Application | Comment | Organism |
---|---|---|
pharmacology | The structure of the variola topoisomerase IBDNA cleavage complex, together with the unique biochemical features of the enzyme, provides a starting point for the rational design of antismallpox therapeutics | Variola virus |
Crystallization (Comment) | Organism |
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crystal structure of the non-covalent variola topoisomerase IBDNA complex and that of the covalent enzymeDNA cleavage complex are known. These structures provide an explanation for some of the unique features of Poxviridae topoisomerase IB. Crystal structures of the variola and human topoisomerase IB-DNA cleavage complexes compared | Variola virus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
additional information | Poxviridae topoisomerase IB is insensitive to camptothecin. Because Poxviridae topoisomerase IB is not essential for the viral life cycle, the preferred strategy would be to develop agents that act as topoisomerase poisons rather than catalytic inhibitors. By trapping the cleavage complex, drug treatment could either fragment the viral genome or block early transcription by placing a covalently attached protein in the path of RNA polymerase. High-throughput screen identified nineteen compounds with activity against vaccinia topoisomerase IB with IC50 values in the low micromolar range and displayed no inhibition of human topoisomerase IB | Variola virus |
Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
---|---|---|---|
32000 | - |
poxviridae topoisomerase smallest known topoisomerase, maintains higher levels of covalent enzyme-cleaved DNA intermediates during its catalytic cycle than the eukaryotic type IB enzyme. Poxviridae topoisomerase is refractory to the drug camptothecin. Poxviridae topoisomerase IB is highly sequence specific. Crystal structure of the non-covalent variola topoisomerase IBDNA complex and that of the covalent enzymeDNA cleavage complex are known. These structures provide an explanation for some of the unique features of Poxviridae topoisomerase IB. Crystal structures of the variola and human topoisomerase IB-DNA cleavage complexes compared | Variola virus |
Organism | UniProt | Comment | Textmining |
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Variola virus | - |
- |
- |
Synonyms | Comment | Organism |
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Poxviridae topoisomerase IB | - |
Variola virus |
variola topoisomerase IB | type IB | Variola virus |