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. 2020 Jan 21;9(2):266. doi: 10.3390/cells9020266

Table 1.

Chemotherapeutics affecting Pol I transcription.

Drug Type Drug Specific Pol I Inhibitor General Mechanism of Action Effect on Pol I Transcription NSP Activation Clinical Use References
Alkylating Agent Cisplatin No DNA damage
DNA synthesis inhibition
Inhibition—Sequestration of UBF Yes Yes [47,48,49]
Oxaliplatin No DNA damage
DNA synthesis inhibition
Inhibition—Sequestration of UBF Yes Yes [47,49,50]
Anti-Metabolite 5-Fluorouracil No Uracil analogue
Thymidine Synthetase inhibitor
Intercalation into DNA and RNA
Inhibition of rRNA processing
Intercalation into rRNA
No Yes [47]
Methotoxate No Folate analogue
Disruption of thymidine synthesis
Inhibition
Undetermined mechanism
Yes Yes [47]
Antibiotics Actinomycin D No DNA intercalation Inhibition of transcription elongation Yes Yes [51]
Doxorubicin No DNA intercalation
Topoisomerase II inhibitor
Inhibition—Likely prevention of transcription initiation Yes Yes [52]
Mitoxantrone No DNA intercalation
Topoisomerase II inhibitor
Inhibition—Likely prevention of transcription initiation Yes Yes [52]
Mitomycin C No DNA alkylation Inhibition—Undetermined mechanism Yes Yes [47]
Plant Alkaloids Campthotecin No Topoisomerase inhibitor
DNA intercalation
Inhibition—Undetermined mechanism Yes Yes [53]
Irinotecan No Topoisomerase inhibitor Inhibition—Undetermined mechanism Yes Yes [47,53]
Etoposide No Topoisomerase inhibitor Inhibition—Undetermined mechanism Yes Yes [53]
Ellipticine derivatives No SL-1 displacement
Topoisomerase II inhibitor
Inhibition of transcription initiation Yes Failed clinical trial phase II [54]
Specific Pol I Inhibitors CX-3543 No Dissociation of Nucleolin-rDNA
G-quadruplex complexes
Inhibition—Undetermined mechanism Yes Clinical trial phase II [55]
CX-5461 No Disruption of interaction between SL-1 and Pol I at the rRNA promoter Inhibition of transcription initiation Yes Clinical trial phase II [56]
BMH-21 No Degradation of RPA194 and displacement of RRN3 Inhibition of transcription elongation No No [57]