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Literature summary for 2.7.11.21 extracted from
- Structure of the Brachydanio rerio Polo-like kinase 1 (Plk1) catalytic domain in complex with an extended inhibitor targeting the adaptive pocket of the enzyme (2008), Acta Crystallogr. Sect. F, 64, 686-691.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | Plk1 is a target for the development of anticancer therapeutics | Danio rerio |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| full-length zPlk1 cDNA and the zPlk1 kinase domain sequence, encompassing residues 17-312, are cloned, the expression plasmid pGEX6P-1 is used | Danio rerio |
Crystallization (Commentary)
| Crystallization (Comment) | Organism |
|---|---|
| the structure of zPlk1 KD in complex with the inhibitor is solved to 2.85 A resolution | Danio rerio |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| T196D | variant containing an activating substitution | Danio rerio |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 1-(5-methyl-2-trifluoro-methyl-furan-3-yl)-3-(5-[2-[6-(1H-[1,2,4]triazol-3-ylamino)-pyrimidin-4-ylamino]-ethyl]-thiazol-2-yl)urea | - |
Danio rerio |  |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 34390 | - |
expected molecular weight of the protein with the N-terminal Gly-Pro-Leu-Gly-Ser linker residues and a T196D substitution | Danio rerio |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + protein | Danio rerio | - |
ADP + phosphoprotein | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Danio rerio | Q4KMI8 | - |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
- |
Danio rerio |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + 5FAM-RALMEASFADQAR-NH2 | substrate peptide, based on human Cdc25C, used in biochemical activity assay | Danio rerio | ADP + phosphorylated 5FAM-RALMEASFADQAR-NH2 | - |
? | |
| ATP + protein | - |
Danio rerio | ADP + phosphoprotein | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Plk1 | - |
Danio rerio |
| Polo-like kinase 1 | - |
Danio rerio |
| zPlk1 | - |
Danio rerio |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.2 | - |
activity assay | Danio rerio |
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Release 2023.1 (January 2023)
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