Abstract 2784 Development of Novel Sigma-2 Receptor Inhibitors: An in vitro and in silico study
The sigma-2 receptor (S2R, encoded by TMEM97) is a transmembrane protein that has emerged as a promising target for therapeutic intervention in various disease areas, including cancer biomarker detection, neurodegenerative disorders, and neuropathic pain. Additionally, sigma-2 receptors are implicated in critical cellular functions such as cell proliferation, immune modulation, and ion channel regulation. To address the unmet medical need, we designed and synthesized a novel class of benzodiazepines that selectively target the σ2 receptor without binding to GABA(A) receptors.
Authors
- Mubaraq A Toriola (ORCID: https://orcid.org/0000-0002-0754-4225)
- Leggy A. Arnold (ORCID: https://orcid.org/0000-0003-1411-1572)
- Douglas C. Stafford (ORCID: https://orcid.org/0000-0003-1032-7800)
- M. Rohan Fernando (ORCID: https://orcid.org/0000-0002-3596-3160)
Institutions
- Bridge University (SS)
Publication Details
- Journal
- Journal of Biological Chemistry
- Published
- 2025-05-01
- DOI
- https://doi.org/10.1016/j.jbc.2025.109083
- Primary Topic
- Pharmacological Receptor Mechanisms and Effects
- Type
- article
- Field-Weighted Citation Impact
- 0.00