δ-opioid receptor (DOR) is a promising therapeutic target for developing safer treatments for pain and neuroprotection. In this study, we applied a structure-guided drug-repurposing workflow to identify FDA-approved drugs with predicted DOR-binding and agonist-like structural features. Using a validated GNINA-based docking protocol with an active-state DOR model (PDB ID: 6PT3), we screened 2342 approved compounds and identified 39 candidates with predicted submicromolar binding affinities. These hits were further evaluated through molecular dynamics simulations, binding pocket volume analysis, and principal component analysis, which enabled the prioritization of two leading candidates, aprepitant and mavorixafor. Both compounds formed stable receptor-ligand complexes, maintained persistent interactions with Asp128, promoted contraction of the orthosteric pocket, and retained favorable redocking scores on the MD-refined receptor conformations. Overall, these results identify aprepitant and mavorixafor as promising putative DOR agonists and provide a rational foundation for their experimental validation through binding, functional, and in vivo pain studies in the future.

Structure-Guided Repurposing of Approved Drugs Identifies Aprepitant and Mavorixafor as Putative δ-Opioid Receptor Agonist Candidates

Rocco Buccheri;Carlo Reale;Carmela Parenti;Lorella Pasquinucci;Antonio Rescifina
2026-01-01

Abstract

δ-opioid receptor (DOR) is a promising therapeutic target for developing safer treatments for pain and neuroprotection. In this study, we applied a structure-guided drug-repurposing workflow to identify FDA-approved drugs with predicted DOR-binding and agonist-like structural features. Using a validated GNINA-based docking protocol with an active-state DOR model (PDB ID: 6PT3), we screened 2342 approved compounds and identified 39 candidates with predicted submicromolar binding affinities. These hits were further evaluated through molecular dynamics simulations, binding pocket volume analysis, and principal component analysis, which enabled the prioritization of two leading candidates, aprepitant and mavorixafor. Both compounds formed stable receptor-ligand complexes, maintained persistent interactions with Asp128, promoted contraction of the orthosteric pocket, and retained favorable redocking scores on the MD-refined receptor conformations. Overall, these results identify aprepitant and mavorixafor as promising putative DOR agonists and provide a rational foundation for their experimental validation through binding, functional, and in vivo pain studies in the future.
2026
analgesia
conformational dynamics
drug repurposing
molecular docking
virtual screening
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.11769/719391
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus ND
  • ???jsp.display-item.citation.isi??? 0
social impact