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Literature summary for 2.7.11.21 extracted from

  • O'Connor, A.; Maffini, S.; Rainey, M.D.; Kaczmarczyk, A.; Gaboriau, D.; Musacchio, A.; Santocanale, C.
    Requirement for PLK1 kinase activity in the maintenance of a robust spindle assembly checkpoint (2015), Biol. Open, 5, 11-19.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
BI 6727 i.e. volasertib Homo sapiens
GW843682X potent inhibitor Homo sapiens
hesperadin almost complete inhibition Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
kinetochore
-
Homo sapiens 776
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + a protein Homo sapiens
-
ADP + a phosphoprotein
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P53350
-
-

Source Tissue

Source Tissue Comment Organism Textmining
U2-OS cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + a protein
-
Homo sapiens ADP + a phosphoprotein
-
?

Synonyms

Synonyms Comment Organism
PLK1 kinase
-
Homo sapiens
Polo-like kinase 1
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

General Information

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