Article
- Heat acclimation defense against exertional heat stroke by improving the function of preoptic TRPV1 neurons.Theranostics · 2025Article
- Protective Effects of Capsaicinoid Glucoside from Fresh Hot Peppers Against Hydrogen peroxide-induced Oxidative Stress in HepG2 Cells Through-dependent Signaling Pathway.Plant foods for human nutrition (Dordrecht, Netherlands) · 2024Article
- Direct Photobiomodulation Therapy on the Sciatic Nerve Significantly Attenuates Acute Nociceptive Sensitivity Without Affecting Motor Output.Neuromodulation : journal of the International Neuromodulation Society · 2024Article
- TRPV1: The key bridge in neuroimmune interactions.Journal of intensive medicine · 2024Review
- Three-Dimensional Quantitative Structure-Activity Relationship Study of Transient Receptor Potential Vanilloid 1 Channel Antagonists Reveals Potential for Drug Design Purposes.International journal of molecular sciences · 2024Article
- Article
- Capsaicin orchestrates metastasis in gastric cancer via modulating expression of TRPV1 channels and driving gut microbiota disorder.Cell communication and signaling : CCS · 2023Article
31 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
Abstract
The transient receptor potential cation channel subfamily V member 1 (TRPV1) or vanilloid receptor 1 is a nonselective cation channel that is involved in the detection and transduction of nociceptive stimuli. Inflammation and nerve damage result in the up-regulation of TRPV1 transcription, and, therefore, modulators of TRPV1 channels are potentially useful in the treatment of inflammatory and neuropathic pain. Understanding the binding modes of known ligands would significantly contribute to the success of TRPV1 modulator drug design programs. The recent cryo-electron microscopy structure of TRPV1 only provides a coarse characterization of the location of capsaicin (CAPS) and resiniferatoxin (RTX). Herein, we use the information contained in the experimental electron density maps to accurately determine the binding mode of CAPS and RTX and experimentally validate the computational results by mutagenesis. On the basis of these results, we perform a detailed analysis of TRPV1-ligand interactions, characterizing the protein ligand contacts and the role of individual water molecules. Importantly, our results provide a rational explanation and suggestion of TRPV1 ligand modifications that should improve binding affinity.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.