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Literature summary extracted from
- DNA topoisomerase I from parasitic protozoa: a potential target for chemotherapy (2006), Biochim. Biophys. Acta, 1759, 117-131.
Application
| EC Number | Application | Comment | Organism |
|---|---|---|---|
| 5.6.2.1 | drug development | DNA topoisomerase I is a potential target for chemotherapy | Trypanosoma brucei |
| 5.6.2.1 | drug development | DNA topoisomerase I is a potential target for chemotherapy | Plasmodium falciparum |
| 5.6.2.1 | drug development | DNA topoisomerase I is a potential target for chemotherapy | Homo sapiens |
| 5.6.2.1 | drug development | DNA topoisomerase I is a potential target for chemotherapy | Leishmania major |
| 5.6.2.1 | drug development | DNA topoisomerase I is a potential target for chemotherapy | Mammalia |
| 5.6.2.1 | drug development | DNA topoisomerase I is a potential target for chemotherapy | Trypanosoma congolense |
| 5.6.2.1 | drug development | DNA topoisomerase I is a potential target for chemotherapy | Trypanosoma cruzi |
| 5.6.2.1 | drug development | DNA topoisomerase I is a potential target for chemotherapy | Leishmania donovani |
Protein Variants
| EC Number | Protein Variants | Comment | Organism |
|---|---|---|---|
| 5.6.2.1 | G185R/D325E | highly camptothecin-resistant with two substitutions in the core domain of the protein | Leishmania donovani |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 5.6.2.1 | 5,7-dioxo-5,6,7,13-tetrahydro-12H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-12-yl D-allopyranoside | dideschlororebeccamycin, RM762, indolocarbazole derivative | Leishmania donovani |  |
| 5.6.2.1 | arciriaflavin A | RM62, indolocarbazole derivative | Leishmania donovani | |
| 5.6.2.1 | Berberine | a polyheterocyclic class I topoisomerase inhibitor with a structure resembling the intercalant drug benzo[a]acridine. Several berberine analogues tested | Leishmania donovani | |
| 5.6.2.1 | Berberine | is a polyheterocyclic class I topoisomerase inhibitor with a structure resembling the intercalant drug benzo[a]acridine. Several berberine analogues tested | Trypanosoma brucei | |
| 5.6.2.1 | Berberine | is a polyheterocyclic class I topoisomerase inhibitor with a structure resembling the intercalant drug benzo[a]acridine. Several berberine analogues tested | Trypanosoma congolense | |
| 5.6.2.1 | camptothecin | class I topoisomerase poison. Pentacyclic natural alkaloid produced by the plant Camptotheca accuminata | Homo sapiens | |
| 5.6.2.1 | camptothecin | class I topoisomerase poison. Pentacyclic natural alkaloid produced by the plant Camptotheca accuminata | Leishmania donovani | |
| 5.6.2.1 | camptothecin | class I topoisomerase poison. Pentacyclic natural alkaloid producted by the plant Camptotheca accuminata. Camptothecin is cytotoxic for the erythrocytic forms of Plasmodium falciparum | Plasmodium falciparum | |
| 5.6.2.1 | camptothecin | class I topoisomerase poison. Pentacyclic natural alkaloid produced by the plant Camptotheca accuminata | Trypanosoma brucei | |
| 5.6.2.1 | coralyne | derivative of berberine has shown effectively combat Trypanosoma cruzi infection | Trypanosoma cruzi | |
| 5.6.2.1 | dihydrobetulinic acid | DHBA inhibits by preventing enzyme DNA binary complex formation. Inhibits also topoisomerase II | Leishmania donovani | |
| 5.6.2.1 | diospyrin | naphthoquinone derivative | Leishmania donovani | |
| 5.6.2.1 | irinotecan | water soluble derivatives of camptothecin, hardly effective against bloodstream forms of Trypanosoma brucei | Trypanosoma brucei | |
| 5.6.2.1 | MJ-III-65 | indenoisoquinoline analogue | Leishmania major | |
| 5.6.2.1 | additional information | intercalation of indolocarbazole drugs in the DNA molecule is reinforced by the existance of the sugar moiety, which helps to stabilize the insertion complex by binding with the major groove of the ternary duplex DNA. The presence of chlorine atoms disminishes topoisomerase I inhibition | Leishmania donovani | |
| 5.6.2.1 | rebeccamycin | REB, indolocarbazole derivative | Leishmania donovani | |
| 5.6.2.1 | rebeccamycin | - |
Trypanosoma brucei | |
| 5.6.2.1 | topotecan hydrochloride | water soluble derivatives of camptothecin, hardly effective against bloodstream forms of Trypanosoma brucei | Trypanosoma brucei | |
Molecular Weight [Da]
| EC Number | Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|---|
