在 PNU 存在的情况下，MrIC 是一种新型的α-芋螺毒素激动剂，作用于内源性α7 烟碱型乙酰胆碱受体。
MrIC, a novel α-conotoxin agonist in the presence of PNU at endogenous α7 nicotinic acetylcholine receptors.
机构信息
Institute for Molecular Bioscience, The University of Queensland , Brisbane, QLD 4072, Australia , and Discipline of Pharmacology, The University of Sydney , Sydney, NSW 2006, Australia.
出版信息
Biochemistry. 2014 Jan 14;53(1):1-3. doi: 10.1021/bi400882s. Epub 2013 Dec 30.
α-Conotoxins are competitive antagonists of nicotinic acetylcholine receptors (nAChRs). Their high selectivity and affinity for the various subtypes of nAChRs have led to significant advances in our understanding of the structure and function of these key ion channels. Here we report the discovery of a novel 4/7 α-conotoxin, MrIC from the venom duct of Conus marmoreus, which acts as an agonist at the endogenous human α7 nAChR in SH-SY5Y cells pretreated with PNU120596 (PNU). This unique agonist activity of MrIC at α7 nAChRs may guide the development of novel α7 nAChR modulators.
α- 芋螺毒素是烟碱型乙酰胆碱受体 (nAChRs) 的竞争性拮抗剂。它们对各种亚型 nAChRs 的高选择性和亲和力，使得我们对这些关键离子通道的结构和功能有了更深入的了解。在这里，我们报道了一种新型的 4/7 α-芋螺毒素 MrIC 的发现，它来自 Conus marmoreus 的毒腺，在 PNU120596 (PNU) 预处理的 SH-SY5Y 细胞中作为内源性人 α7 nAChR 的激动剂发挥作用。MrIC 在 α7 nAChRs 上的这种独特激动剂活性可能指导新型 α7 nAChR 调节剂的开发。
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