In silico pharmacology · 2026
Drug repurposing for psoriasis: virtual screening, molecular dynamics, and ADMET profiling for the identification of potential DHFR inhibitors.
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Mazzone Patrizio, Peretto Giovanni, Radinovic Andrea, Limite Luca Rosario, Marzi Alessandra, Sala Simone, Cireddu Manuela, Vegara Pasquale, Baratto Francesca, Paglino Gabriele, D'Angelo Giuseppe, Cianfanelli Lorenzo, Altizio Savino, Lipartiti Felicia, Frontera Antonio, Bisceglia Caterina, Gulletta Simone, Bella Paolo Della
Аннотация
UNLABELLED: Psoriasis is a chronic dermatological disorder affecting approximately 43 million people globally, with current treatments limited by toxicity and high costs. Dihydrofolate reductase (DHFR), a crucial enzyme in folate metabolism essential for DNA synthesis, represents a validated therapeutic target for psoriasis. This study aimed to identify FDA-approved drugs with potential DHFR inhibitory activity using an integrated computational approach combining molecular docking, ADMET prediction, and molecular dynamics simulations. A total of 2311 FDA-approved drugs from DrugBank were docked against human DHFR (PDB ID: 1S3V). Ten compounds exhibited strong binding affinities (MolDock scores: -209.9 to -261.3 kcal/mol), with Velpatasvir showing the highest score (-261.3 kcal/mol), followed by Ledipasvir (-242.4 kcal/mol). ADMET profiling classified both compounds as Medium Priority. To evaluate binding stability, 20 ns triplicate MD simulations and MM-GBSA calculations were performed. Both compounds formed stable complexes, with mean protein RMSD values of 2.36 ± 0.10 Å (Velpatasvir) and 2.37 ± 0.26 Å (Ledipasvir). Velpatasvir demonstrated more consistent binding across replicates (RMSF: 2.79 ± 1.65 Å; MM-GBSA SD: 5.52 kcal/mol) compared to Ledipasvir (RMSF: 6.22 ± 2.12 Å; MM-GBSA SD: 13.01 kcal/mol). PCA and DCCM analyses revealed that Velpatasvir induced highly consistent motion patterns, while Ledipasvir exhibited more variable conformational sampling. Both compounds showed favourable binding free energies (Velpatasvir: -43.39 ± 5.52 kcal/mol; Ledipasvir: -49.19 ± 13.01 kcal/mol). These findings suggest Velpatasvir and Ledipasvir as promising DHFR inhibitors warranting experimental validation, and demonstrate drug repurposing as a cost-effective strategy for discovering novel psoriasis therapies.
SUPPLEMENTARY INFORMATION: The online version contains supplementary material available at https://doi.org/10.1007/s40203-026-00761-x.
SUPPLEMENTARY INFORMATION: The online version contains supplementary material available at https://doi.org/10.1007/s40203-026-00761-x.