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Literature summary for 5.6.2.1 extracted from

  • Osheroff, N.
    Unraveling the structure of the variola topoisomerase IB-DNA complex: a possible new twist on smallpox therapy (2006), Mol. Interv., 6, 245-248.
    View publication on PubMed
Search for more literature for 5.6.2.1

Application

Application Comment Organism
pharmacology The structure of the variola topoisomerase IB–DNA 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 (Commentary)

Crystallization (Comment) Organism
crystal structure of the non-covalent variola topoisomerase IB–DNA complex and that of the covalent enzyme–DNA 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

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 [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 IB–DNA complex and that of the covalent enzyme–DNA 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

Organism UniProt Comment Textmining
Variola virus
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Synonyms

Synonyms Comment Organism
Poxviridae topoisomerase IB
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 Variola virus
variola topoisomerase IB type IB Variola virus