αN-Acetyl β-Endorphin Is an Endogenous Ligand of σ1Rs That Regulates Mu-Opioid Receptor Signaling by Exchanging G Proteins for σ2Rs in σ1R Oligomers
By Javier Garzón-Niño, Elsa Cortés-Montero, María Rodríguez-Muñoz, and Pilar Sánchez-Blázquez Excerpt from the article published in the International Journal of Molecular Sciences. 2023; 24(1):582, 29 December 2022, DOI: https://doi.org/10.3390/ijms24010582 Editor’s Highlights Abstract The opioid peptide β-endorphin coexists in the pituitary and brain in its αN-acetylated form, which does not bind to opioid receptors. We now report […]
Continue ReadingSigma Antagonists for Treatment of Neuropathic Pain Syndromes in Cancer Patients: A Narrative Review
By Joseph V. Pergolizzi, Jr. and Jo Ann LeQuang Article published in Journal of Cancer Research Updates, 11, 70–77, 2022-10-27, DOI: https://doi.org/10.30683/1929-2279.2022.11.10 Abstract Almost 40% of cancer patients have neuropathic pain or mixed pain with a neuropathic component, which can be intense, debilitating, and challenging to treat. New studies on sigma receptors show these enigmatic ligand-binding […]
Continue ReadingSafe and Efficient Sigma1 Ligand: A Potential Drug Candidate for Multiple Sclerosis
By Bénédicte Oxombre, Fahima Madouri, Anne-Sophie Journé, Séverine Ravez, Eloise Woitrain, Pascal Odou, Nathalie Duhal, Sandro Ninni, David Montaigne, Nadira Delhem, Patrick Vermersch, and Patricia Melnyk Excerpt from the article published in International Journal of Molecular Sciences 23, no. 19: 11893. 6 October 2022. DOI: https://doi.org/10.3390/ijms231911893 Editor’s Highlights In the last few decades, the sigma1 (S1R) […]
Continue ReadingSpecific detection and deletion of the sigma-1 receptor widely expressed in neurons and glial cells in vivo
By Qing Liu, Qilin Guo, Li-Pao Fang, Honghong Yao, Anja Scheller, Frank Kirchhoff, and Wenhui Huang Excerpt from the article published in Journal of Neurochemistry, 00, 1– 22, 09 September 2022, DOI: https://doi.org/10.1111/jnc.15693 Editor’s Highlights Abstract The chaperon protein sigma-1 receptor (S1R) has been discovered over 40 years ago. Recent pharmacological studies using S1R exogenous ligands demonstrated a promising […]
Continue ReadingDefining the Ligand-dependent Interactome of the Sigma 1 Receptor
By Jing Zhao, Rajalakshmi Veeranan-Karmegam, Frederick C. Baker, Barbara A. Mysona, Pritha Bagchi, Yutao Liu, Sylvia B. Smith, Graydon B. Gonsalvez, and Kathryn E. Bollinger Excerpt from the article published in bioRxiv 2022.06.22.497210; Published June 25, 2022, DOI: https://doi.org/10.1101/2022.06.22.497210 Editor’s Highlights The sigma 1 receptor (S1R) is a therapeutic target for a wide spectrum of pathological conditions. S1R has […]
Continue ReadingMitochondrial transfer/transplantation: an emerging therapeutic approach for multiple diseases
By Zonghan Liu, Yi Sun, Zhengtang Qi, Lu Cao, and Shuzhe Ding Excerpt from the article published in Cell and Bioscience 12, 66 (2022). Published: 19 May 2022, DOI: https://doi.org/10.1186/s13578-022-00805-7 Editor’s Highlights Mitochondria are semiautonomous, semiself-replicating, highly dynamic organelles, endowed with their own circular, double-stranded DNA molecule that spans 16.6 kb and intramitochondrial replication and translational machinery. Intercellular mitochondrial […]
Continue ReadingIntracellular dynamics of the Sigma-1 receptor observed with super-resolution imaging microscopy
By Sergei Kopanchuk, Edijs Vavers , Santa Veiksina, Kadri Ligi, Liga Zvejniece, Maija Dambrova, and Ago Rinken Excerpt from the article published in PLoS ONE 17(5): e0268563. May 18, 2022, DOI: https://doi.org/10.1371/journal.pone.0268563 Editor’s Highlights The sigma-1 receptor (Sig1R) has been described as an intracellular protein modulator, a chaperone protein that localizes in the endoplasmic reticulum […]
Continue ReadingAn open-like conformation of the sigma-1 receptor reveals its ligand entry pathway
By Meng, F., Xiao, Y., Ji, Y. et al. Excerpt from the article published in Nat Commun 13, 1267 (2022). https://doi.org/10.1038/s41467-022-28946-w Editor’s Highlights Data suggest that access to the σ1R ligand binding site is likely achieved by protein conformational changes that involve the carboxy-terminal two-helix bundle, rather than structural changes in the cupin-fold domain. The PATH2 access hypothesis […]
Continue ReadingNovel Therapeutic Target for Prevention of Neurodegenerative Diseases: Modulation of Neuroinflammation with Sig-1R Ligands
By Ferenc Bogár, Lívia Fül. and Botond Penke Excerpt from the article published in Biomolecules 2022, 12, 363, Published: 25 February 2022, DOI: https://doi.org/10.3390/biom12030363 Editor’s Highlights Sigma-1 Receptor is a Central Regulator of Cell Survival As Sig-1R controls ER stress and the inflammatory processes in the cells, Sig-1R agonists have been tested in preclinical studies and […]
Continue ReadingThe Sigma-1 receptor is an ER-localized type II membrane protein
By Neeraj Sharma, Chaitanya Patel, Marina Shenkman, Amit Kessel, Nir Ben-Tal, Gerardo Z. Lederkremer Excerpt from the article published in Journal of Biological Chemistry, 297, 5, 101299, November 2021 DOI: https://doi.org/10.1016/j.jbc.2021.101299 Editor’s Highlights The Sigma-1 receptor (S1R) is a small transmembrane protein (25 KDa), which is localized predominantly in the endoplasmic reticulum (ER), preferentially at the […]
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