Small-Molecule Modulators of Sigma1 and Sigma2/TMEM97 in the Context of Cancer: Foundational Concepts and Emerging Themes
By Halley M. Oyer, Christina M. Sanders, and Felix J. Kim Excerpt from the article published in Frontiers in Pharmacology, volume 10, 21 October 2019 | https://doi.org/10.3389/fphar.2019.01141 Editor’s Highlights Over the past two decades, a number of publications have suggested a potential role for Sigma1 and Sigma2/TMEM97 in tumor biology. Sigma1 RNAi knockdown and some small-molecule […]
Continue ReadingSigma‐1 receptor protects against ferroptosis in hepatocellular carcinoma cells
By Tao Bai, Pengxu Lei, Hao Zhou, Ruopeng Liang, Rongtao Zhu, Weijie Wang, Lin Zhou, and Yuling Sun Excerpt from the article published in Journal of Cellular and Molecular Medicine 2019 Nov; 23(11): 7349–7359. DOI: 10.1111/jcmm.14594 Editor’s Highlights Hepatocellular carcinoma (HCC) is a common type of cancer that is ranked sixth in prevalence and third in mortality worldwide. […]
Continue ReadingNeuronal Sigma-1 Receptors: Signaling Functions and Protective Roles in Neurodegenerative Diseases
by Daniel A. Ryskamp, Svetlana Korba, Vladimir Zhemkov, Nina Kraskovskaya, and Ilya Bezprozvanny Excerpt from the article published in Front. Neurosci., 28 August 2019 | https://doi.org/10.3389/fnins.2019.00862 Editor’s Highlights Abstract Sigma-1 receptor (S1R) is a multi-functional, ligand-operated protein situated in endoplasmic reticulum (ER) membranes and changes in its function and/or expression have been associated with various neurological disorders including amyotrophic lateral sclerosis/frontotemporal dementia, […]
Continue ReadingSigma-1 receptor modulates neuroinflammation associated with mechanical hypersensitivity and opioid tolerance in a mouse model of osteoarthritis pain
By Mireia Carcolé, Sami Kummer, Leonor Gonçalves, Daniel Zamanillo, Manuel Merlos, Anthony H. Dickenson, Begoña Fernández-Pastor, David Cabañero, and Rafael Maldonado Excerpt from the article published in British Journal of Pharmacology, 23 July 2019; 176: 3939– 3955. DOI: https://doi.org/10.1111/bph.14794 Abstract Background and Purpose: Osteoarthritic pain is a chronic disabling condition lacking effective treatment. Continuous use of opioid drugs during […]
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 ReadingSigma-2 receptor as a potential therapeutic target for treating central nervous system disorders
by Terada K, Migita K, Matsushima Y, Kamei C. Excerpt from the article published in Neural Regen Res 2019;14:1893-4 DOI: 10.4103/1673-5374.259609 The sigma receptor (Sig-R) was first reported by Martin et al. (1976) and was initially classified into the opioid receptor family. However, Sig-R was subsequently found to differ from the opioid receptor in various studies […]
Continue ReadingLigands Exert Biased Activity to Regulate Sigma 1 Receptor Interactions With Cationic TRPA1, TRPV1, and TRPM8 Channels
By Elsa Cortés-Montero, Pilar Sánchez-Blázquez, Yara Onetti, Manuel Merlos and Javier Garzón Excerpt from the article published in Frontiers in Pharmacology, 2019 volume 10 DOI=10.3389/fphar.2019.00634 Editor’s Highlights The sigma 1 receptor (σ1R) and the mu-opioid receptor (MOR) regulate the transient receptor potential (TRP) V1 calcium channel. TRP ankyrin member 1 (TRPA1) receptors are coexpressed with TRPV1 […]
Continue ReadingSigma-2 receptor/TMEM97 agonist PB221 as an alternative drug for brain tumor
By Chia-Chi Liu, Ching-Fang Yu, Shu-Chi Wang, Hsueh-Yin Li, Chiu-Min Lin, Hsia-Han Wang, Carmen Abate, and Chi-Shiun Chiang Excerpt from the article published in MC Cancer 19, 473 (2019). https://doi.org/10.1186/s12885-019-5700-7 Editor’s Highlights In adults, glioblastoma and astrocytoma are the most malignant and lethal forms of primary brain tumors. The antitumor activities of sigma-2 agonists are mediated mainly […]
Continue ReadingBlockade of the Sigma-1 Receptor Relieves Cognitive and Emotional Impairments Associated to Chronic Osteoarthritis Pain
By Mireia Carcolé, Daniel Zamanillo, Manuel Merlos, Begoña Fernández-Pastor, David Cabañero, and Rafael Maldonado Excerpt from the article published in Frontiers in Pharmacology, 03 May 2019Sec. Experimental Pharmacology and Drug Discovery DOI: https://doi.org/10.3389/fphar.2019.00468 Abstract Osteoarthritis is the most common musculoskeletal disease worldwide, often characterized by degradation of the articular cartilage, chronic joint pain and disability. Cognitive dysfunction, […]
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 […]
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