Chemical inhibitors of transcription-associated kinases. (October 2022)

• Record Type: Journal Article
• Authors: Clopper, Kevin C.; Taatjes, Dylan J.
• Is Part Of: Current opinion in chemical biology. Volume 70(2022)
• Publication Date: 2022-10
• Subjects: Transcription -- Kinase -- Kinase inhibitor -- CDK7 -- CDK8 -- CDK19 -- CDK9 -- CDK12 -- CDK13 -- RNA polymerase II; Bioorganic chemistry -- Periodicals; Biology -- Periodicals; Biochemistry -- Periodicals; Clinical biochemistry -- Periodicals; Biochemistry -- Periodicals; Chimie bio-organique -- Périodiques; Biologie -- Périodiques; 572.05
• DOI: 10.1016/j.cbpa.2022.102186
• Languages: English
• ISSNs: 1367-5931

Abstract

Abstract: Transcription by RNA polymerase II (pol II) is regulated by kinases. In recent years, many selective and potent inhibitors of pol II transcription-associated kinases have been developed, and these molecules have advanced understanding of kinase function in mammalian cells. Here, we focus on chemical inhibitors of the transcription-associated kinases CDK7, CDK8, CDK9, CDK12, CDK13, and CDK19. We provide a brief overview of the function of these kinases and common activation mechanisms. We then highlight the advantages of kinase inhibitors compared with other basic research methods, and describe the caveats associated with non-selective compounds (e.g. flavopiridol). We conclude with strategies and recommendations for implementation of chemical inhibitors for experimental analysis of transcription-associated kinases.