Inhibiting eukaryotic transcription: which compound to choose? How to evaluate its activity
Open accessAbstract
This review first discusses ways in which we can evaluate transcription inhibition, describe changes in nuclear structure due to transcription inhibition, and report on genes that are paradoxically stimulated by transcription inhibition. Next, it summarizes 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 and flavopiridol are fast and reversible but many genes escape transcription inhibition. New compounds, such as triptolide, are fast and selective and able to completely arrest transcription by triggering rapid degradation of RNAP II.
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ActD nonspecifically blocks all types of RNA polymerase.
“ActD nonspecifically blocks all types of RNA polymerase (96).”
From Impaired function of rDNA transcription initiation machinery leads to derepression of ribosomal genes with insertions of R2 retrotransposon (2022) · cites this paper as [96]
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- Authors
- Bensaude, O.
- Affiliations
- Centre National de la Recherche Scientifique (FR)
- Corresponding author
- Bensaude, Olivier
- ORCID
- Bensaude, Olivier
- Venue
- Transcription
- Publisher
- Informa UK Limited
- Published
- 2011-05
- Volume
- 2
- Issue
- 3
- Pages
- 103-108
- ISSN
- 2154-1264 (ISSN-L)
- 2154-1272
- PMC
- PMC3173647
- OpenAlex
- W2196899564
- Cited by
- 574
- References
- 2
- Citations by year
- 2026: 23 · 2025: 40 · 2024: 50 · 2023: 36 · 2022: 57 · 2021: 64 · 2020: 40 · 2019: 56 · 2018: 58 · 2017: 35 · 2016: 29 · 2015: 27 · 2014: 29 · 2013: 24 · 2012: 5
- FWCI
- 7.54
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- cc-by-nc
- Locations
- Transcription (publishedVersion, cc-by-nc)
- Europe PMC (PubMed Central) (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Genomics and Chromatin Dynamics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nuclear Structure and Function
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Histone Deacetylase Inhibitors Research
- Keywords
- transcription inhibition, eukaryotic transcription, RNA polymerase II, RNA polymerase III, alpha-amanitin, actinomycin D, CDK9 inhibitor, DRB, flavopiridol, triptolide, nuclear structure
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