Niraparib Demonstrates Therapeutic Potential in Multiple Sclerosis through Inhibition of IL-17A Receptor Interaction and Promotion of Remyelination
IL-17A is a pro-inflammatory cytokine that significantly contributes to the pathogenesis of autoimmune diseases, including multiple sclerosis (MS). Previous studies have suggested that PARP-1 inhibitors can modulate IL-17A-mediated inflammation, prompting the investigation of Niraparib, an FDA-approved PARP-1 inhibitor, as a potential therapeutic agent for MS. In this study, we hypothesized that Niraparib could disrupt the interaction between IL-17A and its receptor, IL-17RA. To evaluate this, we employed a binary quantitative structure-activity relationship (QSAR) model against anti-inflammatory diseases, which indicated Niraparib's potential efficacy against MS. In silico analyses were conducted to identify key interaction sites and critical amino acid residues involved in the IL-17A/IL-17RA binding. Molecular docking simulations demonstrated Niraparib's capability to interfere with these interactions. It has demonstrated significant efficacy in inhibiting the interaction between the IL-17A ligand and its receptor via reporter assay. In vivo assessments were performed using a cuprizone-induced demyelination model. Immune profiling revealed modulation of various T cell subsets and B cells, while cytokine analysis indicated a shift in inflammatory responses. Histological evaluations confirmed reduced demyelination and enhanced remyelination in affected brain regions. These findings support Niraparib's potential as a therapeutic option for MS, warranting further exploration of its mechanisms and clinical relevance.
Authors
- Müge Didem Orhan (ORCID: https://orcid.org/0000-0001-9014-3838)
- Lalehan Oktay (ORCID: https://orcid.org/0000-0002-3293-5551)
- Hüseyin Tunç (ORCID: https://orcid.org/0000-0001-6450-5380)
- Fatih Eren (ORCID: https://orcid.org/0000-0001-8126-2413)
- Serdar Durdağı (ORCID: https://orcid.org/0000-0002-0426-0905)
- Ayse Kurt Cinar
- Aybek Kagan Yesil
Institutions
- Bahçeşehir University (TR)
- Society for Neuroscience (US)
- University of Bonn (DE)
- Recep Tayyip Erdoğan University (TR)
- Kochi Medical School Hospital (JP)
- Laboratory of Molecular Genetics (PL)
- Faculty (United Kingdom) (GB)
- California Liver Research Institute (US)
- Institute of Neurology, Psychiatry and Narcology (UA)
- Institute of Molecular Biology and Biophysics (RU)
- International Drug Development (FR)
- Marmara University (TR)
- Graduate School USA (US)
Publication Details
- Journal
- ACS Chemical Neuroscience
- Published
- 2025-09-09
- DOI
- https://doi.org/10.1021/acschemneuro.5c00519
- Primary Topic
- PARP inhibition in cancer therapy
- Type
- article
- Field-Weighted Citation Impact
- 0.00