Cloned (Comment) | Organism |
---|---|
- |
Mycobacterium tuberculosis |
- |
Mycolicibacterium smegmatis |
Crystallization (Comment) | Organism |
---|---|
hanging drop vapor diffusion | Mycobacterium tuberculosis |
hanging drop vapor diffusion | Mycolicibacterium smegmatis |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
rifampicin | - |
Mycobacterium tuberculosis | |
rifampicin | - |
Mycolicibacterium smegmatis | |
sorangicin A | inhibits the wild-type and mutant (S447/S456L) RNA polymerase through different mechanisms. It has a better pharmacokinetic profile than rifampicin, making it a suitable starting molecule to design drugs to be used for the treatment of tuberculosis patients with comorbidities who require multiple medications | Mycobacterium tuberculosis | |
sorangicin A | inhibits the wild-type and mutant (S447/S456L) RNA polymerase through different mechanisms. It has a better pharmacokinetic profile than rifampicin, making it a suitable starting molecule to design drugs to be used for the treatment of tuberculosis patients with comorbidities who require multiple medications; the inhibitor binds in the Rif-binding pocket of RNA. It inhibits inhibits the wild-type enzyme (RNAP) by a similar mechanism as rifampicin by preventing the translocation of very short RNAs. It inhibits the RifR S456L enzyme at an earlier step, preventing the transition of a partially unwound promoter DNA intermediate to the fully opened DNA and blocking the template-strand DNA from reaching the active site in the RNAP catalytic center | Mycolicibacterium smegmatis |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Mycobacterium tuberculosis | P9WGY9 AND P9WGY7 AND P9WGZ1 AND P9WGY5 AND P9WGI1 | P9WGY9: subunit beta, P9WGY7: subunit beta', P9WGZ1: subunit alpha, P9WGY5: omega subunit, P9WGI1: sigma factor SigA, the RNAP catalytic core consists of 2 alpha, 1 beta, 1 beta' and 1 omega subunit. When a sigma factor is associated with the core the holoenzyme is formed, which can initiate transcription | - |
Mycobacterium tuberculosis ATCC 25618 | P9WGY9 AND P9WGY7 AND P9WGZ1 AND P9WGY5 AND P9WGI1 | P9WGY9: subunit beta, P9WGY7: subunit beta', P9WGZ1: subunit alpha, P9WGY5: omega subunit, P9WGI1: sigma factor SigA, the RNAP catalytic core consists of 2 alpha, 1 beta, 1 beta' and 1 omega subunit. When a sigma factor is associated with the core the holoenzyme is formed, which can initiate transcription | - |
Mycolicibacterium smegmatis | A0QSL8 AND P60281 AND A0QS66 AND A0QWT1 | A0QSL8: rpoA, subunit alpha, P60281: rpoB, subunit beta, A0QS66: rpoC, subunit beta', A0QWT1: rpoZ, subunit omega | - |
Mycolicibacterium smegmatis | P60281 AND A0QS66 AND A0QSL8 AND A0QWT1 AND A0QW02 | P60281: beta subunit, A0QS66: beta' subunit, A0QSL8: alpha subunit, A0QWT1: omega subunit, A0QW02: sigma factor The RNAP catalytic core consists of 2 alpha, 1 beta, 1 beta' and 1 omega subunit. When a sigma factor is associated with the core the holoenzyme is formed, which can initiate transcription | - |
Mycolicibacterium smegmatis ATCC 700084 | A0QSL8 AND P60281 AND A0QS66 AND A0QWT1 | A0QSL8: rpoA, subunit alpha, P60281: rpoB, subunit beta, A0QS66: rpoC, subunit beta', A0QWT1: rpoZ, subunit omega | - |
Mycolicibacterium smegmatis ATCC 700084 | P60281 AND A0QS66 AND A0QSL8 AND A0QWT1 AND A0QW02 | P60281: beta subunit, A0QS66: beta' subunit, A0QSL8: alpha subunit, A0QWT1: omega subunit, A0QW02: sigma factor The RNAP catalytic core consists of 2 alpha, 1 beta, 1 beta' and 1 omega subunit. When a sigma factor is associated with the core the holoenzyme is formed, which can initiate transcription | - |
Purification (Comment) | Organism |
---|---|
- |
Mycobacterium tuberculosis |
- |
Mycolicibacterium smegmatis |
Synonyms | Comment | Organism |
---|---|---|
rifampicin-resistant RNA polymerase | - |
Mycolicibacterium smegmatis |
RNAP | - |
Mycolicibacterium smegmatis |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000005 | - |
pH 7.9, 37°C | Mycolicibacterium smegmatis | sorangicin A | |
0.000008 | - |
pH 7.9, 37°C | Mycolicibacterium smegmatis | rifampicin | |
0.00001 | - |
pH 7.9, 37°C | Mycobacterium tuberculosis | rifampicin | |
0.000033 | - |
pH 7.9, 37°C | Mycobacterium tuberculosis | sorangicin A | |
0.005 | - |
pH and temperature not specified in the publication | Mycolicibacterium smegmatis | rifampicin | |
0.008 | - |
pH and temperature not specified in the publication | Mycolicibacterium smegmatis | sorangicin A |
General Information | Comment | Organism |
---|---|---|
drug target | sorangicin A inhibits the wild-type and mutant RNA polymerase through different mechanisms. It has a better pharmacokinetic profile than rifampicin, making it a suitable starting molecule to design drugs to be used for the treatment of tuberculosis patients with comorbidities who require multiple medications | Mycobacterium tuberculosis |
drug target | sorangicin A inhibits the wild-type and mutant RNA polymerase through different mechanisms. It has a better pharmacokinetic profile than rifampicin, making it a suitable starting molecule to design drugs to be used for the treatment of tuberculosis patients with comorbidities who require multiple medications | Mycolicibacterium smegmatis |