Discovery of Bavachin as a Dual Trk-A/Trk-B Agonist via Integrated Computational Screening and Experimental Validation
Sachin P. PatiliD, Bella R. Kuehn, Ryan Schlosser, John Samohod
Abstract
Neurotrophins regulate neuronal survival, differentiation, and synaptic plasticity through activation of tropomyosin receptor kinase (Trk) receptors, and their dysregulation is strongly implicated in neurodegenerative disorders, including Alzheimer's disease. However, the therapeutic application of recombinant neurotrophins remains limited by poor bioavailability, rapid degradation, and inadequate blood brain barrier permeability. Here, we report the discovery of Bavachin as a dual Trk-A/Trk-B neurotrophin mimetic via an integrated computational screening and experimental validation approach. Structure-based virtual screening of a bioactive natural product library derived from Traditional Chinese Medicine, combined with a novel consensus-ranking strategy, enabled the identification of flavonoid scaffolds targeting neurotrophin-binding sites of Trk receptors. Among these, Bavachin demonstrated robust, dose-dependent activation of both Trk-A and Trk-B receptors, but not Trk-C, indicating receptor selectivity. Induced-fit docking and molecular dynamics simulations revealed stable binding of Bavachin within conserved and receptor-specific ligand-binding pockets, consistent with its dual agonist activity. Collectively, this study identifies Bavachin as a putative small-molecule neurotrophin mimetic and establishes an integrated computational and experimental framework for the discovery of dual Trk-A/Trk-B agonists for neurodegenerative disease therapeutics.
02 /Specification & Classification
Click any tag to browse matching papers- Citations
- 0
- Research Focus
- Approach
Reproducibility ledger
Nobody has reported trying to reproduce this paper yet. Did you replicate an experiment or run the code? Your report saves the next lab a week.
Sign in to file a reproducibility report.
Related papers
- In silico analysis of Bacopa monnieri (L.) Wettst. compounds for drug development against Neurodegenerative Disorders
S. Sangeet, A. Khan, … P. K. Hui·bioRxiv·Mar 30, 2022
- Structural Basis for the transmembrane signaling and antidepressant-induced activation of the receptor tyrosine kinase TrkB
E. F. Kot, S. A. Goncharuk, … K. S. Mineev·bioRxiv·Jun 6, 2023
- Structure-Based Virtual Screening Identifies TREM2-Targeted Small Molecules that Enhance Microglial Phagocytosis
Sungwoo Cho, Baljit Kaur, … Moustafa Tarek Gabr·ChemMedChemPeer-reviewed·Jan 1, 2026
- Simulation of neurotrophin receptor transmembrane helix interactions reveals active states and distinct signaling mechanisms
Christina Athanasiou, Ainara Claveras Cabezudo, … Rebecca C. Wade·JACS AuPeer-reviewed·Apr 27, 2025
- Antidepressant drugs act by directly binding to TRKB neurotrophin receptors
Plinio Cabrera Casarotto, Mykhailo Girych, … Eero Ċastrén·CellPeer-reviewed·Feb 18, 2021
- Identification of novel and structurally diverse N-Methyl-D-Aspartate Receptor Antagonists: Successful Application of Pharmacophore Modeling, Virtual Screening and Molecular Docking
Mukta Sharma, Anupama Mittal, … Sarvesh Paliwal·bioRxiv·May 4, 2018