Recent advances in the development of cyclin-dependent kinase 7 inhibitors.

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ID: 77178
2019
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Abstract
Cyclin dependent kinase 7 (CDK7) plays a double role as it activates several other cyclin dependent kinases and participates to the initiation of transcription. This kinase is overexpressed in various types of tumors. Relatively few selective CDK7 inhibitors have been up to now disclosed. Most of these inhibitors belong to two chemical families: pyrazolopyrimidines and pyrazolotriazines on one side and pyrimidines on another side. They also differ by their molecular mechanism of action. Some are acting as competitive inhibitors and some others are covalent inhibitors. With these tools, the understanding of the potential therapeutic interest of CDK7 inhibitors in cancer is rapidly growing. They display antiproliferative activity against various types of tumors and leukemia and synergies have been identified. Two inhibitors are undergoing clinical testing. The most potent compounds inhibit a large number of cell-lines with IC < 200 nM.
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teng2019recenteuropean Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Teng, Yuou;Lu, Kui;Zhang, Qian;Zhao, Lianbo;Huang, Yuna;Ingarra, Angela Maria;Galons, Hervé;Li, Tingshen;Cui, Shanshan;Yu, Peng;Oumata, Nassima;
Journal European journal of medicinal chemistry
Year 2019
DOI
S0223-5234(19)30775-5
URL
Keywords
Cancer kinase covalent inhibitor cyclin-dependent kinase 7

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