Any feedback?
Literature summary for 2.7.11.21 extracted from
- Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity (2007), Biochemistry, 46, 9551-9563.
Application
| Application | Comment | Organism |
|---|---|---|
| additional information | with respect to both substrate and ATP-site specificity, highest similarity is between PLK2 and PLK3, PLK1 is next most similar, and PLK4 is least similar | Homo sapiens |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| GST-tagged PLK1 (1-331) expressed in SF9 cells | Homo sapiens |
| His-tagged PLK4 (1-269) expressed in Escherichia coli | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2-ol | selectivity profile of PLK2/4 over PLK1/3 | Homo sapiens |  |
| AG-013736 | selective inhibition of PLK4 relative to PLK1-3 | Homo sapiens | |
| BAY 439006 | selective inhibition of PLK4 relative to PLK1-3 | Homo sapiens | |
| BI 2536 | time-dependent inhibition; time-dependent inhibition; time-dependent inhibition of PLK1 | Homo sapiens | |
| CHIR-258 | selectivity profile of PLK2/4 over PLK1/3; selectivity profile of PLK2/4 over PLK1/3 | Homo sapiens | |
| CP 547632 | selective inhibition of PLK4 relative to PLK1-3 | Homo sapiens | |
| GO 6976 | loses PLK1 activity by at least an order of magnitude, relative to staurosporine; loses PLK2 activity by at least an order of magnitude, relative to staurosporine; loses PLK3 activity by at least an order of magnitude, relative to staurosporine | Homo sapiens | |
| H-1152 | selective inhibition of PLK4 relative to PLK1-3 | Homo sapiens | |
| imatinib | selective inhibition of PLK4 relative to PLK1-3 | Homo sapiens | |
| LY294002 | selective inhibition of PLK4 relative to PLK1-3 | Homo sapiens | |
| additional information | GO 6976 retains PLK4 activity | Homo sapiens | |
| PP1 | - |
Homo sapiens | |
| staurosporine | specific for PLK4 | Homo sapiens | |
| SU11248 | selective inhibition of PLK4 relative to PLK1-3 | Homo sapiens | |
| VX-680 | selective inhibition of PLK4 relative to PLK1-3 | Homo sapiens | |
| Wortmannin | time-dependent irreversible inhibition with PLK1 | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0002 | - |
ATP | - |
Homo sapiens | |
| 0.0008 | - |
ATP | - |
Homo sapiens | |
| 0.001 | - |
ATP | - |
Homo sapiens | |
| 0.002 | - |
ATP | PLK2 | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | O00444 | - |
- |
| Homo sapiens | P53350 | - |
- |
| Homo sapiens | Q9H4B4 | - |
- |
| Homo sapiens | Q9NYY3 | - |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| affinity purified | Homo sapiens |
| on Ni2+ resin | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + Cdc25C | preferentially phosphorylates Ser 198 and 191 | Homo sapiens | ADP + phosphorylated Cdc25C | - |
? | |
| ATP + cJun peptide | strong preference of PLK1 versus PLK2 and PLK3 | Homo sapiens | ADP + phosphorylated cJun peptide | - |
? | |
| ATP + PLKtide | substrate corresponds to the consensus sequence for positions -7 to +6 supplemented with residues from Cdc25C for positions -23 to -8. PLK1 displays greatly enhanced activity and a strong preference for the residue corresponding to Ser198 in the optimized substrate | Homo sapiens | ADP + phosphorylated PLKtide | - |
? | |
| ATP + PLKtide | substrate corresponds to the consensus sequence for positions -7 to +6 supplemented with residues from Cdc25C for positions -23 to -8. PLK2 displays greatly enhanced activity and a strong preference for the residue corresponding to Ser198 in the optimized substrate | Homo sapiens | ADP + phosphorylated PLKtide | - |
