ArticleBiochemical and biophysical research communications2019
A distinct structural mechanism underlies TRPV1 activation by piperine.
Article in Biochemical and biophysical research communications, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers, 1 of them a synthesis that pooled it.
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The trial behind it
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
25 citing papers in PubMed, 1 synthesis or guideline pooled it, 51 citations in OpenAlex.
- A Systematic Review of the Anti-seizure and Antiepileptic Effects and Mechanisms of Piperine.Central nervous system agents in medicinal chemistry · 2025Pooled it
- Effect of pipernonaline from Piper retrofractum on memory disorder in mice and neurite outgrowth activity of PC12 cells.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Article
- Article
- Piperine disrupts the OFF state of the resting thick filament of rat skeletal muscle, enhancing dynamic contractility in a fibre-type-dependent manner.The Journal of physiology · 2026Article
- Topical Piperine for the Management of Burning Mouth Syndrome: A Case Series.Journal of clinical medicine · 2026Article
- "Pepper": Different Spices, One Name-Analysis of Sensory and Biological Aspects.Molecules (Basel, Switzerland) · 2025Review
- Natural solutions for glowing skin: spices.Frontiers in nutrition · 2025Review
- Isolation, Structure Elucidation, and Bioactivity Evaluation of Two Alkaloids FromFood science & nutrition · 2024Article
- Capsaicin: Emerging Pharmacological and Therapeutic Insights.Current issues in molecular biology · 2024Review
- How much does TRPV1 deviate from an ideal MWC-type protein?Biophysical journal · 2024Article
- A Stable Cell Line Co-expressing hTRPV1 and GCaMP6s: A Novel Cell-based Assay For High-throughput Screening of hTRPV1 Agonists.Combinatorial chemistry & high throughput screening · 2024Article
- Impact of TRPV1 on Pathogenesis and Therapy of Neurodegenerative Diseases.Molecules (Basel, Switzerland) · 2023Review
- Pungency Perception and the Interaction with Basic Taste Sensations: An Overview.Foods (Basel, Switzerland) · 2023Review
- Opening of capsaicin receptor TRPV1 is stabilized equally by its four subunits.The Journal of biological chemistry · 2023Article
- Natural Active Ingredients and TRPV1 Modulation: Focus on Key Chemical Moieties Involved in Ligand-Target Interaction.Plants (Basel, Switzerland) · 2023Review
- Extent of intrinsic disorder and NMR chemical shift assignments of the distal N-termini from human TRPV1, TRPV2 and TRPV3 ion channels.Biomolecular NMR assignments · 2022Article
- Piperine and Its Metabolite's Pharmacology in Neurodegenerative and Neurological Diseases.Biomedicines · 2022Review
- Eugenol improves high-fat diet/streptomycin-induced type 2 diabetes mellitus (T2DM) mice muscle dysfunction by alleviating inflammation and increasing muscle glucose uptake.Frontiers in nutrition · 2022Article
- Molecular and pharmacological aspects of piperine as a potential molecule for disease prevention and management: evidence from clinical trials.Beni-Suef University journal of basic and applied sciences · 2022Review
- Lipid-dependent sequential allosteric activation of heat-sensing TRPV1 channels by anchor-stereoselective "hot" vanilloid compounds and analogs.Biochemistry and biophysics reports · 2021Review
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
Abstract
Piperine, the principle pungent compound in black peppers, is known to activate the capsaicin receptor TRPV1 ion channel. How piperine interacts with the channel protein, however, remains unclear. Here we show that piperine binds to the same ligand-binding pocket as capsaicin but in different poses. There was no detectable detrimental effect when T551 and E571, two major sites known to form hydrogen bond with capsaicin, were mutated to a hydrophobic amino acid. Computational structural modeling suggested that piperine makes interactions with multiple amino acids within the ligand binding pocket, including T671 on the pore-forming S6 segment. Mutations of this residue could substantially reduce or even eliminate piperine-induced activation, confirming that T671 is an important site. Our results suggest that the bound piperine may directly interact with the pore-forming S6 segment to induce channel opening. These findings help to explain why piperine is a weak agonist, and may guide future efforts to develop novel pharmaceutical reagents targeting TRPV1.
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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.