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Literature summary for 2.7.11.21 extracted from

  • Mita, Y.; Noguchi-Yachide, T.; Ishikawa, M.; Hashimoto, Y.
    Small-molecular, non-peptide, non-ATP-competitive polo-like kinase 1 (Plk1) inhibitors with a terphenyl skeleton (2013), Bioorg. Med. Chem., 21, 608-617.
    View publication on PubMed
Search for more literature for 2.7.11.21

Application

Application Comment Organism
medicine overexpression of Plk1 is strongly correlated with aggressiveness and prognosis of many cancers, so Plk1 is a potential target for anticancer therapy Homo sapiens

Protein Variants

Protein Variants Comment Organism
additional information human full-length Plk1 with the mutation T210D in the active-site loop of kinase domain Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2'-(2-hydroxyethoxy)-5'-methyl-(1,1':3',1''-terphenyl)-4,4''-dinitrile 0.3 mM, 11% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain Homo sapiens
2'-(2-hydroxyethoxy)-5'-methyl-(1,1':3':1''-terphenyl)-4''-(1H-tetrazol-5-yl)-4-nitrile 0.3 mM, 66% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain Homo sapiens
2'-(2-hydroxyethoxy)-5'-methyl-[1,1':3',1''-terphenyl]-3,3'',5,5''-tetrafluoro-4,4''-diol 0.3 mM, 61% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain Homo sapiens
2'-(2-hydroxyethoxy)-5'-methyl-[1,1':3',1''-terphenyl]-4,4''-diacetic acid 0.3 mM, 53% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain Homo sapiens
2'-(2-hydroxyethoxy)-5'-methyl-[1,1':3',1''-terphenyl]-4,4''-dicarboxylic acid 0.3 mM, 14% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain Homo sapiens
2'-(2-hydroxyethoxy)-5'-methyl-[1,1':3',1''-terphenyl]-4,4''-dipropionic acid 0.3 mM, 26% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain Homo sapiens
2'-hydroxy-5'-methyl-[1,1':3',1''-terphenyl]-4,4''-dicarboxylic acid 0.3 mM, 36% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain Homo sapiens
2-[5'-methyl-4,4''-ditetrazol-5-yl-(1,1':3',1''-terphenyl)-2'-oxy]ethanol 0.3 mM, 47% inhibition, full-length enzyme Plk1 with the mutation T210D in the active-site loop of kinase domain Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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Synonyms

Synonyms Comment Organism
polo-like kinase
-
 Homo sapiens

General Information

General Information Comment Organism
physiological function the enzyme plays a critical role in cell division Homo sapiens