摘要
Sigma-2受体在促进肿瘤细胞凋亡、增强抗肿瘤药物疗效、阻断Aβ寡聚体控制的信号转导、调节Ca2+稳态和保护神经细胞等方面起着关键作用。 研究表明sigma-2受体可能与ROS、LDL、mTOR、RAS、PLC/PKC、溶酶体自噬和线粒体超氧化应激密切相关。 此外,该受体在增殖细胞和神经细胞中的高表达表明 sigma-2 受体是癌症、阿尔茨海默病、精神分裂症和创伤性脑损伤的成像和治疗开发的理想分子靶标。 各种 sigma-2 激动剂已显示出有希望的抗癌活性,而 sigma-2 拮抗剂已显示出神经保护作用和对阿尔茨海默病患者大脑中 Aβ 寡聚体的抑制作用。 因此,sigma-2 激动剂和拮抗剂都是治疗癌症和神经退行性疾病的潜在有用疗法。
关键词: Sigma-2 受体、药物靶点、Aβ 蛋白、生物标志物、抗癌、阿尔茨海默病。
Current Medicinal Chemistry
Title:Sigma-2 Receptor as a Potential Drug Target
Volume: 28 Issue: 21
关键词: Sigma-2 受体、药物靶点、Aβ 蛋白、生物标志物、抗癌、阿尔茨海默病。
摘要: 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:
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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