The sigma-1 receptor as a pluripotent modulator in living systems

TP Su, TC Su, Y Nakamura, SY Tsai - Trends in pharmacological sciences, 2016 - cell.com
The sigma-1 receptor (Sig-1R) is an endoplasmic reticulum (ER) protein that resides
specifically in the mitochondria-associated endoplasmic reticulum (ER) membrane (MAM) …

Repurposing sigma-1 receptor ligands for COVID-19 therapy?

JM Vela - Frontiers in Pharmacology, 2020 - frontiersin.org
Outbreaks of emerging infections, such as COVID-19 pandemic especially, confront health
professionals with the unique challenge of treating patients. With no time to discover new …

Structures of the σ2 receptor enable docking for bioactive ligand discovery

A Alon, J Lyu, JM Braz, TA Tummino, V Craik… - Nature, 2021 - nature.com
The σ2 receptor has attracted intense interest in cancer imaging, psychiatric disease,
neuropathic pain,–and other areas of biology,. Here we determined the crystal structure of …

Highly specific σ2R/TMEM97 ligand FEM-1689 alleviates neuropathic pain and inhibits the integrated stress response

MS Yousuf, JJ Sahn, H Yang… - Proceedings of the …, 2023 - National Acad Sciences
The sigma 2 receptor (σ2R) was described pharmacologically more than three decades ago,
but its molecular identity remained obscure until recently when it was identified as …

Small molecules selectively targeting sigma-1 receptor for the treatment of neurological diseases

N Ye, W Qin, S Tian, Q Xu, EA Wold… - Journal of medicinal …, 2020 - ACS Publications
The sigma-1 (σ1) receptor, an enigmatic protein originally classified as an opioid receptor
subtype, is now understood to possess unique structural and functional features of its own …

Cannabidiol enhances morphine antinociception, diminishes NMDA-mediated seizures and reduces stroke damage via the sigma 1 receptor

M Rodríguez-Muñoz, Y Onetti, E Cortés-Montero… - Molecular brain, 2018 - Springer
Cannabidiol (CBD), the major non-psychotomimetic compound present in the Cannabis
sativa plant, exhibits therapeutic potential for various human diseases, including chronic …

[HTML][HTML] Efficacy of a novel sigma-1 receptor antagonist for oxaliplatin-induced neuropathy: a randomized, double-blind, placebo-controlled phase IIa clinical trial

J Bruna, S Videla, AA Argyriou, R Velasco, J Villoria… - …, 2018 - Elsevier
This trial assessed the efficacy of MR309 (a novel selective sigma-1 receptor ligand
previously developed as E-52862) in ameliorating oxaliplatin-induced peripheral …

Roles of sigma-1 receptors on mitochondrial functions relevant to neurodegenerative diseases

TY Weng, SYA Tsai, TP Su - Journal of biomedical science, 2017 - Springer
Abstract The sigma-1 receptor (Sig-1R) is a chaperone that resides mainly at the
mitochondrion-associated endoplasmic reticulum (ER) membrane (called the MAMs) and …

Sigma 1 receptor: a new therapeutic target for pain

D Zamanillo, L Romero, M Merlos, JM Vela - European Journal of …, 2013 - Elsevier
Abstract Sigma 1 receptor (σ 1 receptor) is a unique ligand-regulated molecular chaperone
located mainly in the endoplasmic reticulum and the plasma membrane. σ 1 receptor is …

TRPA1 modulation by Sigma-1 receptor prevents oxaliplatin-induced painful peripheral neuropathy

A Marcotti, J Fernández-Trillo, A González… - Brain, 2023 - academic.oup.com
Chemotherapy-induced peripheral neuropathy is a frequent, disabling side effect of
anticancer drugs. Oxaliplatin, a platinum compound used in the treatment of advanced …