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Literature summary for 2.7.1.153 extracted from

  • Fernandez-Acero, T.; Rodriguez-Escudero, I.; Vicente, F.; Monteiro, M.C.; Tormo, J.R.; Cantizani, J.; Molina, M.; Cid, V.J.
    A yeast-based in vivo bioassay to screen for class I phosphatidylinositol 3-kinase specific inhibitors (2012), J. Biomol. Screen., 17, 1018-1029.
    View publication on PubMed
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Application

Application Comment Organism
analysis low-cost bioassay that readily measures phosphatidylinositol 3-kinase inhibition. The in vivo assay is based on the fact that the overproduction of phosphatidylinositol 3-kinase is toxic in yeast, and uses the ability of commercial phosphatidylinositol 3-kinase inhibitors to rescue cell growth. The use of 0.003% sodium dodecyl sulfate and the elimination of the Snq2 detoxification pump, optimize the bioassay by enhancing its sensitivity. From 9600 extracts tested, 0.6% lead to a recovery of yeast growth reproducibly, selectively, and in a dose-dependent manner Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expression in Saccharomyces cerevisiae Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-[4-(morpholin-4-yl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol among the compounds tested, treatment with 3-[4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-2-yl]phenol or 3-[4-(morpholin-4-yl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol leads to the most efficient inhibition Homo sapiens
3-[4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-2-yl]phenol among the compounds tested, treatment with 3-[4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-2-yl]phenol or 3-[4-(morpholin-4-yl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol leads to the most efficient inhibition Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P42336 catalytic subunit alpha isoform
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