ArticleNature communications2022
Structural insights into TRPV2 activation by small molecules.
Article in Nature communications, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 45 papers.
What it found
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Who cites it
45 citing papers in PubMed, 59 citations in OpenAlex.
- Reprogramming macrophage mechanosensation via TRPV4 modulating mechano-immunotherapy controls fibrotic encapsulation of biomaterial implants.Bioactive materials · 2026Article
- An Extracellular Pore‑Targeting Peptide Defines a Designable Allosteric Site in TRPV2.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Structural origins of species-specific differences in TRPV2 activation.Nature communications · 2026Article
- Non-canonical pore architecture underlies constitutive gating of human retinal TRPM1.Nature communications · 2026Article
- Inactivation Switch for Run-up in TRPV2.Research square · 2026Article
- Thermodynamic coupling between cold and heat activations of TRPV2.Scientific reports · 2026Article
- Hyperviscous Diabetic Bone Marrow Niche Impairs BMSCs Osteogenesis via TRPV2-Mediated Cytoskeletal-Nuclear Mechanotransduction.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- TRPV2 regulates cell fate in the human granulosa-like tumor cell line KGN: implications for granulosa cell tumors and cannabidiol.Cell communication and signaling : CCS · 2026Article
- TRPV2 and TRPC5 are potential targets for astringent phytochemicals.Current research in food science · 2026Article
- Tranilast Does Not Inhibit TRPV2.Cells · 2025Article
- Visualizing insecticide control of insect TRP channel function and assembly.Nature communications · 2025Article
- Physiological functions and pharmacological targeting of transient receptor potential channels.Pharmacological reviews · 2025Review
- Article
- TRPV2 Regulates Function of Human Neutrophil Granulocytes.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2025Article
- Molecular determinants of 2-aminoethoxydiphenyl borate sensitivity of transient receptor potential vanilloid 2-unexpected differences between 2 rodent orthologs.Molecular pharmacology · 2025Article
- Structural insights into TRPV2 modulation by probenecid.Nature structural & molecular biology · 2025Article
- Molecular insights into de novo small-molecule recognition by an intron RNA structure.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Heat Shock Strengthens the Protective Potential of MSCs in Liver Injury by Promoting EV Release Through Upregulated Autophagosome Formation.Journal of extracellular vesicles · 2025Article
- Mechanisms of Cell Death Induced by Cannabidiol Against Tumor Cells: A Review of Preclinical Studies.Plants (Basel, Switzerland) · 2025Review
- Forty sites of TRP channel regulation.Current opinion in chemical biology · 2025Review
Corrections and comments
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Authors and funding
12 authors at 4 institutions in 4 countries.
Funding
Abstract
Transient receptor potential vanilloid 2 (TRPV2) is involved in many critical physiological and pathophysiological processes, making it a promising drug target. Here we present cryo-electron microscopy (cryo-EM) structures of rat TRPV2 in lipid nanodiscs activated by 2-aminoethoxydiphenyl borate (2-APB) and propose a TRPV2-specific 2-ABP binding site at the interface of S5 of one monomer and the S4-S5 linker of the adjacent monomer. In silico docking and electrophysiological studies confirm the key role of His521 and Arg539 in 2-APB activation of TRPV2. Additionally, electrophysiological experiments show that the combination of 2-APB and cannabidiol has a synergetic effect on TRPV2 activation, and cryo-EM structures demonstrate that both drugs were able to bind simultaneously. Together, our cryo-EM structures represent multiple functional states of the channel, providing a native picture of TRPV2 activation by small molecules and a structural framework for the development of TRPV2-specific activators.
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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.