Inhibitors | Comment | Organism | Structure |
---|---|---|---|
BI 6727 | i.e. volasertib | Homo sapiens | |
GW843682X | potent inhibitor | Homo sapiens | |
hesperadin | almost complete inhibition | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
kinetochore | - |
Homo sapiens | 776 | - |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | required | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + a protein | Homo sapiens | - |
ADP + a phosphoprotein | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P53350 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
U2-OS cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + a protein | - |
Homo sapiens | ADP + a phosphoprotein | - |
? |
Synonyms | Comment | Organism |
---|---|---|
PLK1 kinase | - |
Homo sapiens |
Polo-like kinase 1 | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
General Information | Comment | Organism |
---|---|---|
malfunction | upon PLK1 inhibition, phosphorylated histone H3 on Thr 3, a marker of Haspin activity, is reduced. PLK1 inhibition, together with partial inhibition of Aurora B, allows efficient spindle assembly checkpoint override to occur. This phenotype is more pronounced than the phenotype observed by combining the same PLK1 inhibitors with partial MPS1 inhibition. PLK1 inhibition does not obviously cooperate with Haspin inhibition to promote spindle assembly checkpoint override. Effects of the PLK1 inhibitors together with partial inhibition of the three major checkpoint kinases Aurora B, MPS1 and Haspin in maintaining the strength of the nocodazole induced mitotic arrest, overview | Homo sapiens |
physiological function | Polo-like kinase 1 (PLK1) plays many roles leading to cell division including promoting entry into, progression through and exit from mitosis. It regulates bipolar spindle formation, centrosome function and k-MT attachment in human cells. PLK1 kinase activity is required in the maintenance of a robust spindle assembly checkpoint. PLK1 kinase plays a major role in mitosis. In nocodazole-arrested U2OS cells, PLK1 activity is continuously required for maintaining Aurora B protein localisation and activity at kinetochores (Aurora B is required for the recruitment of outer kinetochore proteins). Aurora B inhibition causes PLK1 to relocalise from kinetochores into fewer and much larger foci, possibly due to incomplete recruitment of outer kinetochore proteins. PLK1 is directly involved in maintaining efficient spindle assembly checkpoint signalling, possibly by cooperating in a positive feedback loop with Aurora B, and that partially redundant mechanisms exist which reinforce the spindle assembly checkpoint. PLK1 activity appears to be required for continuous maintenance of levels of histone H3 phosphorylated at Thr3 and its accumulation at kinetochores. Upon disruption of microtubules in U2-OS cells PLK1 functions to cooperate with Aurora B to maintain a mitotic cell cycle arrest | Homo sapiens |