Category Archives: Cancer

Lipocalin-2 Regulates Epidermal Growth Factor Receptor Intracellular Trafficking

Lipocalin-2 Regulates Epidermal Growth Factor Receptor Intracellular Trafficking

By Lucie Yammine, Aniela Zablocki, William Baron, Fabiola Terzi, and Morgan Gallazzini Excerpt from the article published in Cell Reports, volume 29, issue 7, P2067-2077.E6, November 12, 2019, DOI: https://doi.org/10.1016/j.celrep.2019.10.015 Editor’s Highlights Lcn2, also known as neutrophil gelatinase-associated lipocalin (NGAL), siderocalin, or uterocalin, is a 25-kDa secreted glycoprotein that belongs to the lipocalin superfamily and has been […]

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Small-Molecule Modulators of Sigma1 and Sigma2/TMEM97 in the Context of Cancer: Foundational Concepts and Emerging Themes

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 […]

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Sigma‐1 receptor protects against ferroptosis in hepatocellular carcinoma cells

Sigma‐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. […]

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Sigma-2 receptor/TMEM97 agonist PB221 as an alternative drug for brain tumor

Sigma-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 […]

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Sigma-2 Receptor/TMEM97 and PGRMC-1 Increase the Rate of Internalization of LDL by LDL Receptor through the Formation of a Ternary Complex

Sigma-2 Receptor/TMEM97 and PGRMC-1 Increase the Rate of Internalization of LDL by LDL Receptor through the Formation of a Ternary Complex

By Aladdin Riad, Chenbo Zeng, Chi-Chang Weng, Harrison Winters, Kuiying Xu, Mehran Makvandi, Tyler Metz, Sean Carlin, and Robert H. Mach Excerpt from the article published in Scientific Reports 8, 16845, 15 November 2018, DOI: https://doi.org/10.1038/s41598-018-35430-3 Editor’s Highlights The disruption of lipoprotein trafficking may also be responsible for the mechanism of action of sigma-2 receptors (TMEM97/σ2R) […]

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Small-Molecule Sigma1 Modulator Induces Autophagic Degradation of PD-L1

Small-Molecule Sigma1 Modulator Induces Autophagic Degradation of PD-L1

By Christina M. Maher; Jeffrey D. Thomas; Derick A. Haas; Charles G. Longen; Halley M. Oyer; Jane Y. Tong; and Felix J. Kim Excerpt from the article published in Molecular Cancer Research, Volume 16, Issue 2; 1 February 2018; 243–255; DOI: https://doi.org/10.1158/1541-7786.MCR-17-0166 Editor’s Highlights Abstract Emerging evidence suggests that Sigma1 (SIGMAR1, also known as sigma-1 […]

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Sigma 1 receptor regulates ERK activation and promotes survival of optic nerve head astrocytes

Sigma 1 receptor regulates ERK activation and promotes survival of optic nerve head astrocytes

By Jing Zhao, Barbara A. Mysona, Jing Wang, Graydon B. Gonsalvez, Sylvia B. Smith, and Kathryn E. Bollinger Excerpt from the article published in PLOS ONE,  September 12, 2017, DOI: https://doi.org/10.1371/journal.pone.0184421 Editor’s Highlights Neuronal and glial cell types throughout the retina and optic nerve contain sigma 1 receptor (S1R), and its agonists display robust neuroprotective […]

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Sigma1 Targeting to Suppress Aberrant Androgen Receptor Signaling in Prostate Cancer

Sigma1 Targeting to Suppress Aberrant Androgen Receptor Signaling in Prostate Cancer

By Jeffrey D. Thomas; Charles G. Longen; Halley M. Oyer; Nan Chen; Christina M. Maher; Joseph M. Salvino; Blase Kania; Kelsey N. Anderson; William F. Ostrander; Karen E. Knudsen; and Felix J. Kim Excerpt from the article published in Cancer Res (2017) 77 (9): 2439–2452. DOI: https://doi.org/10.1158/0008-5472.CAN-16-1055 Editor’s Highlights Androgen receptor (AR) is the primary driver […]

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Sigma-2 receptor agonist derivatives of 1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) induce cell death via mitochondrial superoxide production and caspase activation in pancreatic cancer

Sigma-2 receptor agonist derivatives of 1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) induce cell death via mitochondrial superoxide production and caspase activation in pancreatic cancer

By Maria Laura Pati, John R. Hornick, Mauro Niso, Francesco Berardi, Dirk Spitzer, Carmen Abate, and William Hawkins Excerpt of the article published in BMC Cancer 17, 51 (2017). https://doi.org/10.1186/s12885-016-3040-4 Editor’s Highlights Pancreatic cancer is the fourth leading cause of cancer-related mortalities with an overall five-year survival rate of only 7%. Sigma receptors subtypes, namely sigma-1 and […]

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