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Literature summary for 2.7.11.21 extracted from

  • Schmit, T.L.; Ledesma, M.C.; Ahmad, N.
    Modulating polo-like kinase 1 as a means for cancer chemoprevention (2010), Pharm. Res., 27, 989-998.
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
aurora A Plk1 activity is increased upon phosphorylation at threonine-210 by Aurora A in conjunction with Bora Mammalia
Bora Plk1 activity is increased upon phosphorylation at threonine-210 by Aurora A in conjunction with Bora Mammalia

Application

Application Comment Organism
medicine Plk1 may be a useful target for cancer chemoprevention Mammalia

Inhibitors

Inhibitors Comment Organism Structure
genistein decreases Plk1 expression Mammalia
indirubin decreases Plk1 expression Mammalia
morin enzymatic inhibitor Mammalia
purpurogallin polo box inhibitor Mammalia
quercetin enzymatic inhibitor Mammalia
scytonemin enzymatic inhibitor Mammalia
silibinin decreases Plk1 expression Mammalia
staurosporine enzymatic inhibitor Mammalia
thymoquinone polo box inhibitor Mammalia
trichostatin A decreases Plk1 expression Mammalia
Vanillin decreases Plk1 expression Mammalia
Wortmannin enzymatic inhibitor Mammalia

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Mammalia
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein
-
Mammalia

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
Plk1
-
Mammalia
Polo-like kinase 1
-
Mammalia

Cofactor

Cofactor Comment Organism Structure
ATP
-
Mammalia

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000024
-
-
Mammalia Wortmannin
0.0008
-
-
Mammalia staurosporine
0.002
-
-
Mammalia scytonemin
0.0126
-
-
Mammalia morin
0.064
-
-
Mammalia quercetin

Expression

Organism Comment Expression
Mammalia decline upon mitotic exit into G1 down
Mammalia Plk1 mRNA, protein and activity levels begin to rise in S-phase, peaking at the G2/M transition, over-expressed in a variety of cancers up

General Information

General Information Comment Organism
physiological function Plk1 plays several crucial roles in cell cycle progression and cell division Mammalia