Inhibition of the oncogenic GTPase dynamin-related protein 1 (DRP1) by the FDA-approved drug fosaprepitant: In silico, biophysical, and in vitro characterization of its anti-myeloma activity - PubMed
3 hours ago
- #Mitochondrial Fission
- #Drug Repurposing
- #Multiple Myeloma
- DRP1 is a key GTPase regulating mitochondrial fission and is considered an oncogenic target.
- Virtual screening of FDA-approved drugs identified fosaprepitant as a potential DRP1 inhibitor.
- Fosaprepitant directly binds to DRP1's GTPase domain, inhibiting its activity, as shown by computational docking, GTPase assays, and STD-NMR spectroscopy.
- In multiple myeloma cells, fosaprepitant induces mitochondrial hyperfusion, reduces viability and colony formation, disrupts OXPHOS, and triggers apoptosis.
- This study proposes fosaprepitant as a repurposed anti-cancer drug targeting DRP1, offering a new therapeutic strategy.