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EC Tree
IUBMB Comments The enzyme associates with the spindle pole during mitosis and is thought to play an important role in the dynamic function of the mitotic spindle during chromosome segregation. The human form of the enzyme, Plk1, does not phosphorylate histone H1, enolase and phosvitin but it can phosphorylate myelin basic protein and microtubule-associated protein MAP-2, although to a lesser extent than casein .
The taxonomic range for the selected organisms is: Danio rerio The enzyme appears in selected viruses and cellular organisms
Reaction Schemes
+
a [protein]-(L-serine/L-threonine)
=
+
a [protein]-(L-serine/L-threonine) phosphate
Synonyms
polo-like kinase 1, polo-like kinase, plk-1, polo kinase, polo-like kinase 4, polo-like kinase-1, tbplk, plk1 kinase, cdc5p, polo-like kinase 2,
more
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FGF-inducible kinase
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Proliferation-related kinase
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Plk1
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Polo-like kinase 1
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zPlk1
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phospho group transfer
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ATP:protein phosphotransferase (spindle-pole-dependent)
The enzyme associates with the spindle pole during mitosis and is thought to play an important role in the dynamic function of the mitotic spindle during chromosome segregation. The human form of the enzyme, Plk1, does not phosphorylate histone H1, enolase and phosvitin but it can phosphorylate myelin basic protein and microtubule-associated protein MAP-2, although to a lesser extent than casein [2].
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ATP + 5FAM-RALMEASFADQAR-NH2
ADP + phosphorylated 5FAM-RALMEASFADQAR-NH2
substrate peptide, based on human Cdc25C, used in biochemical activity assay
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-
?
ATP + casein
ADP + phosphocasein
substrate in biochemical activity assay
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-
?
ATP + protein
ADP + phosphoprotein
ATP + protein
ADP + phosphoprotein
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?
ATP + protein
ADP + phosphoprotein
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?
ATP + protein
ADP + phosphoprotein
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?
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ATP + protein
ADP + phosphoprotein
ATP + protein
ADP + phosphoprotein
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?
ATP + protein
ADP + phosphoprotein
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?
ATP + protein
ADP + phosphoprotein
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?
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1-(2-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
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1-(2-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
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1-(3,5-dichlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
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1-(3,5-dimethylphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
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1-(3-bromo-5-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
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1-(3-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
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1-(3-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
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1-(3-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
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1-(4-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
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1-(4-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
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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
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1-[3-(3-aminopropyl)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
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1-[3-(dimethylamino)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
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3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)benzonitrile
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3-methyl-1-(2-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
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3-methyl-1-(3-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
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3-methyl-1-(4-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
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3-methyl-1-phenyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
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3-methyl-1-[3-(1-methylethyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
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3-methyl-1-[3-(methylsulfonyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
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3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanamide
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3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanoic acid
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N-(2-hydroxyethyl)-3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanamide
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N-[2-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]-2-phenylacetamide
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0.0064
ATP
apparent Km, zPlk1 1-312 T196D
0.0076
ATP
apparent Km, zPlk1 1-312 wild type
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0.00229
ATP
zPlk1 1-312 wild type
0.01311
ATP
zPlk1 1-312 T196D
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0.004516
1-(2-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
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0.01445
1-(2-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
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-
0.000641
1-(3,5-dichlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
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-
0.000149
1-(3,5-dimethylphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
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-
0.000274
1-(3-bromo-5-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
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0.000121
1-(3-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
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0.000464
1-(3-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
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0.005928
1-(3-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
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0.003241
1-(4-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
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0.000703
1-(4-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
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0.000059
1-[3-(3-aminopropyl)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
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0.000977
1-[3-(dimethylamino)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
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0.000412
3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)benzonitrile
Danio rerio
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0.007685
3-methyl-1-(2-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
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0.000474
3-methyl-1-(3-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
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0.004528
3-methyl-1-(4-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
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0.001301
3-methyl-1-phenyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
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0.001476
3-methyl-1-[3-(1-methylethyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
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0.000225
3-methyl-1-[3-(methylsulfonyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
Danio rerio
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0.000032
3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanamide
Danio rerio
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-
0.000021
3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanoic acid
Danio rerio
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-
0.000048
N-(2-hydroxyethyl)-3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanamide
Danio rerio
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0.000207
N-[2-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]-2-phenylacetamide
Danio rerio
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-
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7.2
activity assay
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UniProt
brenda
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UniProt
brenda
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brenda
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PLK4_DANRE
940
0
103485
Swiss-Prot
other Location (Reliability: 2 )
F1RB74_DANRE
941
0
103603
TrEMBL
other Location (Reliability: 2 )
A0A8M1NG63_DANRE
941
0
103603
TrEMBL
other Location (Reliability: 2 )
Q7ZVM4_DANRE
644
0
72589
TrEMBL
other Location (Reliability: 5 )
D9IWE5_DANRE
644
0
72536
TrEMBL
other Location (Reliability: 5 )
Q6DRK7_DANRE
595
0
67760
TrEMBL
other Location (Reliability: 2 )
B0S6K2_DANRE
660
0
74319
TrEMBL
other Location (Reliability: 3 )
D9IWE4_DANRE
657
0
74450
TrEMBL
other Location (Reliability: 1 )
A8WHV5_DANRE
657
0
74464
TrEMBL
other Location (Reliability: 1 )
Q4KMI8_DANRE
595
0
67761
TrEMBL
other Location (Reliability: 2 )
A6H8T5_DANRE
657
0
74438
TrEMBL
other Location (Reliability: 1 )
E7EXD4_DANRE
670
0
76334
TrEMBL
other Location (Reliability: 3 )
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34390
expected molecular weight of the protein with the N-terminal Gly-Pro-Leu-Gly-Ser linker residues and a T196D substitution
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
35930
expected molecular weight of the protein with the additional T196D substitution
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the structure of zPlk1 KD in complex with the inhibitor is solved to 2.85 A resolution
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
zPlk1 is crystallized in complex with compound38
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T196D
variant containing an activating substitution
T196D
variant containing an activating substitution
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using a glutathione-Sepharose and a Q-Sepharose column
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full-length zPlk1 cDNA and the zPlk1 kinase domain sequence, encompassing residues 17-312, are cloned, the expression plasmid pGEX6P-1 is used
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
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medicine
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Plk1 is a target for the development of anticancer therapeutics
medicine
Plk1 is a target for the development of anticancer therapeutics
medicine
Plk1 is a target for the development of anticancer therapeutics
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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
Acta Crystallogr. Sect. D
64
909-918
2008
Homo sapiens, Danio rerio (Q6DRK7), Danio rerio
brenda
Elling, R.A.; Fucini, R.V.; Hanan, E.J.; Barr, K.J.; Zhu, J.; Paulvannan, K.; Yang, W.; Romanowski, M.J.
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
Acta Crystallogr. Sect. F
64
686-691
2008
Danio rerio (Q4KMI8), Danio rerio
brenda
Fucini, R.V.; Hanan, E.J.; Romanowski, M.J.; Elling, R.A.; Lew, W.; Barr, K.J.; Zhu, J.; Yoburn, J.C.; Liu, Y.; Fahr, B.T.; Fan, J.; Lu, Y.; Pham, P.; Choong, I.C.; VanderPorten, E.C.; Bui, M.; Purkey, H.E.; Evanchik, M.J.; Yang, W.
Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors
Bioorg. Med. Chem. Lett.
18
5648-5652
2008
Danio rerio
brenda