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抑制单质人体l-乳酸脱酶组装成催化活性同位素酶的可以降低培养细胞中乳酸的合成

Alessandra Stefan^1,2, Luca Gentilucci³, Francesca Ruffolo¹

¹Department of Pharmacy and Biotechnology, University of Bologna, Bologna, Italy.

Protein science : a publication of the Protein Society

|September 14, 2024

概括

研究人员在中性pH下分离了单质人乳酸脱酶A (hLDH-A),以发现新的癌症药物标. 他们确定了抑制hLDH-A组合的,为过度表达这种酶的癌症提供了一种新的治疗策略.

科学领域:

生物化学生物化学
分子生物学分子生物学
癌症研究癌症研究

背景情况:

癌细胞表现出改变的新陈代谢,通常依赖乳酸脱酶A (LDH-A) 获得能量.
在各种癌症中LDH-A过度表达使其成为一个有前途的治疗点.
以前的LDH-A抑制剂需要酸性条件来分离单体,这限制了生理相关性.

研究的目的:

在生理条件下 (中性pH) 隔离原生单体人类LDH-A (hLDH-A).
为了识别抑制四重体hLDH-A组装的.
评估癌症细胞系中已识别的的治疗潜力.

主要方法:

在中性pH下分离复合单体hLDH-A.
选抑制hLDH-A四聚合物的酸.
使用MCF7和BxPC3细胞系进行基于细胞的测定,以评估的有效性和选择性.
对hLDH-A.的C端区域与的相互作用的分析.

主要成果:

在中性pH下成功分离了单质hLDH-A.
确定了八类GQNGISDL,模仿hLDH-A C端,作为一种抑制剂.
发现了循环四甲cGQND作为活性成分.
通过GQND,在MCF7细胞 (hLDH-A表达) 中被证明选择性抑制乳酸分泌,但在BxPC3细胞 (hLDH-B表达) 中没有.

结论:

模仿hLDH-A C终端区域的可以有效地抑制四聚体组合.
GQND四烯代表了开发向癌症治疗的潜在化合物.
这种方法可以在生理条件下进行查,从而增强相关抑制剂的发现.

关键词:

人类乳酸脱酶A.抑制组装的抑制作用一个单质的单质分子.酸是一种酸.子单位子单位的相互作用.

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