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.

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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
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article

Abstract 2784 Development of Novel Sigma-2 Receptor Inhibitors: An in vitro and in silico study

Mubaraq A Toriola, Leggy A. Arnold, Douglas C. Stafford, M. Rohan Fernando
Journal of Biological Chemistry
Pharmacological Receptor Mechanisms and Effects
article

Abstract 2784 Development of Novel Sigma-2 Receptor Inhibitors: An in vitro and in silico study

Mubaraq A Toriola, Leggy A. Arnold, Douglas C. Stafford, M. Rohan Fernando
article en

Abstract

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.

Journal of Biological ChemistryVol. 301(5)
Bridge University (SS)
Openalex Percentile: Top 88%
Pharmacological Receptor Mechanisms and Effects
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Abstract 2784 Development of Novel Sigma-2 Receptor Inhibitors: An in vitro and in silico study — Mubaraq A Toriola, Leggy A. Arnold, et al. · Journal of Biological Chemistry (2025) | TGRS Research Map | TGRS