尼古丁乙酰胆碱受体亚型的表达、功能和药理学:α-酰蛋白毒素的治疗潜力。
Nicotinic acetylcholine receptor subtype expression, function, and pharmacology: Therapeutic potential of α-conotoxins.
发表日期:2023 Mar 29
作者:
Han-Shen Tae, David J Adams
来源:
PHARMACOLOGICAL RESEARCH
摘要:
翻译:五聚体尼古丁乙酰胆碱受体(nAChRs)通常被分类为肌肉型或神经型,但后者也已在非神经细胞中报道。鉴于它们广泛的分布,nAChRs介导许多生理和病理过程,包括突触传递、递质释放的前突触调节、神经病性疼痛、炎症和癌症。共有17种不同的nAChR亚基,这些亚基的组合产生具有不同药理特性的亚型。利用敲除模型已广泛破译了一些nAChR亚型的表达和作用。异种系统中表达的许多nAChR亚型被二硫键富集的α-鼻涕螺毒素选择性靶向。α-鼻涕螺毒素是从鼻涕螺毒液中分离出的小肽,其中许多具有潜在的药物价值。Copyright © 2023. Published by Elsevier Ltd.
The pentameric nicotinic acetylcholine receptors (nAChRs) are typically classed as muscle- or neuronal-type, however, the latter has also been reported in non-neuronal cells. Given their broad distribution, nAChRs mediate numerous physiological and pathological processes including synaptic transmission, presynaptic modulation of transmitter release, neuropathic pain, inflammation, and cancer. There are 17 different nAChR subunits and combinations of these subunits produce subtypes with diverse pharmacological properties. The expression and role of some nAChR subtypes have been extensively deciphered with the aid of knock-out models. Many nAChR subtypes expressed in heterologous systems are selectively targeted by the disulfide-rich α-conotoxins. α-Conotoxins are small peptides isolated from the venom of cone snails, and a number of them have potential pharmaceutical value.Copyright © 2023. Published by Elsevier Ltd.