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解锁Cu (I) 介导的催化途径,通过将基于氧的丁替代物纳入Cu (II) -ATCUN复合体,从而有效生成ROS

Yen Jea Lee¹, Yujeong Kim², Haesol Kim³

¹Department of Chemistry, Gwangju Institute of Science and Technology, Gwangju 61005, Republic of Korea.

Inorganic chemistry

|June 21, 2023

概括

研究人员用 thiazole 和 oxazole 修改了铜结合基因 (ATCUN),以改善金属药物反应性氧物种 (ROS) 的产生. 这种设计增强了铜的性能.

科学领域:

协调化学协调化学
药用化学医学化学
生物物理化学生物物理化学

背景情况:

氨基终端铜和 (ATCUN) 基因结合Cu (II) 并表现出用于产生活性氧物种 (ROS) 的催化氧化还原活性.
在ATCUN图案中强大的Cu (II) 结合限制了Cu (I) 的可用性,阻碍了用于金属制药应用的高效ROS生产.
开发调节Cu (I) /Cu (II) 反氧循环的策略对于增强ROS介导生物分子氧化至关重要.

研究的目的:

设计新的ATCUN联体与修改的N-捐赠者部分,以提高Cu (I) 的可访问性和ROS生成.
研究用 thiazole 或 oxazole 取代 histidine imidazole 对 Cu(II) -ATCUN 复合物的催化活性的影响.
探索这些修饰图案在开发先进的ROS介导金属药物中的潜力.

主要方法:

合成Gly-Gly-His-NH2 (GGHa) 类似物,其中提亚 (GGThia) 和氧沙 (GGOxa) 取代了伊米达.
使用电子磁共振光谱学,X射线晶体学和X射线吸收光谱学对Cu (II) -ATCUN复合体进行表征.
通过ROS介导的DNA裂变试验,电化学测量和密度函数理论计算来评估催化活性.

主要成果:

对GGHa,GGThia和GGOxa复合体观察到类似的正方形平面Cu(II) -N4协调几何学.
与正规的GGHa动机相比,醇修饰显著提高了ROS介导的DNA裂变的速率.
分析显示,醇修饰通过调节N供体性质,提高了ROS生成期间Cu (I) 的可访问性.

结论:

在 ATCUN 基因中用 thiazole 或 oxazole 替换 histidine 提供了一种可行的策略,以增强 redox 循环和 ROS 生成.
开发的含醇/醇的ATCUN图案为具有可调节N捐赠能力的配体提供了一种新的设计方法.
这些发现为推进ROS介导金属药物和相关治疗策略具有重大潜力.

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