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Updated: Jun 23, 2025

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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用三酸连体发现新型CDK9抑制剂:设计,合成和生物评估

Ye Zhong1, Jing Xu2, Shaoyue Ding1

  • 1Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China.

Bioorganic chemistry
|June 15, 2024
PubMed
概括

新的三酸配体为癌症治疗提供选择性CDK9抑制. 化合物Z4-7a通过通过RNA聚合酶II抑制诱导亡,有效地抑制HCT116细胞增殖.

关键词:
细胞灭亡 (apoptosis) 是一种死亡的过程.在CDK9中,CDK9是CDK9.结肠直肠癌是一种癌症.抑制剂的抑制剂三酸联体三酸联体.

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Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
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