| 5.6.2.1 | 28000 | - |
small subunit LdTOPIB, on chromosome 4, encoding for a 262-amino acid polypeptide. The small subunit contains SKXXY motif placed at the C-terminal domain of all type I DNA topoisomerases, which conserves the tyrosine residue that plays a role in DNA cleavage | Leishmania donovani |
| 5.6.2.1 | 73000 | - |
large subunit LdTOPIA, on chromosome 34, encoding for a 636-amino acid polypeptide | Leishmania donovani |
| 5.6.2.1 | 91000 | - |
- |
Homo sapiens |
| 5.6.2.1 | 91000 | - |
- |
Mammalia |
| 5.6.2.1 | 104000 | - |
- |
Plasmodium falciparum |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 5.6.2.1 | Homo sapiens | - |
- |
- |
| 5.6.2.1 | Leishmania donovani | - |
- |
- |
| 5.6.2.1 | Leishmania major | - |
- |
- |
| 5.6.2.1 | Mammalia | - |
- |
- |
| 5.6.2.1 | Plasmodium falciparum | - |
- |
- |
| 5.6.2.1 | Trypanosoma brucei | Q581U8 | - |
- |
| 5.6.2.1 | Trypanosoma congolense | - |
- |
- |
| 5.6.2.1 | Trypanosoma cruzi | - |
- |
- |
Subunits
| EC Number | Subunits | Comment | Organism |
|---|---|---|---|
| 5.6.2.1 | heterodimer | presence of two separate genes encoding for the core and catalytic domains, indicating that this singular feature is common to all trypanosomatids | Trypanosoma cruzi |
| 5.6.2.1 | heterodimer | the genes encoding each protein subunit are located on different chromosomes | Leishmania donovani |
| 5.6.2.1 | monomer | Three structural domains, N-terminus domain (134 amino acids) poorly conserved, a 500 amino acid length block of conserved amino acids with high homology to the core domain of the human protein, the C-terminal domain is smaller than the hosts' but conserves the active tyrosine at position 798 which makes the enzyme fully active | Plasmodium falciparum |
| 5.6.2.1 | monomer | 765 amino acids. All type IB topoisomerases contain a conserved SKXXY signature in the region in which a tyrosine residue (Tyr-723 in the human topoisomeraseI) is the DNA-cleaving amino acid | Homo sapiens |
| 5.6.2.1 | monomer | 765 amino acids. All type IB topoisomerases contain a conserved SKXXY signature in the regionin which a tyrosine residue is the DNA-cleaving amino acid | Mammalia |
| 5.6.2.1 | additional information | multimeric status of Trypanosoma brucei TopI. Molecular mass determination by gel filtration chromatography suggests that the native enzyme might exist as a tetrameric active A2B2 form or two heterodimers would facilitate the binding at the helical crossover points of DNA | Trypanosoma brucei |
| 5.6.2.1 | additional information | regulation of DNA topoisomerase I, different expression patterns described in the distinct life cycle stages of Plasmodium falciparum. An indirect evidence of potential post-translational mechanisms which could operate on Plasmodium topoisomerases at different stages of its life cycle | Plasmodium falciparum |
| 5.6.2.1 | additional information | relaxation activity of human TopI by adding to the core domain a series of peptides containing the C-terminal domain in the presence of DNA. Reinforced by using a two-hybrid expression system, identified proteins containing part of the linker and the C-terminal domain that supplemented the catalytic core of Saccharomyces cerevisiae topoisomerase I | Homo sapiens |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 5.6.2.1 | DNA topoisomerase I | - |
Trypanosoma brucei |
| 5.6.2.1 | DNA topoisomerase I | - |
Plasmodium falciparum |
| 5.6.2.1 | DNA topoisomerase I | - |
Homo sapiens |
| 5.6.2.1 | DNA topoisomerase I | - |
Leishmania major |
| 5.6.2.1 | DNA topoisomerase I | - |
Mammalia |
| 5.6.2.1 | DNA topoisomerase I | - |
Trypanosoma congolense |
| 5.6.2.1 | DNA topoisomerase I | - |
Trypanosoma cruzi |
| 5.6.2.1 | DNA topoisomerase I | - |
Leishmania donovani |
| 5.6.2.1 | PfTopI | - |
Plasmodium falciparum |
| 5.6.2.1 | TopI | - |
Homo sapiens |
pI Value
| EC Number | Organism | Comment | pI Value Maximum | pI Value |
|---|---|---|---|---|
| 5.6.2.1 | Trypanosoma brucei | overall charge difference observed, proposed that the protein regions bearing these differences may contribute to establishing ionic interactions that hold the subunits together | - |
additional information |
| 5.6.2.1 | Trypanosoma brucei | small subunit | - |
5.21 |
| 5.6.2.1 | Trypanosoma brucei | large subunit | - |
9.47 |
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