Results 11 to 20 of about 1,201,382 (297)

Activation of sigma-1 receptor chaperone in the treatment of neuropsychiatric diseases and its clinical implication

Journal of Pharmacological Sciences, 2015
Endoplasmic reticulum (ER) protein sigma-1 receptor represents unique chaperone activity in the central nervous system, and it exerts a potent influence on a number of neurotransmitter systems. Several lines of evidence suggest that activation of sigma-1
Kenji Hashimoto
doaj   +3 more sources

Sigma-1 receptor: The novel intracellular target of neuropsychotherapeutic drugs

Journal of Pharmacological Sciences, 2015
Sigma-1 receptor ligands have been long expected to serve as drugs for treatment of human diseases such as neurodegenerative disorders, depression, idiopathic pain, drug abuse, and cancer.
Teruo Hayashi
doaj   +3 more sources

Differences in the signaling pathways of α1A- and α1B-adrenoceptors are related to different endosomal targeting [PDF]

, 2013
Aims: To compare the constitutive and agonist-dependent endosomal trafficking of α1A- and α1B-adrenoceptors (ARs) and to establish if the internalization pattern determines the signaling pathways of each subtype.
A Hirasawa, AC Hanyaloglu, AL Lattion, B Lei, BL Wolfe, C Moyano, C Stenbergen, CD Wright, D Calebiro, D Chalothorn, D Diviani, D Gesty-Palmer, D Wu, DM Perez, DP Morris, DP Morris, E Oliver, EJ Adie, EJ Adie, Elena Carceller, F Liu, Fermí Montó, Graeme Milligan, Ian Christie McGrath, James Porter, JB Morris, JD Pediani, JD Pediani, JL Benovic, John Pediani, KA DeFea, L Stanasila, LM Luttrell, M von Zastrow, María Antonia Noguera, MC Lyssand JS De Fino, Miguel Pérez-Aso, MW Lee, MY Tsang, P Lajoie, PA Patel, Pilar D’Ocon, RH Oakley, RR Price, S Ahn, S Alexander, S Keffel, S Mhaouty-Kodja, S Terrillon, SK Shenoy, SM DeWire, SS Ferguson, TL Theroux, Vanessa Segura, Y Huang   +54 more
core   +18 more sources

Adamantane-derived scaffolds targeting the sigma-2 receptor; an in vitro and in silico study

Saudi Pharmaceutical Journal, 2021
Novel adamantane-based compounds were synthesized and assessed as potential sigma-2 receptor ligands. Molecular docking and 50 ns molecular dynamic simulation were carried out to determine the binding modes, mechanism of interaction, and stability of ...
Mohammed A. Alamri, Mubarak A. Alamri
doaj   +1 more source

Hazards of Using Masking Protocols When Performing Ligand Binding Assays: Lessons From the Sigma-1 and Sigma-2 Receptors

Frontiers in Pharmacology, 2020
Sigma-1 and sigma-2 receptors are emerging therapeutic targets. Although the molecular identity of the sigma-2 receptor has recently been determined, receptor quantitation has used, and continues to use, the sigma-1 selective agents (+) pentazocine or ...
Haider Abbas, Haider Abbas, Preeti Borde, Gary B. Willars, David R. Ferry, Stephen T. Safrany   +5 more
doaj   +1 more source

The Sigma Enigma: A Narrative Review of Sigma Receptors

Cureus, 2023
The sigma-1 and sigma-2 receptors were first discovered in the 1960s and were thought to be a form of opioid receptors initially. Over time, more was gradually learned about these receptors, which are actually protein chaperones, and many of their unique or unusual properties can contribute to a range of important new therapeutic applications.
Pergolizzi, Joseph, Varrassi, Giustino, Coleman, Mark, Breve, Frank, Christo, Dana K, Christo, Paul J, Moussa, Charbel   +6 more
openaire   +2 more sources

Sigma-2 Receptor—A Potential Target for Cancer/Alzheimer’s Disease Treatment via Its Regulation of Cholesterol Homeostasis

Molecules, 2020
The sigma receptors were classified into sigma-1 and sigma-2 receptor based on their different pharmacological profiles. In the past two decades, our understanding of the biological and pharmacological properties of the sigma-1 receptor is increasing ...
Kai Yang, Cheng Zeng, Changcai Wang, Meng Sun, Dan Yin, Taolei Sun   +5 more
doaj   +1 more source

Sigma 1 Receptor Co-Localizes with NRF2 in Retinal Photoreceptor Cells

Antioxidants, 2021
Sigma 1 receptor (Sig1R), a modulator of cell survival, has emerged as a novel target for retinal degenerative disease. Studies have shown that activation of Sig1R, using the high affinity ligand (+)-pentazocine ((+)-PTZ), improves cone function in a ...
Shannon R. Barwick, Mevish S. Siddiq, Jing Wang, Haiyan Xiao, Brendan Marshall, Elizabeth Perry, Sylvia B. Smith   +6 more
doaj   +1 more source

Sigma Receptor (σR) Ligands with Antiproliferative and Anticancer Activity. [PDF]

Molecules, 2017
Georgiadis MO, Karoutzou O, Foscolos AS, Papanastasiou I.   +3 more
europepmc   +2 more sources

TMEM97 and PGRMC1 do not mediate sigma-2 ligand-induced cell death [PDF]

, 2019
Sigma-2 receptors have been implicated in both tumor proliferation and neurodegenerative diseases. Recently the sigma-2 receptor was identified as transmembrane protein 97 (TMEM97).
Hawkins, William G., Jin, Linda, Mach, Robert H., Makvandi, Mehran, Puentes, Laura, Riad, Aladdin, Schneider, Mark E., Jr., Weng, Chi-Chang, Xu, Kuiying, Zeng, Chenbo   +9 more
core   +3 more sources