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Therapeutic Targeting of the General RNA Polymerase II Transcription Machinery.
Ryan D Martin, Terence E Hébert, Jason C Tanny
International journal of molecular sciences 2020 May 09
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Inhibitors targeting the general RNA polymerase II (RNAPII) transcription machinery are candidate therapeutics in cancer and other complex diseases. Here, we review the molecular targets and mechanisms of action of these compounds, framing them within the steps of RNAPII transcription. We discuss the effects of transcription inhibitors in vitro and in cellular models (with an emphasis on cancer), as well as their efficacy in preclinical and clinical studies. We also discuss the rationale for inhibiting broadly acting transcriptional regulators or RNAPII itself in complex diseases.
Citation
Ryan D Martin, Terence E Hébert, Jason C Tanny.
Therapeutic Targeting of the General RNA Polymerase II Transcription Machinery.
International journal of molecular sciences.
2020 May 09;21(9)
Mesh Tags
Antineoplastic Agents
Catalysis
Clinical Trials as Topic
Cyclin-Dependent Kinase 8
Cyclin-Dependent Kinase 9
Cyclin-Dependent Kinases
Drug Screening Assays, Antitumor
Gene Expression Regulation, Neoplastic
Humans
Molecular Targeted Therapy
Neoplasm Proteins
Neoplasms
Protein Kinase Inhibitors
RNA Polymerase II
Transcription, Genetic
Substances
Antineoplastic Agents
Neoplasm Proteins
Protein Kinase Inhibitors
CDK8 protein, human
CDK9 protein, human
Cyclin-Dependent Kinase 8
Cyclin-Dependent Kinase 9
Cyclin-Dependent Kinases
RNA Polymerase II
PMID: 32397434
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