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发现了强大的抗疟疾II型激酶抑制剂,其选择性超过人类激酶

Lushun Wang1, Monica J Bohmer2, Jinhua Wang3,4

  • 1Department of Chemical and Systems Biology, ChEM-H, Stanford Cancer Institute, School of Medicine, Stanford University, Stanford, California 94305, United States.

Journal of medicinal chemistry
|January 12, 2024
PubMed
概括

新型抗疟疾化合物是通过重新利用人类激酶抑制剂来开发的. 化合物1针对EphA2被优化为化合物33,显示出针对疟疾的改善活性.

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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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