ArticleJournal of enzyme inhibition and medicinal chemistry2022
A new era for the design of TRPV1 antagonists and agonists with the use of structural information and molecular docking of capsaicin-like compounds.
Article in Journal of enzyme inhibition and medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 23 citations in OpenAlex.
- Exploring molecular frameworks for modulating NLRP3-driven neuroinflammation in Alzheimer's disease.Molecular diversity · 2026Review
- Design, synthesis and structural mechanism of action of TRPV1 agonist MSP20 with long-lasting analgesic effect.Nature communications · 2026Article
- Phytochemical Composition and Biological Activities ofPlants (Basel, Switzerland) · 2026Review
- Inhibition of TRPV1 Ameliorates Depression-Like Behaviors in Male Mice by Regulating Neuroinflammation and Neurogenesis via the JAK2/STAT3 Pathway.Molecular neurobiology · 2026Article
- Cibotii Rhizoma extract protects rat dorsal root ganglion neurons against HBMC complementary medicine and therapies · 2025Article
- Review
- Involvement of TRPV1 and MOR-NMDAR complex on the antiallodynic effect of LMH-2, a sigma-1 receptor antagonist, in mouse model of diabetic neuropathy - a behavioral approach.Pharmacological reports : PR · 2025Article
- Paracetamol: the potential therapeutic pathways defining its clinical use.Inflammopharmacology · 2025Review
- Indole-2-Carboxamide as an Effective Scaffold for the Design of New TRPV1 Agonists.Molecules (Basel, Switzerland) · 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
- Nerelimomab Alleviates Capsaicin-Induced Acute Lung Injury by Inhibiting TNF Signaling and Apoptosis.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Capsaicin: Emerging Pharmacological and Therapeutic Insights.Current issues in molecular biology · 2024Review
- To Explore the Putative Molecular Targets of Diabetic Nephropathy and their Inhibition Utilizing Potential Phytocompounds.Current medicinal chemistry · 2024Review
- Binding interactions of fatty acyl lipid mediators within the vanilloid pocket of TRPV1: A molecular dynamics study.Prostaglandins & other lipid mediators · 2023Review
- In Silico Drug Repurposing Framework Predicts Repaglinide, Agomelatine and Protokylol as TRPV1 Modulators with Analgesic Activity.Pharmaceutics · 2022Article
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1 author at 1 institution in 1 country.
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No grant is acknowledged in the PubMed record.
Abstract
The design of TRPV1 antagonists and agonists has reached a new era since TRPV1 structures at near-atomic resolution are available. Today, the ligand-binding forms of several classical antagonists and agonists are known; therefore, the specific role of key TRPV1's residues in binding of ligands can be elucidated. It is possible to place the well-defined pharmacophore of TRPV1 ligands, conformed by head, neck, and tail groups, in the right pocket regions of TRPV1. It will allow a more thorough use of molecular modelling methods to conduct more effective rational drug design protocols. In this work, important points about the interactions between TRPV1 and capsaicin-like compounds are spelled out, based on the known pharmacophore of the ligands and the already available TRPV1 structures. These points must be addressed to generate reliable poses of novel candidates and should be considered during the design of novel TRPV1 antagonists and agonists.
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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.