Publication at Faculty of Mathematics and Physics |
2009
Abstract
Although transcription is of central importance to cell survival, only few antimicrobial agents have been directed towards the RNA polymerase (RNAP) enzyme. Rifampicin, one of the most potent and broad spectrum antibiotics and a key component of anti-tuberculosis therapy, binds in a pocket of the RNAP deep within the DNA/RNA channel, but more than 12 ao away from the active site.
Unfortunately, binding of Rifampicin can be easily disturbed by enzyme mutations. Therefore, we are interested in blocking of active sites of bacterial RNAPs directly - using analogs of NTPs.