Cytotoxic sigma-2 ligands trigger cancer cell death via cholesterol-induced-ER-stress
By Rony Takchi, Bethany C. Prudner, Qingqing Gong, Takaomi Hagi, Kenneth F. Newcomer, Linda X. Jin, Suwanna Vangveravong, Brian A. Van Tine, William G. Hawkins, and Dirk Spitzer Excerpt from the article published in Cell Death & Disease volume 15, Article number: 309, 02 May 2024, DOI: https://doi.org/10.1038/s41419-024-06693-8 Abstract Sigma-2-ligands (S2L) are characterized by high […]
Continue ReadingTransmembrane protein 97 is a potential synaptic amyloid beta receptor in human Alzheimer’s disease
By Martí Colom-Cadena, Jamie Toombs, Elizabeth Simzer, Kristjan Holt, Robert McGeachan, Jane Tulloch, Rosemary J. Jackson, James H. Catterson, Maxwell P. Spires-Jones, Jamie Rose, Lora Waybright, Anthony O. Caggiano, Declan King, Francesco Gobbo, Caitlin Davies, Monique Hooley, Sophie Dunnett, Robert Tempelaar, Soraya Meftah, Makis Tzioras, Mary E. Hamby, Nicholas J. Izzo, Susan M. Catalano, Claire […]
Continue ReadingHighly specific σ2R/TMEM97 ligand FEM-1689 alleviates neuropathic pain and inhibits the integrated stress response
By Muhammad Saad Yousuf, James J. Sahn, Hongfen Yang, Eric T. David, Stephanie Shiers, Marisol Mancilla Moreno, Jonathan Iketem, Danielle M. Royer, Chelsea D. Garcia, Jennifer Zhang, Veronica M. Hong, Subhaan M. Mian, Ayesha Ahmad, Benedict J. Kolber, Daniel J. Liebl, Stephen F. Martin, and Theodore J. Price Excerpt from the article published in Proceedings […]
Continue ReadingTMEM97/Sigma 2 Receptor Increases Estrogen Receptor α Activity in Promoting Breast Cancer Cell Growth
By Yuanqin Zhang, Xiangwei Fang, Jiuhui Wang and Daotai Nie Excerpt from the article published in Cancers 2023, 15(23): 5691. 2 December 2023. DOI: https://doi.org/10.3390/cancers15235691 Editor’s Highlitghts Simple Summary Selective estrogen receptor modulators are a major treatment modality for estrogen receptor-positive breast cancers, but the emergence of resistance or a lack of initial responsiveness is a […]
Continue ReadingSigma Receptor Ligands Prevent COVID Mortality In Vivo: Implications for Future Therapeutics
By Reed L. Berkowitz, Andrew P. Bluhm, Glenn W. Knox, Christopher R. McCurdy, David A. Ostrov, and Michael H. Norris Excerpt from the article published in International Journal of Molecular Sciences. 29 October 2023; 24(21):15718. DOI: https://doi.org/10.3390/ijms242115718 Editor’s Highlights Abstract The emergence of lethal coronaviruses follows a periodic pattern which suggests a recurring cycle of […]
Continue ReadingSigma Receptors: Novel Regulators of Iron/Heme Homeostasis and Ferroptosis
By Nhi T. Nguyen, Valeria Jaramillo-Martinez, Marilyn Mathew, Varshini V. Suresh, Sathish Sivaprakasam, Yangzom D. Bhutia, and Vadivel Ganapathy Excerpt from the article published in International Journal of Molecular Sciences. 28 September 2023; 24(19):14672. DOI: https://doi.org/10.3390/ijms241914672 Editor’s Higlights Abstract Sigma receptors are non-opiate/non-phencyclidine receptors that bind progesterone and/or heme and also several unrelated xenobiotics/chemicals. They […]
Continue ReadingBS148 Reduces the Aggressiveness of Metastatic Melanoma via Sigma-2 Receptor Targeting
By Claudia Sorbi, Silvia Belluti, Claudio Giacinto Atene, Federica Marocchi, Pasquale Linciano, Neena Roy, Elia Paradiso, Livio Casarini, Simone Ronsisvalle, Tommaso Zanocco-Marani, Livio Brasili, Luisa Lanfrancone, Carol Imbriano, Giulia Di Rocco, and Silvia Franchini Excerpt from the article published in the International Journal of Molecular Sciences. 2 June 2023; 24(11):9684. DOI: https://doi.org/10.3390/ijms24119684 Editor’s Highlights Abstract […]
Continue ReadingValidation of σ2R/TMEM97 as a neuropathic pain target: Specificity, human expression and mechanism of action
By Muhammad Saad Yousuf, James J. Sahn, Eric T. David, Stephanie Shiers, Danielle M. Royer, Chelsea D. Garcia, Jennifer Zhang, Veronica M. Hong, Ayesha Ahmad, Benedict J. Kolber, Daniel J Liebl, Stephen F. Martin, and Theodore J. Price Excerpt from the article published in bioRxiv 2023.04.11., 536439; DOI: https://doi.org/10.1101/2023.04.11.536439 Editor’s Highlights Abstract The Sigma 2 receptor (σ2R) […]
Continue ReadingSigma-2 Receptor Ligand Binding Modulates Association between TSPO and TMEM97
By Bashar M. Thejer, Vittoria Infantino, Anna Santarsiero, Ilaria Pappalardo, Francesca S. Abatematteo, Sarah Teakel, Ashleigh Van Oosterum, Robert H. Mach, Nunzio Denora, Byung Chul Lee, Nicoletta Resta, Rosanna Bagnulo, Mauro Niso, Marialessandra Contino, Bianca Montsch, Petra Heffeter, Carmen Abate, and Michael A. Cahill Excerpt from the article published in the International Journal of Molecular […]
Continue ReadingSigma-2 Receptors—From Basic Biology to Therapeutic Target: A Focus on Age-Related Degenerative Diseases
By Britney N. Lizama, Jennifer Kahle, Susan M. Catalano, Anthony O. Caggiano, Michael Grundman, and Mary E. Hamby Excerpt from the article published in the International Journal of Molecular Sciences. 24(7):6251. 26 March 2023. DOI: https://doi.org/10.3390/ijms24076251 Editor’s Highlights Abstract There is a large unmet medical need to develop disease-modifying treatment options for individuals with age-related […]
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