Sigma-2 Receptor as a Potential Drug Target

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.

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