Inhibiting eukaryotic transcription. Which compound to choose? How to evaluate its activity?
Volume 2, Issue 3
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Pages 103 - 108http://dx.doi.org/10.4161/trns.2.3.16172
Authors: Olivier Bensaude View affiliations
This review deals first with general questions: how to evaluate transcription inhibition, describe changes in nuclear structure due to transcription inhibition, report on genes that are paradoxically stimulated by transcription inhibition. Next, it reviews the characteristics and mechanisms of commonly used inhibitors. α-amanitin is highly selective for RNAP II and RNAP III but its action is slow, actinomycin D is fast but its selectivity is poor, CDK9 inhibitors such as DRB, flavopiridol, are fast and reversible but many genes escape transcription inhibition. New compounds such as triptolide are fast, selective and completely arrest transcription as they trigger rapid degradation of RNAP II.
Received: April 12, 2011; Accepted: April 28, 2011