Sigma receptors and neurological disorders
By Agnieszka Piechal, Alicja Jakimiuk, and Dagmara Mirowska-Guzel Excerpt from the article published in Pharmacological Reports 73, 1582–1594 (2021). Published: 05 August 2021. DOI: https://doi.org/10.1007/s43440-021-00310-7 Editor’s Highlights Sigma receptors are an insufficiently understood group of receptors. S1R is unlike any traditional receptor. Intracellularly, it acts as chaperones, facilitating the correct folding of other proteins, regulating inositol-3-phosphate […]
Continue ReadingThe role of sigma 1 receptor in organization of endoplasmic reticulum signaling microdomains
By Vladimir Zhemkov, Jonathon A Ditlev, Wan-Ru Lee, Mikaela Wilson, Jen Liou, Michael K Rosen, Ilya Bezprozvanny Excerpt from the article published in eLife 2021;10:e65192 DOI: 10.7554/eLife.65192 Editor’s Highlights Sigma-1 receptor (S1R) modulates many physiological processes, such as cell excitability, transcriptional activity, Ca2+ homeostasis, stress response, and autophagy. Many biological functions of the Sigma-1 receptor can be explained […]
Continue ReadingCrystal structures of the σ2 receptor template large-library docking for selective chemotypes active in vivo
By Assaf Alon, Jiankun Lyu, Joao M. Braz, Tia A. Tummino, Veronica Craik, Matthew J.O’Meara, Chase M. Webb, Dmytro S. Radchenko, Yurii S. Moroz, Xi-Ping Huang, Yongfeng Liu, Bryan L. Roth, John J. Irwin, Allan I. Basbaum, Brian K. Shoichet, and Andrew C. Kruse Excerpt from the article published in bioRxiv 2021.04.29.441652; April 30, 2021; DOI: https://doi.org/10.1101/2021.04.29.441652 Editor’s Highlights Abstract The σ2 receptor is a poorly understood transmembrane receptor that has attracted intense interest in many areas of biology including cancer imaging, Alzheimer’s disease, schizophrenia, and neuropathic pain. However, […]
Continue ReadingNegative Impact of Sigma-1 Receptor Agonist Treatment on Tissue Integrity and Motor Function Following Spinal Cord Injury
By Alise Lattard, Gaëtan Poulen, Sylvain Bartolami, Yannick N. Gerber, and Florence E. Perrin Excerpt from the article published in Frontiers in Pharmacology, 10 February 2021Sec. Neuropharmacology, Volume 12 – 2021, DOI: https://doi.org/10.3389/fphar.2021.614949 Editors Highlights Abstract In traumatic spinal cord injury, the initial trauma is followed by a cascade of impairments, including excitotoxicity and calcium […]
Continue ReadingDistinct Regulation of σ1 Receptor Multimerization by Its Agonists and Antagonists in Transfected Cells and Rat Liver Membranes
By Weimin Conrad Hong Excerpt from the article published in Journal of Pharmacology and Experimental Therapeutics, May 2020, 373 (2) 290-301; DOI: https://doi.org/10.1124/jpet.119.262790 Editor’s Highlights The sigma-1 receptor (σ1R) interacts with and modulates the activity of a plethora of partner proteins, including channels, receptors, and transporters, and regulates their function. Changes in σ1R oligomerization by ligands can modulate the availability of σ1R […]
Continue ReadingThe Sigma-1 Receptor in Cellular Stress Signaling
By Teruo Hayashi Excerpt from the article published in Frontiers in Neuroscience, 16 July 2019 | https://doi.org/10.3389/fnins.2019.00733 Editor’s Highlights The sigma-1 receptor (Sig-1R)’s structure, is an integral endoplasmic reticulum (ER) membrane protein which shares no homology with any other mammalian protein. Sig-1R is enriched in a specialized ER subdomain which physically contacts the mitochondria, called the […]
Continue ReadingMolecular Interplay Between the Sigma-1 Receptor, Steroids, and Ion Channels
By Sara L. Morales-Lázaro, Ricardo González-Ramírez, and Tamara Rosenbaum Excerpt from the article published in Frontiers in Pharmacology, 10.,24 April 2019Sec. Experimental Pharmacology and Drug Discovery, DOI: https://doi.org/10.3389/fphar.2019.00419 Editor’s Highlights Abstract Cell excitability is tightly regulated by the activity of ion channels that allow for the passage of ions across cell membranes. Ion channel activity is […]
Continue ReadingSIGMAR1/Sigma-1 receptor ablation impairs autophagosome clearance
By Huan Yang, Hongtao Shen, Jing Li, and Lian-Wang Guo Excerpt from the article published in Autophagy, 15:9, 1539-1557, Published online: 14 Mar 2019 DOI: 10.1080/15548627.2019.1586248 Editor’s Highlights Autophagy lysosome-mediated pathway (ALP) degrades and recycles cellular wastes including proteins, lipids, and dysfunctional organelles, and is a key element of the Proteostasis Network. SIGMAR1 is a putative chaperone protein primarily […]
Continue ReadingSmall-Molecule Sigma1 Modulator Induces Autophagic Degradation of PD-L1
By Christina M. Maher; Jeffrey D. Thomas; Derick A. Haas; Charles G. Longen; Halley M. Oyer; Jane Y. Tong; and Felix J. Kim Excerpt from the article published in Molecular Cancer Research, Volume 16, Issue 2; 1 February 2018; 243–255; DOI: https://doi.org/10.1158/1541-7786.MCR-17-0166 Editor’s Highlights Abstract Emerging evidence suggests that Sigma1 (SIGMAR1, also known as sigma-1 […]
Continue Reading