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Literature summary for 2.7.11.21 extracted from

  • Lenart, P.; Petronczki, M.; Steegmaier, M.; Di Fiore, B.; Lipp, J.J.; Hoffmann, M.; Rettig, W.J.; Kraut, N.; Peters, J.M.
    The small-molecule inhibitor BI 2536 reveals novel insights into mitotic roles of polo-like kinase 1 (2007), Curr. Biol., 17, 304-315.
    View publication on PubMed

Application

Application Comment Organism
additional information Plk1 has specific functions in Emi1 degradation, activation of Cdk1-cyclin B, cohesin release, centrosome function, and regulation of microtubule-kinetochore attachments, Plk1 is not required for prophase entry, but is required for timely entry into prometaphase Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
BI 2536 potent and selective inhibitor of Plk1, delays prophase and entrance into prometaphase, initiates cyclin A destruction without degrading Emi1, leads to spindle-assembly-checkpoint-induced prometaphase arrest, prevents Plk1’s enrichment at kinetochores and centrosomes, in metaphase cells induces detachment of microtubules from kinetochores and leads to spindle collapse, the inhibitor may serve as a powerful tool in mitosis research Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
centrosome
-
Homo sapiens 5813
-
centrosome Plk1’s accumulation depends on its own activity, activity is required for maintaining centrosome function Homo sapiens 5813
-
kinetochore
-
Homo sapiens 776
-
kinetochore Plk1’s accumulation depends on its own activity, activity is required for maintaining kinetochore function Homo sapiens 776
-
spindle
-
Homo sapiens 5819
-

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HeLa cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + Cdc25C
-
Homo sapiens ADP + phosphorylated Cdc25C
-
?
ATP + protein
-
Homo sapiens ADP + phosphoprotein
-
?

Synonyms

Synonyms Comment Organism
Plk1
-
Homo sapiens
Polo-like kinase 1
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000083
-
-
Homo sapiens BI 2536