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人类赫索金酶域含蛋白1的表征和抑制揭示了一种具有独特催化和调节特征的酶

Alexander T Piwko¹, Madeline A Jeffes¹, James H Frederich¹

¹Department of Chemistry and Biochemistry, Laboratories of Molecular Recognition, Florida State University, 95 Chieftan Way, Tallahassee, Florida 32306, United States.

ACS chemical biology

|November 4, 2025

概括

含有蛋白1 (HKDC1) 的赫索基纳酶域是一种强大的酶,具有独特的动力学,不受常见抑制剂的影响. 这项研究描述了HKDC1,揭示了其独特的特性和潜在的疾病相关性.

科学领域:

生物化学生物化学
分子生物学分子生物学
酶学是一种酶学.

背景情况:

含有蛋白质1 (HKDC1) 的六金酶域是一种新发现的人类六金酶单酶.
在各种癌症中,HKDC1的升高调节,但其功能特征仍然不太清楚.
以前的细胞研究表明HKDC1的酶活性较低.

研究的目的:

描述重组人类HKDC1.1的动力和调节性质.
调查HKDC1域在其酶活性中的作用.
探索HKDC1对各种抑制剂和疾病相关变异的敏感性.

主要方法:

重组人类HKDC1的表达和净化.
酶动力学测试以确定动力学参数 (kcat,Km).
分析由葡萄糖6酸盐,Dinaciclib和一种葡萄糖胺衍生物抑制酶的分析.
包括T58M在内的HKDC1变种的特征.

主要成果:

再组合的HKDC1表现出强大的六金酶活性,具有独特的葡萄糖Km (0.49±0.07毫米).
C端域负责酶的活性,而N端域是不活跃的.
虽然HKDC1对葡萄糖6酸盐和迪纳西克利布的产品抑制不敏感,但它被一种合成葡萄糖胺衍生物 (IC50 = 103 ± 6 nM) 强烈抑制.
与视网膜炎染色体相关的T58M变体显示,催化效率下降了2倍.

结论:

与其他人类基酶相比,HKDC1是一种具有明显的动力和调节性质的催化活性基酶.
它的独特特征,包括对某些抑制剂的不敏感性,表明它在细胞代谢和疾病中发挥了特定的作用.
对HKDC1的功能进行进一步的研究是有必要的,以了解其与癌症和视网膜色素炎等人类疾病的联系.

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