Size matters, so does shape: Inhibition of transcription of T7 RNA polymerase by iron(II) clathrochelates

• T7 RNA polymerase is inhibited by iron(II) clathrochelates.
• Topoisomerase I functionality is not affected by the compounds studied.
• Mechanism of inhibition of transcription does not include intercalation.
• Binding pocket is formed by the surfaces of the protein, DNA and transcribed RNA.

Coordination and organoelement compounds are rarely proposed as the drug candidates despite their vast potential in the area owing to their strictly controlled geometry and rather extensive surface. This is the first example of the inhibition of transcription in the system of T7 RNA polymerase by cage metal complexes. Their IC50 values reach as low as the nanomolar range, placing them among the most potent metal-based transcription inhibitors.

The first example of the inhibition of transcription in the system of T7 RNA polymerase by cage metal complexes.Figure optionsDownload as PowerPoint slide