POLR2E Inhibitors

POLR2E Inhibitors comprises diverse compounds, many of which target RNA polymerase II or influence associated cellular pathways, thereby indirectly affecting the POLR2E subunit. α-Amanitin, renowned for its potency, directly inhibits RNA polymerase II. Actinomycin D's mechanism involves DNA intercalation, rendering the progression of RNA polymerase II impossible. On the other hand, Triptolide operates by specifically binding to the XPB subunit of the polymerase, blocking its function.

Several compounds exert influence indirectly. DRB and Flavopiridol meddle with the phosphorylation state of RNA polymerase II, a process vital for transcription. JQ1's mechanism is even more indirect, targeting BET bromodomains that play crucial roles in transcriptional regulation. The effects of Pladienolide B, which disturbs pre-mRNA splicing, and THZ1, targeting CDK7, also manifest on RNA polymerase II. Other compounds like Cordycepin and MLN4924 bring in a breadth of mechanisms. While Cordycepin prompts early transcription termination, MLN4924 impacts a variety of cellular processes. Kinase inhibitors like Sorafenib and Ibrutinib can modulate RNA polymerase II's function through their broad cellular impacts.