The sigma-1 receptor curtails endogenous opioid analgesia during sensitization of TRPV1 nociceptors
By M. Carmen Ruiz-Cantero, Elsa Cortés-Montero, Aakanksha Jain, Ángeles Montilla-García, Inmaculada Bravo-Caparrós, Jaehoon Shim, Pilar Sánchez-Blázquez, Clifford J. Woolf, José M. Baeyens, and Enrique J. Cobos Excerpt from the article published in British Journal of Pharmacology, 1– 20, 07 December 2022, DOI: https://doi.org/10.1111/bph.16003 Editor’s Highlights Abstract Background and Purpose: Peripheral sensitization contributes to pathological pain. While prostaglandin […]
Continue ReadingProtein Misfolding and Aggregation in the Brain: Common Pathogenetic Pathways in Neurodegenerative and Mental Disorders
By Aleksandra Ochneva, Yana Zorkina, Olga Abramova, Olga Pavlova, Valeriya Ushakova, Anna Morozova, Eugene Zubkov, Konstantin Pavlov, Olga Gurina, and Vladimir Chekhonin Excerpt from the article published in International Journal of Molecular Sciences 23, no. 22: 14498. 21 November 2022, DOI: https://doi.org/10.3390/ijms232214498 Editor’s Highlights Abstract Mental disorders represent common brain diseases characterized by substantial impairments of […]
Continue ReadingSigma-1 receptor agonist PRE-084 confers protection against TAR DNA-binding protein-43 toxicity through NRF2 signalling
By Christelle Lasbleiz, Amandine Peyrel, Pauline Tarot, Jérôme Sarniguet, Lucie Crouzier, Nicolas Cubedo, Benjamin Delprat, Mireille Rossel, Tangui Maurice, Jean-Charles Liévens Excerpt from the article published in Redox Biology, 17 November 2022, 102542, ISSN 2213-2317,DOI: https://doi.org/10.1016/j.redox.2022.102542. Editor’s Highlights Autors’ Highlights Abstract Amyotrophic lateral sclerosis (ALS) is a neurodegenerative disease affecting upper and lower motor neurons. […]
Continue ReadingThe regulatory role of endoplasmic reticulum chaperone proteins in neurodevelopment
By Hongji Sun, Mengxue Wu, Minxin Wang, Xiaomin Zhang, and Jia Zhu Excerpt from the article published in Frontiers of Neuroscience, 15 November 2022, Sec. Neurodevelopment, DOI: https://doi.org/10.3389/fnins.2022.1032607 Editor’s Highlights Abstract The endoplasmic reticulum (ER) is the largest tubular reticular organelle spanning the cell. As the main site of protein synthesis, Ca2+ homeostasis maintenance and lipid […]
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 ReadingBispecific sigma-1 receptor antagonism and mu-opioid receptor partial agonism: WLB-73502, an analgesic with improved efficacy and safety profile compared to strong opioids
By Alba Vidal-Torres, Begoña Fernández-Pastor, Mónica García, Eva Ayet, Anna Cabot, Javier Burgueño, Xavier Monroy, Bertrand Aubel, Xavier Codony, Luz Romero, Rosalía Pascual, Maria Teresa Serafini, Gregorio Encina, Carmen Almansa, Daniel Zamanillo, Manuel Merlos, and José Miguel Vela Excerpt from the article published in Acta Pharmaceutica Sinica B, September 25, 2022, ISSN 2211-3835, DOI: https://doi.org/10.1016/j.apsb.2022.09.018 […]
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 ReadingThe Adhesion GPCR VLGR1/ADGRV1 Regulates the Ca2+ Homeostasis at Mitochondria-Associated ER Membranes
By Jacek Krzysko, Filip Maciag, Anna Mertens, Baran Enes Güler, Joshua Linnert, Karsten Boldt, Marius Ueffing, Kerstin Nagel-Wolfrum, Martin Heine, and Uwe Wolfrum Excerpt from the article published in Cells. 2022; 11(18):2790. 7 September 2022. DOI: https://doi.org/10.3390/cells11182790 Editor’s Highlights The VLGR1 (very large G protein-coupled receptor-1), also known as ADGRV1, GPR98, and MASS, is the […]
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 […]
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