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Review Article

CRAC通道作为自身免疫性疾病药物靶点的结构和机理研究

卷 21, 期 1, 2020

页: [55 - 75] 页: 21

弟呕挨: 10.2174/1389450120666190926150258

价格: $65

摘要

背景：钙（Ca2 +）离子是一种主要的细胞内信号传递信使，控制着各种细胞功能，例如基因表达，分泌，细胞生长，增殖和凋亡。控制这种Ca2 +稳态的主要机制是存储操作的Ca2 +释放激活的Ca2 +（CRAC）通道。 CRAC通道是主要由两种蛋白（基质相互作用分子（STIM）和ORAI）构成的完整膜蛋白。在内质网（ER）存储中的Ca2 +耗尽之后，STIM1与ORAI1相互作用并导致CRAC通道门打开，因此允许Ca2 +离子流入。大量研究报告称，由于ORAI1和STIM1的功能丧失或获得功能突变而导致的异常CRAC通道活性干扰了Ca2 +稳态，并导致了几种自身免疫性疾病。因此，它清楚地表明，CRAC通道的治疗靶标为治疗自身免疫性疾病的新方法提供了空间。 目的：这篇综述旨在提供参与CRAC通道调控的STIM1，ORAI1和其他分子调节剂的关键结构和力学见解。 结果与结论：了解蛋白质的结构和功能是通过限制其潜在副作用来改善有效靶标特异性的最重要步骤。本文中，综述主要集中于CRAC通道门控机制的结构基础及其生物物理特性，这将为协助开发针对自身免疫性疾病的新型靶向药物提供坚实的基础。最后，简要总结了由于CRAC通道突变引起的免疫缺陷和目前使用的具有其局限性的药理阻断剂。

关键词: 自身免疫性疾病，钙，SOCE，CRAC通道，ORAI，STIM。

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图形摘要

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