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Literature summary extracted from

  • Elling, R.A.; Fucini, R.V.; Romanowski, M.J.
    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.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.11.21 medicine Plk1 is a target for the development of anticancer therapeutics Homo sapiens
2.7.11.21 medicine Plk1 is a target for the development of anticancer therapeutics Danio rerio

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.11.21 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
2.7.11.21 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)

EC Number Crystallization (Comment) Organism
2.7.11.21 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

EC Number Protein Variants Comment Organism
2.7.11.21 T196D variant containing an activating substitution Danio rerio
2.7.11.21 T210D variant containing an activating substitution Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.21 Wortmannin
-
 Danio rerio
2.7.11.21 Wortmannin
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.7.11.21 0.0055
-
 ATP apparent Km, hPlk1 1-346 T210D Homo sapiens
2.7.11.21 0.0064
-
 ATP apparent Km, zPlk1 1-312 T196D Danio rerio
2.7.11.21 0.0076
-
 ATP apparent Km, zPlk1 1-312 wild type Danio rerio

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.7.11.21 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
2.7.11.21 35930
-
 expected molecular weight of the protein with the additional T196D substitution Danio rerio
2.7.11.21 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
2.7.11.21 39060
-
 expected molecular weight of the protein with the additional T210D substitution Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.21 ATP + protein Homo sapiens
-
 ADP + phosphoprotein
-
 ?
2.7.11.21 ATP + protein Danio rerio
-
 ADP + phosphoprotein
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.21 Danio rerio Q6DRK7
-
-
2.7.11.21 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.11.21 using a glutathione-Sepharose and a Q-Sepharose column Homo sapiens
2.7.11.21 using a glutathione-Sepharose and a Q-Sepharose column Danio rerio

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.21 ATP + casein substrate in biochemical activity assay Homo sapiens ADP + phosphocasein
-
 ?
2.7.11.21 ATP + casein substrate in biochemical activity assay Danio rerio ADP + phosphocasein
-
 ?
2.7.11.21 ATP + protein
-
 Homo sapiens ADP + phosphoprotein
-
 ?
2.7.11.21 ATP + protein
-
 Danio rerio ADP + phosphoprotein
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.21 hPlk1
-
 Homo sapiens
2.7.11.21 Plk1
-
 Homo sapiens
2.7.11.21 Plk1
-
 Danio rerio
2.7.11.21 Polo-like kinase 1
-
 Homo sapiens
2.7.11.21 Polo-like kinase 1
-
 Danio rerio
2.7.11.21 zPlk1
-
 Danio rerio

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.7.11.21 0.00229
-
 ATP zPlk1 1-312 wild type Danio rerio
2.7.11.21 0.01311
-
 ATP zPlk1 1-312 T196D Danio rerio
2.7.11.21 0.01386
-
 ATP hPlk1 1-346 T210D Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.7.11.21 7.2
-
 activity assay Homo sapiens
2.7.11.21 7.2
-
 activity assay Danio rerio