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 …

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 …

Targeting sigma receptors for the treatment of neurodegenerative and neurodevelopmental disorders

DS Malar, P Thitilertdecha, KS Ruckvongacheep… - CNS drugs, 2023 - Springer
The sigma-1 receptor is a 223 amino acid-long protein with a recently identified structure.
The sigma-2 receptor is a genetically unrelated protein with a similarly shaped binding …

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 …

Pharmacological properties of S1RA, a new sigma‐1 receptor antagonist that inhibits neuropathic pain and activity‐induced spinal sensitization

L Romero, D Zamanillo, X Nadal… - British journal of …, 2012 - Wiley Online Library
BACKGROUND AND PURPOSE The sigma‐1 (σ1) receptor is a ligand‐regulated molecular
chaperone that has been involved in pain, but there is limited understanding of the actions …

Synthesis and Biological Evaluation of the 1-Arylpyrazole Class of σ1 Receptor Antagonists: Identification of 4-{2-[5-Methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy] …

JL Díaz, R Cuberes, J Berrocal… - Journal of medicinal …, 2012 - ACS Publications
The synthesis and pharmacological activity of a new series of 1-arylpyrazoles as potent σ1
receptor (σ1R) antagonists are reported. The new compounds were evaluated in vitro in …

[HTML][HTML] Role of sigma-1 receptors in paclitaxel-induced neuropathic pain in mice

FR Nieto, CM Cendán, C Sánchez-Fernández… - The journal of pain, 2012 - Elsevier
Sigma-1 (σ1) receptors play a role in different types of pain and in central sensitization
mechanisms; however, it is unknown whether they are involved in chemotherapy-induced …

Sigma 2 receptor/Tmem97 agonists produce long lasting antineuropathic pain effects in mice

JJ Sahn, GL Mejia, PR Ray, SF Martin… - ACS chemical …, 2017 - ACS Publications
Neuropathic pain is an important medical problem with few effective treatments. The sigma 1
receptor (σ1R) is known to be a potential target for neuropathic pain therapeutics, and …

Sigma-1 receptors control neuropathic pain and macrophage infiltration into the dorsal root ganglion after peripheral nerve injury

I Bravo Caparrós, MC Ruiz Cantero, G Perazzoli… - 2020 - digibug.ugr.es
Neuron-immune interaction in the dorsal root ganglia (DRG) plays a pivotal role in the
neuropathic pain development after nerve injury. Sigma-1 receptor (Sig-1R) is expressed by …

Discovery of a Highly Selective Sigma-2 Receptor Ligand, 1-(4-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-3-methyl-1H-benzo[d]imidazol-2(3H)-one …

S Intagliata, A Sharma, TI King, C Mesangeau… - The AAPS Journal, 2020 - Springer
The sigma-2 receptor has been cloned and identified as Tmem97, which is a
transmembrane protein involved in intracellular Ca 2+ regulation and cholesterol …