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Literature summary for 2.7.11.21 extracted from
- Structures of the wild-type and activated catalytic domains of Brachydanio rerio Polo-like kinase 1 (Plk1): changes in the active-site conformation and interactions with ligands (2008), Acta Crystallogr. Sect. D, 64, 909-918.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | Plk1 is a target for the development of anticancer therapeutics | Homo sapiens |
| medicine | Plk1 is a target for the development of anticancer therapeutics | Danio rerio |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| full-length hPlk1 cDNA is inserted into a pCMV plasmid and subcloned into pGEX6P-1, the hPlk1 kinase domain sequences for crystallography and activity constructs encompassing amino acids 1-346 | Homo sapiens |
| full-length zPlk1 cDNA is inserted into the pME18S-FL3 plasmid and subcloned into pGEX6P-1, the zPlk1 kinase domain sequences for crystallography and activity constructs encompassing amino acids 1-312 or 17-312 | Danio rerio |
Crystallization (Commentary)
| Crystallization (Comment) | Organism |
|---|---|
| the structures of wild-type zPlk KD, mutant T196D, wild-type zPlk KD in complex with ADP and the mutant T196D in complex with wortmannin are determined at resolutions of 2.8, 2.4, 2.6 and 2.6 A, respectively | Danio rerio |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| T196D | variant containing an activating substitution | Danio rerio |
| T210D | variant containing an activating substitution | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| Wortmannin | - |
Danio rerio |  |
| Wortmannin | - |
Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0055 | - |
ATP | apparent Km, hPlk1 1-346 T210D | Homo sapiens | |
| 0.0064 | - |
ATP | apparent Km, zPlk1 1-312 T196D | Danio rerio | |
| 0.0076 | - |
ATP | apparent Km, zPlk1 1-312 wild type | Danio rerio | |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 35920 | - |
expected molecular weight of the protein with the N-terminal Gly-Pro-Leu-Gly-Ser linker residues that separate the GST protein from Plk1 KD | Danio rerio |
| 35930 | - |
expected molecular weight of the protein with the additional T196D substitution | Danio rerio |
| 39050 | - |
expected molecular weight of the protein with the N-terminal Gly-Pro-Leu-Gly-Ser linker residues that separate the GST protein from Plk1 KD | Homo sapiens |
| 39060 | - |
expected molecular weight of the protein with the additional T210D substitution | Homo sapiens |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + protein | Homo sapiens | - |
ADP + phosphoprotein | - |
? | |
| ATP + protein | Danio rerio | - |
ADP + phosphoprotein | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Danio rerio | Q6DRK7 | - |
- |
| Homo sapiens | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| using a glutathione-Sepharose and a Q-Sepharose column | Homo sapiens |
| using a glutathione-Sepharose and a Q-Sepharose column | Danio rerio |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + casein | substrate in biochemical activity assay | Homo sapiens | ADP + phosphocasein | - |
? | |
| ATP + casein | substrate in biochemical activity assay | Danio rerio | ADP + phosphocasein | - |
? | |
| ATP + protein | - |
Homo sapiens | ADP + phosphoprotein | - |
? | |
| ATP + protein | - |
Danio rerio | ADP + phosphoprotein | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| hPlk1 | - |
Homo sapiens |
| Plk1 | - |
Homo sapiens |
| Plk1 | - |
Danio rerio |
| Polo-like kinase 1 | - |
Homo sapiens |
| Polo-like kinase 1 | - |
Danio rerio |
| zPlk1 | - |
Danio rerio |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00229 | - |
ATP | zPlk1 1-312 wild type | Danio rerio | |
| 0.01311 | - |
ATP | zPlk1 1-312 T196D | Danio rerio | |
| 0.01386 | - |
ATP | hPlk1 1-346 T210D | Homo sapiens | |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.2 | - |
activity assay | Homo sapiens |
| 7.2 | - |
activity assay | Danio rerio |
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