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Review Article

可溶性鸟苷酸环化酶的治疗靶向

卷 26, 期 15, 2019

页: [2730 - 2747] 页: 18

弟呕挨: 10.2174/0929867326666190108095851

价格: $65

摘要

可溶性鸟苷酸环化酶（sGC）是一氧化氮的生理传感器，其功能的改变主动涉及多种病理生理条件。过去20年来的大量研究工作提供了有关其监管的重要信息，最终合理开发了经批准的药物或研究性铅分子，这些分子通过新机制靶向并与sGC相互作用。但是，有许多问题仍然没有答案。正在进行的研究，结构化学研究的关键帮助，试图进一步阐明酶的结构特征，分别定义血红素部分存在或不存在时sGC的“刺激物”或“激活剂”的关联，以及精确的构象属性，将允许设计更具创新性和有效的药物。该综述涉及在理解该酶的功能方面取得的进展，特别是在过去10年中所取得的进展，并着重于a）其在疾病情况下的治疗靶向的基本原理和结果，取决于酶的状态（氧化与否，血红蛋白携带与否）和b）最近的结构研究，应该允许改进设计未来的治疗分子，旨在直接上调sGC的活动。

关键词: 6可溶性鸟苷酸环化酶（sGC），环磷酸鸟苷（cGMP），一氧化氮（NO），sGC激活剂，sGC刺激剂，H-NOX结构域，血红素，Fe。

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