2. Academic Validation
  3. Recent advances in the development of cyclin-dependent kinase 7 inhibitors

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

  • Eur J Med Chem. 2019 Dec 1:183:111641. doi: 10.1016/j.ejmech.2019.111641.
Yuou Teng 1,  Kui Lu 1,  Qian Zhang 1,  Lianbo Zhao 1,  Yuna Huang 1,  Angela Maria Ingarra 2,  Hervé Galons 3,  Tingshen Li 1,  Shanshan Cui 1,  Peng Yu 1,  Nassima Oumata 4
Affiliations

Affiliations

  • 1 China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Biotechnology, Tianjin University of Science and Technology, Tianjin, 300457, China.
  • 2 Unité de Technologies Chimiques et Biologiques pour la Santé, Université Paris Descartes UMR-S 1022 Inserm, 4 avenue de l'Observatoire, Paris, 75006, France; Dipartimento di Scienze e Tecnologie Biologiche Chimiche eFarmaceutiche (STEBICEF), Universita degli Studi di Palermo, Via Archirafi 32, 90123, Palermo, Italy.
  • 3 Unité de Technologies Chimiques et Biologiques pour la Santé, Université Paris Descartes UMR-S 1022 Inserm, 4 avenue de l'Observatoire, Paris, 75006, France.
  • 4 Unité de Technologies Chimiques et Biologiques pour la Santé, Université Paris Descartes UMR-S 1022 Inserm, 4 avenue de l'Observatoire, Paris, 75006, France. Electronic address: nessoumata@yahoo.fr.
PMID: 31514062 DOI: 10.1016/j.ejmech.2019.111641
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 IC50 < 200 nM.

Keywords

Cancer; Covalent inhibitor; Cyclin-dependent kinase 7; Kinase.

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