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Literature summary for 2.7.1.153 extracted from

  • Park, S.; Chapuis, N.; Bardet, V.; Tamburini, J.; Gallay, N.; Willems, L.; Knight, Z.A.; Shokat, K.M.; Azar, N.; Viguie, F.; Ifrah, N.; Dreyfus, F.; Mayeux, P.; Lacombe, C.; Bouscary, D.
    PI-103, a dual inhibitor of class IA phosphatidylinositide 3-kinase and mTOR, has antileukemic activity in AML (2008), Leukemia, 22, 1698-1706.
    View publication on PubMed

Application

Application Comment Organism
medicine in human leukemic cell lines and in primary blast cells from acute myelogenous leukemia patients, inhibitor 4-[4-(morpholin-4-yl)-5a,6-dihydro[1]benzofuro[3,2-d]pyrimidin-2-yl]phenol/PI-103 inhibits constitutive and growth factor-induced PI3K/Akt and mTORC1 activation. PI-103 is essentially cytostatic for cell lines and induces cell cycle arrest in the G1 phase. In blast cells, PI-103 inhibits leukemic proliferation, the clonogenicity of leukemic progenitors and induces mitochondrial apoptosis. PI-103 has additive proapoptotic effects with etoposide in blast cells and in immature leukemic cells. PI-103 does not induce apoptosis in normal CD34รพ cells and has moderate effects on their clonogenic and proliferative properties Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-[4-(morpholin-4-yl)-5a,6-dihydro[1]benzofuro[3,2-d]pyrimidin-2-yl]phenol i.e. PI-103. In human leukemic cell lines and in primary blast cells from acute myelogenous leukemia patients, PI-103 inhibits constitutive and growth factor-induced PI3K/Akt and mTORC1 activation. PI-103 is essentially cytostatic for cell lines and induces cell cycle arrest in the G1 phase. In blast cells, PI-103 inhibits leukemic proliferation, the clonogenicity of leukemic progenitors and induces mitochondrial apoptosis. PI-103 has additive proapoptotic effects with etoposide in blast cells and in immature leukemic cells. PI-103 does not induce apoptosis in normal CD34รพ cells and has moderate effects on their clonogenic and proliferative properties Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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patients with acute myelogenous leukemia
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