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TRPM2: a candidate therapeutic target for treating neurological diseases.
Acta Pharmacologica Sinica ( IF 8.2 ) Pub Date : 2018-May-01 , DOI: 10.1038/aps.2018.31
Jillian Corinne Belrose , Michael Frederick Jackson

Transient receptor potential melastatin 2 (TRPM2) is a calcium (Ca2+)-permeable non-selective cation channel belonging to the TRP ion channel family. Oxidative stress-induced TRPM2 activation provokes aberrant intracellular Ca2+ accumulation and cell death in a variety of cell types, including neurons. Aberrant TRPM2 function has been implicated in several neurological disorders including ischemia/stroke, Alzheimer's disease, neuropathic pain, Parkinson's disease and bipolar disorder. In addition to research identifying a role for TRPM2 in disease, progress has been made in the identification of physiological functions of TRPM2 in the brain, including recent evidence that TRPM2 is necessary for the induction of N-methyl-D-aspartate (NMDA) receptor-dependent long-term depression, an important form of synaptic plasticity at glutamate synapses. Here, we summarize recent evidence on the role of TRPM2 in the central nervous system (CNS) in health and disease and discuss the potential therapeutic implications of targeting TRPM2. Collectively, these studies suggest that TRPM2 represents a prospective novel therapeutic target for neurological disorders.

中文翻译:

TRPM2:用于治疗神经系统疾病的候选治疗靶标。

瞬态受体电位褪黑素2(TRPM2)是可渗透钙(Ca 2+)的非选择性阳离子通道,属于TRP离子通道家族。氧化应激诱导的TRPM2激活引起异常的细胞内Ca 2+多种细胞类型(包括神经元)中的聚集和细胞死亡。TRPM2异常功能与多种神经系统疾病有关,包括缺血/中风,阿尔茨海默氏病,神经性疼痛,帕金森氏病和躁郁症。除了确定TRPM2在疾病中的作用的研究之外,在鉴定TRPM2在脑中的生理功能方面也取得了进展,包括最近的证据表明TRPM2对于诱导N-甲基-D-天冬氨酸(NMDA)受体是必需的。依赖的长期抑郁症,这是谷氨酸突触中突触可塑性的一种重要形式。在这里,我们总结了有关TRPM2在健康和疾病中的中枢神经系统(CNS)中的作用的最新证据,并讨论了靶向TRPM2的潜在治疗意义。总的来说,
更新日期:2018-04-19
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