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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Review Article

Sigma-2 Receptor as a Potential Drug Target

Author(s): Ai-Fang Chen, Wen-Hui Ma, Xiao-Yang Xie and Yun-Sheng Huang*

Volume 28, Issue 21, 2021

Published on: 02 September, 2020

Page: [4172 - 4189] Pages: 18

DOI: 10.2174/0929867327666200902172615

Price: $65


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.

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