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Literature summary for 2.7.1.153 extracted from

  • Chiarini, F.; Fala, F.; Tazzari, P.L.; Ricci, F.; Astolfi, A.; Pession, A.; Pagliaro, P.; McCubrey, J.A.; Martelli, A.M.
    Dual inhibition of class IA phosphatidylinositol 3-kinase and mammalian target of rapamycin as a new therapeutic option for T-cell acute lymphoblastic leukemia (2009), Cancer Res., 69, 3520-3528.
    View publication on PubMedView publication on EuropePMC
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Application

Application Comment Organism
medicine application of PI3K/Akt/mTOR inhibitors in T-cell acute lymphoblastic leukemia, T-ALL Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-[4-(4-morpholinyl)thieno(3,2-d)pyrimidin-2-yl]-phenol a p110 PI3K isoform selective inhibitor Homo sapiens
5-[2,2-difluoro-benzo(1,3)-dioxol-5-ylmethylene]-thiazolidine-2,4-dione a p110 PI3K isoform selective inhibitor Homo sapiens
LY294002
-
 Homo sapiens
PI-103 a dual PI3K/mTOR inhibitor and a small synthetic molecule of the pyridofuropyrimidine class. PI-103 induces caspase activation and is cytotoxic to all T-cell acute lymphoblastic leukemia cell lines affecting PI3K/Akt/mTOR signaling, mechanism, overview Homo sapiens
TGX-221 a p110 PI3K isoform selective inhibitor Homo sapiens
Wortmannin
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens PI3K generates phosphatidylinositol 3,4,5 trisphosphate ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
CCRF-CEM cell CEM-S cell Homo sapiens
-
CCRF-CEM cell CEM-R cell Homo sapiens
-
JURKAT cell
-
 Homo sapiens
-
MOLT-4 cell
-
 Homo sapiens
-
T-cell acute lymphoblastic leukemia cell all cell lines express the catalytic subunit isoforms p110alpha, p110beta, p110gamma, and p110delta Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information PI3K generates phosphatidylinositol 3,4,5 trisphosphate Homo sapiens ?
-
 ?

Subunits

Subunits Comment Organism
heterodimer PI3K is formed by a catalytic subunit p110, occuring in four isoforms p110alpha, p110beta, p110gamma, and p110delta, and a regulatory subunit p85 Homo sapiens

Synonyms

Synonyms Comment Organism
PI3K
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00004
-
 about, versus p110beta PI3K Homo sapiens TGX-221
0.00025
-
 about, versus p110gamma PI3K Homo sapiens 5-[2,2-difluoro-benzo(1,3)-dioxol-5-ylmethylene]-thiazolidine-2,4-dione
0.00058
-
 versus p110alpha PI3K Homo sapiens 3-[4-(4-morpholinyl)thieno(3,2-d)pyrimidin-2-yl]-phenol

General Information

General Information Comment Organism
malfunction constitutively activated phosphatidylinositol 3-kinase/Akt/mammalian target of rapamycin, mTOR, signaling is a common feature of T-cell acute lymphoblastic leukemia, where it strongly influences growth and survival Homo sapiens
metabolism PI3K/Akt/mTOR signaling, overview Homo sapiens
physiological function p110 isoforms alpha, beta, and gamma PI3K are involved in T-cell acute lymphoblastic leukemia cell survival, but not p110delta PI3K Homo sapiens