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Literature summary for 2.7.11.21 extracted from

  • Nappi, T.C.; Salerno, P.; Zitzelsberger, H.; Carlomagno, F.; Salvatore, G.; Santoro, M.
    Identification of Polo-like kinase 1 as a potential therapeutic target in anaplastic thyroid carcinoma (2009), Cancer Res., 69, 1916-1923.
    View publication on PubMed

Application

Application Comment Organism
medicine PLK1 is a promising target for the molecular therapy of anaplastic thyroid carcinoma, ATC Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-((R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydro-pteridin-2-ylamino)-3-methoxy-N-(1-methyl-piperidin-4-yl)-benzamide BI 2536 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
8505C cell anaplastic thyroid carcinoma cell line Homo sapiens
-
ACT-1 cell anaplastic thyroid carcinoma cell line Homo sapiens
-
CAL-62 cell anaplastic thyroid carcinoma cell line Homo sapiens
-
OCUT-1 cell anaplastic thyroid carcinoma cell line Homo sapiens
-
SW-1736 cell anaplastic thyroid carcinoma cell line 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
-
Homo sapiens
Polo-like kinase 1
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
activity assay Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
activity assay Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000083
-
-
Homo sapiens 4-((R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydro-pteridin-2-ylamino)-3-methoxy-N-(1-methyl-piperidin-4-yl)-benzamide

Expression

Organism Comment Expression
Homo sapiens PLK1 is highly expressed in anaplastic thyroid carcinoma, ATC up

General Information

General Information Comment Organism
physiological function PLK1 is a key regulator of multiple steps during mitotic progression Homo sapiens