Sigma 2 Receptor - Advantx Pharmaceuticals Inc.

PGRMC1 acts as a size-selective cargo receptor to drive ER-phagic clearance of mutant prohormones

By Yu-Jie Chen, Jeffrey Knupp, Anoop Arunagiri, Leena Haataja, Peter Arvan, and Billy Tsai Excerpt from the article published in Nature Communications 12, 5991 (2021), 13 October 2021, DOI: https://doi.org/10.1038/s41467-021-26225-8 Editor’s Highlights Protein misfolding in the endoplasmic reticulum (ER) causes a myriad of human diseases, including neurodegenerative diseases, cancer, and diabetes. Amongst the most well characterized of […]

Multifunctional thiosemicarbazones targeting sigma receptors: in vitro and in vivo antitumor activities in pancreatic cancer models

By Mauro Niso, Joanna Kopecka, Francesca Serena Abatematteo, Francesco Berardi, Chiara Riganti, and Carmen Abate Excerpt from the article published in Cellular Oncology 44, 1307–1323 (2021). https://doi.org/10.1007/s13402-021-00638-5 Editor’s Highlights Pancreatic cancer is one of the most aggressive forms of cancer characterized by a poor prognosis and a five-year survival rate of ~ 8 %. Surgery represents the […]

Crystal 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, […]

The ER protein Ema19 [tmem97] facilitates the degradation of nonimported mitochondrial precursor proteins

By Janina Laborenz, Yury S. Bykov, Katharina Knöringer, Markus Räschle, Sabine Filker, Cristina Prescianotto-Baschong, Anne Spang, Takashi Tatsuta, Thomas Langer, Zuzana Storchová, Maya Schuldiner, and Johannes M. Herrmann Excerpt from the article published on Molecular Biology of the Cell, Volume 32, Issue 8, Published Online: 13 Apr 2021, DOI: https://doi.org/10.1091/mbc.E20-11-0748 Editor’s Highlights Ema19 is the […]

The Sigma-2 Receptor / Transmembrane protein 97 (σ2R/TMEM97) Modulator JVW-1034 Reduces Heavy Alcohol Drinking and Associated Pain States in Male Mice

By Sema G. Quadir, Sean M. Tanino, Christian D. Rohl, James J. Sahn, Emily J. Yao, Luíza dos Reis Cruz, Pietro Cottone, Stephen F. Martin, and Valentina Sabino Excerpt from the article published in Neuropharmacology, Volume 184, 108409, 15 February 2021. DOI: https://doi.org/10.1016/j.neuropharm.2020.108409. Author manuscript available at NCBI HHS public access: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7856185/ Editor’s Highlights Abstract Alcohol Use Disorder […]

TMEM97 increases in synapses and is a potential synaptic Aβ binding partner in human Alzheimer’s disease

By Martí Colom-Cadena, Jane Tulloch, Rosemary J Jackson, James H Catterson, Jamie Rose, Caitlin Davies, Monique Hooley, Alejandro Anton-Fernandez, Sophie Dunnett, Robert Tempelaar, Makis Tzioras, Nicholas J Izzo, Susan M. Catalano, Colin Smith, and Tara L. Spires-Jones Excerpt from the article published in bioRxiv 2021.02.01, 428238; DOI: https://doi.org/10.1101/2021.02.01.428238 Editor’s Highlights Abstract Synapse loss correlates with cognitive decline in […]

Sigma-2 receptor antagonists rescue neuronal dysfunction induced by Parkinson’s patient brain-derived α-synuclein

By Colleen S. Limegrover, Raymond Yurko, Nicholas J. Izzo, Kelsie M. LaBarbera, Courtney Rehak, Gary Look, Gilbert Rishton, Hank Safferstein, and Susan M. Catalano Excerpt from the article published in Journals of Neuroscience Research; 99: 1161– 1176, 22 January 2021, DOI: https://doi.org/10.1002/jnr.24782 Editor’s Highlights Oligomeric α-synuclein proteins found in Parkinson’s disease patient brain tissue cause neuron dysfunction. α-synuclein […]

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

By Kai Yang, Cheng Zeng, Changcai Wang, Meng Sun, Dan Yin, and Taolei Sun Excerpt from the article published in Molecules 25, no. 22: 5439, 2020 https://doi.org/10.3390/molecules25225439 Editor’s Highlights Recently transmembrane protein 97 (TMEM97) was identified as a sigma-2 receptor identity using mass spectrometry after affinity purification from the liver. TMEM97/sigma-2 receptor forms a trimeric complex […]

The Sigma 2 receptor promotes and the Sigma 1 receptor inhibits mu-opioid receptor-mediated antinociception

By Sánchez-Blázquez, P., Cortés-Montero, E., Rodríguez-Muñoz, M. et al. Excerpt from the article published in Mol Brain 13, 150 (2020). https://doi.org/10.1186/s13041-020-00676-4 Editor’s Highlights σ2R is essential for the antinociceptive effects of exogenous and endogenous ligands of MOR but not for the antinociceptive effects of other families of G-receptors that also mediate analgesia, such as DOR, CB1R and α2AR. […]

The Sigma-2 Receptor, PGRMC1, and LDL Receptor complex are responsible for the cellular uptake of Aβ42 and its protein aggregates

by Aladdin Riad, Zsofia Lengyel-Zhand, Chenbo Zeng, Chi-Chang Weng, Virginia M.-Y. Lee, John Q. Trojanowski, and Robert H. Mach Excerpt from the article published in final edited form as: Mol Neurobiol. 2020 September DOI: 10.1007/s12035-020-01988-1 Editor’s Highlights Sigma-2 receptor (TMEM97) and PGRMC1 are therapeutic targets for inhibiting neuronal uptake of Aβ42 and ApoE-associated Aβ42 and potentially […]

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