Reactome | PI3K/mutant PI3K inhibitors [cytosol]

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PI3K/mutant PI3K inhibitors [cytosol] Show undefined attributes

compartment	[Compartment:70101] cytosol
componentOf	[Complex:R-HSA-2400008] PI3K Inhibitors:PI3K [cytosol] - Homo sapiens
consumedByEvent	[Reaction:R-HSA-2400009] PI3K inhibitors block PI3K catalytic activity - Homo sapiens
created	[InstanceEdit:2399727] Orlic-Milacic, M, 2012-07-12
crossReference	[DatabaseIdentifier:12020745] Mondo:0004992
dbId	2399811
disease	[Disease:1500689] cancer
displayName	PI3K/mutant PI3K inhibitors [cytosol]
hasCandidate	[ChemicalDrug:R-ALL-2399768] GSK1059615 [cytosol]
hasMember	[ChemicalDrug:R-ALL-2399744] BEZ235 [cytosol] [ChemicalDrug:R-ALL-2399772] BGT226 [cytosol] [ChemicalDrug:R-ALL-2399771] BKM120 [cytosol] [ChemicalDrug:R-ALL-2399863] XL765 [cytosol] [ChemicalDrug:R-ALL-2399886] XL147 [cytosol] [ChemicalDrug:R-ALL-2399804] GDC0941 [cytosol] [ChemicalDrug:R-ALL-2399860] PX-866 [cytosol] [ChemicalDrug:R-ALL-2399739] LY294002 [cytosol] [ChemicalDrug:R-ALL-2399848] wortmannin [cytosol]
inDisease	true
literatureReference	[LiteratureReference:2399890] NVP-BEZ235, a dual PI3K/mTOR inhibitor, prevents PI3K signaling and inhibits the growth of cancer cells with activating PI3K mutations [LiteratureReference:2399826] Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity [LiteratureReference:2399837] Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo [LiteratureReference:2399821] Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor [LiteratureReference:2399754] Inhibition of PI3K/mTOR pathways in glioblastoma and implications for combination therapy with temozolomide [LiteratureReference:2399733] Feedback upregulation of HER3 (ErbB3) expression and activity attenuates antitumor effect of PI3K inhibitors [LiteratureReference:2399831] The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer [LiteratureReference:1358728] Ligand-independent HER2/HER3/PI3K complex is disrupted by trastuzumab and is effectively inhibited by the PI3K inhibitor GDC-0941 [LiteratureReference:2399870] Targeting the phosphoinositide 3-kinase pathway in cancer [LiteratureReference:2399785] Wortmannin inactivates phosphoinositide 3-kinase by covalent modification of Lys-802, a residue involved in the phosphate transfer reaction
maxDepth	2
modified	[InstanceEdit:9732444] Stephan, Ralf, 2021-05-27
name	PI3K/mutant PI3K inhibitors
schemaClass	CandidateSet
stId	R-ALL-2399811
summation	[Summation:2404236] PI3K inhibitors bind the catalytic subunit of PIK3CA, blocki...
updateTrackers	[UpdateTracker:9902491] Update Tracker - [CandidateSet:2399811] PI3K/mutant PI3K inhibitors [cytosol] - v78:[modifyName]

Referrals

(updatedInstance)	[UpdateTracker:9902491] Update Tracker - [CandidateSet:2399811] PI3K/mutant PI3K inhibitors [cytosol] - v78:[modifyName]
(hasComponent)	[Complex:R-HSA-2400008] PI3K Inhibitors:PI3K [cytosol]
(input)	[Reaction:R-HSA-2400009] PI3K inhibitors block PI3K catalytic activity

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