? | |
| ATP + PLKtide | substrate corresponds to the consensus sequence for positions -7 to +6 supplemented with residues from Cdc25C for positions -23 to -8. PLK3 displays greatly enhanced activity and a strong preference for the residue corresponding to Ser198 in the optimized substrate | Homo sapiens | ADP + phosphorylated PLKtide | - |
? | |
| ATP + TPSDSLIYDDGLS | - |
Homo sapiens | ADP + phosphorylated TPSDSLIYDDGLS | - |
? | |
| additional information | consensus substrate sequences for PLK2 | Homo sapiens | ? | - |
? | |
| additional information | consensus substrate sequences for PLK3 | Homo sapiens | ? | - |
? | |
| additional information | consensus substrate sequences for PLK4 | Homo sapiens | ? | - |
? | |
| additional information | expanded consensus substrate sequence for PLK1 | Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Plk1 | - |
Homo sapiens |
| Plk2 | - |
Homo sapiens |
| Plk3 | - |
Homo sapiens |
| PLK4 | - |
Homo sapiens |
| Polo-like kinase 1 | - |
Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.000001 | - |
BI 2536 | time-dependent inhibition | Homo sapiens | |
| 0.0000026 | - |
staurosporine | - |
Homo sapiens | |
| 0.0000034 | - |
GO 6976 | - |
Homo sapiens | |
| 0.0000042 | - |
AG-013736 | - |
Homo sapiens | |
| 0.000011 | - |
N-[4-({4-[(Z)-(5-methyl-1,2-dihydro-3H-pyrazol-3-ylidene)amino]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl}sulfanyl)phenyl]cyclopropanecarboxamide | - |
Homo sapiens | |
| 0.00012 | - |
CP 547632 | - |
Homo sapiens | |
| 0.00012 | - |
H-1152 | - |
Homo sapiens | |
| 0.00015 | - |
staurosporine | - |
Homo sapiens | |
| 0.00024 | - |
BAY 439006 | - |
Homo sapiens | |
| 0.0003 | - |
SU11248 | - |
Homo sapiens | |
| 0.00079 | - |
staurosporine | - |
Homo sapiens | |
| 0.00079 | - |
PP1 | - |
Homo sapiens | |
| 0.00085 | - |
4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2-ol | - |
Homo sapiens | |
| 0.0012 | - |
staurosporine | - |
Homo sapiens | |
| 0.0014 | - |
CHIR-258 | - |
Homo sapiens | |
| 0.0015 | - |
Wortmannin | time-dependent irreversible inhibition | Homo sapiens | |
| 0.0022 | - |
imatinib | - |
Homo sapiens | |
| 0.0028 | - |
Wortmannin | - |
Homo sapiens | |
| 0.003 | - |
Wortmannin | - |
Homo sapiens | |
| 0.0061 | - |
LY294002 | - |
Homo sapiens | |
| 0.0075 | - |
LY294002 | - |
Homo sapiens | |
| 0.008 | - |
GO 6976 | - |
Homo sapiens | |
| 0.0093 | - |
SU11248 | - |
Homo sapiens | |
| 0.016 | - |
LY294002 | - |
Homo sapiens | |
| 0.016 | - |
GO 6976 | - |
Homo sapiens | |
| 0.018 | - |
imatinib | - |
Homo sapiens | |
| 0.019 | - |
GO 6976 | - |
Homo sapiens | |
| 0.02 | - |
Wortmannin | - |
Homo sapiens | |
| 0.02 | - |
LY294002 | - |
Homo sapiens | |
| 0.02 | - |
imatinib | - |
Homo sapiens | |
| 0.02 | - |
BI 2536 | - |
Homo sapiens | |
| 0.02 | - |
PP1 | - |
Homo sapiens | |
| 0.02 | - |
SU11248 | - |
Homo sapiens | |
| 0.02 | - |
BAY 439006 | - |
Homo sapiens | |
| 0.02 | - |
CP 547632 | - |
Homo sapiens | |
| 0.02 | - |
H-1152 | - |
Homo sapiens | |
| 0.02 | - |
VX-680 | - |
Homo sapiens | |
| 0.02 | - |
AG-013736 | - |
Homo sapiens | |
| 0.02 | - |
CHIR-258 | - |
Homo sapiens | |
| 0.02 | - |
N-methyl-2-({3-[(E)-2-(pyridin-2-yl)ethenyl]-2H-indazol-6-yl}sulfanyl)benzenecarboximidic acid | - |
Homo sapiens | |
| 0.03 | - |
BAY 439006 | - |
Homo sapiens | |
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
Legal
Curated at
Member of
