Abstract
Sigma-2 receptor plays key roles in promoting tumor cell apoptosis, enhancing efficacy of anti-tumor drugs, blocking signal transduction controlled by Aβ oligomers, regulating Ca2+ homeostasis and protecting nerve cells. Studies indicated that sigma-2 receptor may be closely coupled with ROS, LDL, mTOR, RAS, PLC/PKC, lysosomal autophagy and mitochondrial super oxidative stress. In addition, the high expression of this receptor in proliferating cells and nerve cells indicates that sigma-2 receptor is an ideal molecular target for imaging and therapeutic development for cancer, Alzheimer's disease, schizophrenia and traumatic brain injury. Various sigma-2 agonists have shown promising anticancer activities, while sigma-2 antagonists have displayed neuroprotection and inhibition of Aβ oligomers in the brain of Alzheimer's disease patients. Thus, both sigma-2 agonists and antagonists are potentially useful therapeutics for the management of cancer and neurodegenerative disorders.
Keywords: Sigma-2 receptor, drug target, Aβ protein, biomarker, anticancer, Alzheimer's disease.
Current Medicinal Chemistry
Title:Sigma-2 Receptor as a Potential Drug Target
Volume: 28 Issue: 21
Author(s): Ai-Fang Chen, Wen-Hui Ma, Xiao-Yang Xie and Yun-Sheng Huang*
Affiliation:
- School of Pharmacy, Guangdong Medical University, 1 Xincheng Ave, Songshan Lake Technology Park, Dongguan, Guangdong 523808,China
Keywords: Sigma-2 receptor, drug target, Aβ protein, biomarker, anticancer, Alzheimer's disease.
Abstract: Sigma-2 receptor plays key roles in promoting tumor cell apoptosis, enhancing efficacy of anti-tumor drugs, blocking signal transduction controlled by Aβ oligomers, regulating Ca2+ homeostasis and protecting nerve cells. Studies indicated that sigma-2 receptor may be closely coupled with ROS, LDL, mTOR, RAS, PLC/PKC, lysosomal autophagy and mitochondrial super oxidative stress. In addition, the high expression of this receptor in proliferating cells and nerve cells indicates that sigma-2 receptor is an ideal molecular target for imaging and therapeutic development for cancer, Alzheimer's disease, schizophrenia and traumatic brain injury. Various sigma-2 agonists have shown promising anticancer activities, while sigma-2 antagonists have displayed neuroprotection and inhibition of Aβ oligomers in the brain of Alzheimer's disease patients. Thus, both sigma-2 agonists and antagonists are potentially useful therapeutics for the management of cancer and neurodegenerative disorders.
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Cite this article as:
Chen Ai-Fang , Ma Wen-Hui , Xie Xiao-Yang and Huang Yun-Sheng *, Sigma-2 Receptor as a Potential Drug Target, Current Medicinal Chemistry 2021; 28 (21) . https://dx.doi.org/10.2174/0929867327666200902172615
DOI https://dx.doi.org/10.2174/0929867327666200902172615 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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