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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 50  < 200 nM.

Titel:	Recent advances in the development of cyclin-dependent kinase 7 inhibitors.
Autor/in / Beteiligte Person:	Teng, Y ; Lu, K ; Zhang, Q ; Zhao, L ; Huang, Y ; Ingarra, AM ; Galons, H ; Li, T ; Cui, S ; Yu, P ; Oumata, N
Link:	Zum Volltext
Zeitschrift:	European journal of medicinal chemistry, Jg. 183 (2019-12-01), S. 111641
Veröffentlichung:	Paris : Editions Scientifiques Elsevier ; <i>Original Publication</i>: Paris, S.E.C.T. [etc.], 2019
Medientyp:	academicJournal
ISSN:	1768-3254 (electronic)
DOI:	10.1016/j.ejmech.2019.111641
Schlagwort:	Animals Antineoplastic Agents pharmacology Cell Line, Tumor Cell Survival drug effects Drug Development Humans Protein Kinase Inhibitors pharmacology Pyrimidines pharmacology Triazines pharmacology Cyclin-Dependent Kinase-Activating Kinase Antineoplastic Agents chemistry Cyclin-Dependent Kinases antagonists & inhibitors Protein Kinase Inhibitors chemistry Pyrimidines chemistry Triazines chemistry
Sonstiges:	Nachgewiesen in: MEDLINE Sprachen: English Publication Type: Journal Article; Review Language: English [Eur J Med Chem] 2019 Dec 01; Vol. 183, pp. 111641. <i>Date of Electronic Publication: </i>2019 Aug 22. MeSH Terms: Antineoplastic Agents / chemistry ; Cyclin-Dependent Kinases / antagonists & inhibitors ; Protein Kinase Inhibitors / chemistry ; Pyrimidines / chemistry ; Triazines / *chemistry ; Animals ; Antineoplastic Agents / pharmacology ; Cell Line, Tumor ; Cell Survival / drug effects ; Drug Development ; Humans ; Protein Kinase Inhibitors / pharmacology ; Pyrimidines / pharmacology ; Triazines / pharmacology ; Cyclin-Dependent Kinase-Activating Kinase Contributed Indexing: Keywords: Cancer; Covalent inhibitor; Cyclin-dependent kinase 7; Kinase Substance Nomenclature: 0 (Antineoplastic Agents) ; 0 (Protein Kinase Inhibitors) ; 0 (Pyrimidines) ; 0 (Triazines) ; EC 2.7.11.22 (Cyclin-Dependent Kinases) ; EC 2.7.11.22 (Cyclin-Dependent Kinase-Activating Kinase) ; 0 (CDK7 protein, human) Entry Date(s): Date Created: 20190913 Date Completed: 20200114 Latest Revision: 20221207 Update Code: 20240513

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