bioRxiv Science⌕ Search

Biology subjects

Patil, S. P.

Publications and source records attributed to Patil, S. P..

3 recordsLinked to original sources

Discovery of Bavachin as a Dual Trk-A/Trk-B Agonist via Integrated Computational Screening and Experimental Validation

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.

neuroscience↗

Simultaneous Functional Ultrasound, Intrinsic Optical Signal and Widefield Calcium Neuroimaging

Functional ultrasound (fUS) maps cerebral blood volume (CBV) but lacks molecular and neuronal specificity. By simultaneously integrating fUS with optical imaging, we show that fUS-derived CBV correlates with both optically measured hemoglobin and neuronal calcium activity in awake mice. We further derive hemodynamic response functions linking calcium activity to CBV during spontaneous and sensory-evoked activity. Application to a mouse glioblastoma model demonstrates utility for studying neurovascular dysfunction in complex neuropathologies.

neuroscience↗

Loss of clathrin heavy chain enhances actin-dependent stiffness of mouse embryonic stem cells

Mouse embryonic stem cells (mESCs) display unique mechanical properties, including low cell stiffness, and specific responses to features of the underlying substratum. Using atomic force microscopy (AFM), we demonstrate that mESCs lacking the clathrin heavy chain (Cltc), display higher Youngs modulus, indicative of greater cellular stiffness, in comparison to WT mESCs. We have previously shown that mESCs lacking Cltc display a loss of pluripotency, and an initiation of differentiation. The increased stiffness observed in these cells was accompanied by the presence of actin stress fibres and accumulation of the inactive, phosphorylated, actin binding protein, Cofilin. Treatment of Cltc knockdown mESCs with actin polymerization inhibitors resulted in a decrease in the Youngs modulus, to values similar to those obtained with WT mESCs. However, the expression profile of pluripotency factors was not rescued. This indicates that a restoration of mechanical properties, through modulation of the actin cytoskeleton, may not always be accompanied by a change in the expression of critical transcription factors that regulate the state of a stem cell, and that this may be dependent on the presence of active endocytosis in a cell.

cell biology↗