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使用DNA编码化学技术识别强大的泛埃弗林受体激酶抑制剂

Chandrashekhar Madasu^1,2, Zian Liao^1,2,3, Sydney E Parks^1,2

¹Department of Pathology and Immunology, Baylor College of Medicine, Houston, TX 77030.

Proceedings of the National Academy of Sciences of the United States of America

|May 3, 2024

概括

研究人员使用DNA编码化学库 (DECL) 确定了强大的EPH受体 (EPH) 抑制剂CDD-2693和CDD-3167. 这些化合物通过向EPH激酶活性,在治疗子宫内膜异位症和某些癌症方面表现有前途.

科学领域:

生物化学生物化学
分子生物学分子生物学
药理学药理学是指药理学的学科.

背景情况:

EPH受体 (EPHs) 是最大的氨酸激酶家族,在细胞信号传递中至关重要.
在子宫内膜异位病变中观察到EPHA2和EPHA4的表达增加.
EPH信号与细胞迁移和侵入有关,这表明了治疗点.

研究的目的:

为了确定EPHA2和EPHA4的化学抑制剂,用于潜在的子宫内膜异位症治疗.
选DNA编码化学库 (DECL) 强效的EPH激酶抑制剂.
在子宫内膜异位症和癌症细胞模型中评估已识别的抑制剂的疗效.

主要方法:

对DNA编码化学库 (DECL) 的选,以识别EPHA2/4抑制剂.
生物化学测试 (激酶活性,基因组分析) 和NanoBRET目标参与测试.
基于细胞的测试使用子宫内膜上皮细胞和器官,以及癌症细胞系.

主要成果:

被击中化合物CDD-2693显示了针对EPHA2和EPHA4.4的皮科摩尔/纳米摩尔活性.
优化化合物CDD-3167表现出优越的皮科莫尔生物化学和纳米分子细胞基功效,具有更好的选择性.
在子宫内膜异位症模型中,CDD-2693和CDD-3167降低了EPHA2/4酸化,细胞活力,PTGS2表达和器官扩张.
化合物还降低了尤文肉瘤细胞的活力.

结论:

用DNA编码的化学库 (DECL) 有效地识别了强大的泛EPH抑制剂.
CDD-3167对子宫内膜异位症和癌症模型具有显著的特异性和细胞活性.
这些抑制剂代表了对子宫内膜异位症和癌症治疗的有希望的治疗候选者.

关键词:

通过DNA编码的化学成分.子宫内膜异位症是什么?子宫内膜异位症是什么埃弗林受体激酶抑制剂的使用

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