Drug-Resistant Bacterial Topoisomerases
We offer various quinolone- and coumarin-resistant topoisomerase mutants from a range of organisms including E. coli, and S. aureus. The proteins can be supplied as separate subunits or as reconstituted enzyme. Typically the quinolone-resistant mutants confer 50-100 X more resistance to fluoroquinolones than the wild-type. We have more than 25 mutants in different topoisomerases and can make other mutants as requested. For the currently available mutants please see the table below:
| Organism/Subunit | Mutation | Resistance/Activity affected |
| E. coli gyrase | ||
| GyrA | S83T,C,L,W | Quinolone |
| GyrA | S83A/D87A double | Quinolone |
| GyrA | D87A, H, K | Quinolone |
| GyrA | D82N | Quinolone |
| GyrA | R91Q | Simocyclinone |
| GyrA | A84Y | Simocyclinone |
| GyrA | A84R | Simocyclinone |
| GyrA | K42A | Simocyclinone |
| GyrA | M120P | Simocyclinone |
| GyrA | M120K | NXL101 |
| GyrA | L387F | Exit gate mutant |
| GyrA | K465A | Exit gate mutant |
| GyrA55 | L387F A55 | Exit gate mutant |
| GyrA55 | K465A A55 | Exit gate mutant |
| GyrA | C194A/C592A/C716A/C792A/G81C | One cysteine only |
| GyrA | L3461CL463C | Exit gate mutant |
| GyrB | W751R | MicrocinB17 |
| GyrB24 | R136 | Coumarin |
| GyrB | D426N | Quinolone |
| GyrB | K110A | |
| GyrB | K103A K110A | ATP coupling |
| GyrB43 | loopless mutant' | ATP coupling |
| S. aureus gyrase | ||
| GyrA | D83N | Quinolone |
| GyrA | S84L | Quinolone |
| GyrB | T173N | Novobiocin |
| GyrB | G35S | |
| GyrB | S128F | |
| GyrB | R144I | |
| M. tuberculosis gyrase | ||
| GyrA | D94G | Novobiocin |
| GyrB | T539N | Quinolone |
| GyrB | A53S | |
| GyrB | A57V | |
| GyrB | V125L | |
| GyrB | S169A | |
| A. baumanni gyrase | ||
| GyrB | R150C | |
| S. pneumoniae Topo IV | ||
| ParC | S79F | |
| ParC | S80F | |
| E. coli Topo IV | ||
| ParC | S80I | |
| S. aureus Topo IV | ||
| ParC/GrlA | S80F |
Please contact us directly for more information or to request pricing!
We have a range of products that will help your drug discovery efforts, whether you are looking for novel anti-infectives, or new anti-cancer compounds, we have a range of target enzymes, available with and without their substrates, in easy to use kits. We also supply different topological isoforms of our DNA substrates.
Don't see your required enzyme? Contact us to see if we can make it for you or visit our Custom Proteins page!
Not doing drug discovery? Our enzymes and DNA substrates are of extremely high purity and quality, perfect for reliable results!
All of our enzymes can be supplied in large or bulk quantities or at higher concentrations. Please contact us for a quote!
Likewise, if you require enzymes with particular specifications (e.g. low endotoxin, DNase or RNase free, low bioburden etc.), please contact us.
You can contact us on +44(0) 1603 673590 or +44(0) 1603 673591, at [email protected] or by visiting our contact us page to discuss your requirements.