Advancements in chemical biology targeting the kinases and phosphatases of RNA polymerase II-mediated transcription.

ABSTRACT: Phosphorylation of RNA polymerase II (RNAP II) coordinates the temporal progression of eukaryotic transcription. The development and application of chemical genetic methods have enhanced our ability to investigate the intricate and intertwined pathways regulated by the kinases and phosphatases targeting RNAP II to ensure transcription accuracy and efficiency. Although identifying small molecules that modulate these enzymes has been challenging due to their highly conserved structures, powerful new chemical biology strategies such as targeted covalent inhibitors and small molecule degraders have significantly improved chemical probe specificity. The recent success in discovering phosphatase holoenzyme activators and inhibitors, which demonstrates the feasibility of selective targeting of in

SUBMITTER: Kim W 

PROVIDER: S-EPMC8384638 | biostudies-literature | 2021 Aug

REPOSITORIES: biostudies-literature