[HTML][HTML] Flavopiridol inhibits P-TEFb and blocks HIV-1 replication
SH Chao, K Fujinaga, JE Marion, R Taube… - Journal of Biological …, 2000 - ASBMB
Flavopiridol (L86-8275, HMR1275) is a cyclin-dependent kinase (Cdk) inhibitor that is in
clinical trials as a cancer treatment because of its antiproliferative properties. We found that
the flavonoid potently inhibited transcription by RNA polymerase II in vitro by blocking the
transition into productive elongation, a step controlled by P-TEFb. The ability of P-TEFb to
phosphorylate the carboxyl-terminal domain of the large subunit of RNA polymerase II was
inhibited by flavopiridol with aK i of 3 nm. Interestingly, the drug was not competitive with …
clinical trials as a cancer treatment because of its antiproliferative properties. We found that
the flavonoid potently inhibited transcription by RNA polymerase II in vitro by blocking the
transition into productive elongation, a step controlled by P-TEFb. The ability of P-TEFb to
phosphorylate the carboxyl-terminal domain of the large subunit of RNA polymerase II was
inhibited by flavopiridol with aK i of 3 nm. Interestingly, the drug was not competitive with …
