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Details on Person PI3K inhibitors block PI3K catalytic activity

Class:Id	Reaction:2400009
_displayName	PI3K inhibitors block PI3K catalytic activity
_doRelease	TRUE
_timestamp	2021-05-27 12:54:59
authored	[InstanceEdit:2422427] Orlic-Milacic, M, 2012-07-18
compartment	[Compartment:70101] cytosol [Compartment:876] plasma membrane [Compartment:984] extracellular region
created	[InstanceEdit:2400005] Orlic-Milacic, M, 2012-07-13
disease	[Disease:1500689] cancer
edited	[InstanceEdit:2426555] Matthews, L, 2012-08-03
input	[CandidateSet:2400011] PI3K mutants,Activator:PI3K [plasma membrane] [Homo sapiens] [CandidateSet:2399811] PI3K/mutant PI3K inhibitors [cytosol]
isChimeric	FALSE
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:2399821] Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor [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: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:2399785] Wortmannin inactivates phosphoinositide 3-kinase by covalent modification of Lys-802, a residue involved in the phosphate transfer reaction [LiteratureReference:2399870] Targeting the phosphoinositide 3-kinase pathway in cancer [LiteratureReference:2459950] A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling [LiteratureReference:2459949] A drug targeting only p110? can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types [LiteratureReference:2399685] Cancer-derived mutations in the regulatory subunit p85alpha of phosphoinositide 3-kinase function through the catalytic subunit p110alpha [LiteratureReference:2459963] The p110? and p110? isoforms of PI3K play divergent roles in mammary gland development and tumorigenesis [LiteratureReference:2459988] PI 3-kinase p110beta: a new target for antithrombotic therapy [LiteratureReference:2460012] Functional characterization of an isoform-selective inhibitor of PI3K-p110? as a potential anticancer agent [LiteratureReference:2460069] Phosphatidylinositol 3-kinase-? inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals
modified	[InstanceEdit:2404246] Orlic-Milacic, M, 2012-07-16 [InstanceEdit:2428913] Orlic-Milacic, M, 2012-08-08 [InstanceEdit:2457746] Orlic-Milacic, M, 2012-08-28 [InstanceEdit:2459978] Orlic-Milacic, M, 2012-08-29 [InstanceEdit:2460019] Orlic-Milacic, M, 2012-08-29 [InstanceEdit:2460082] Orlic-Milacic, M, 2012-08-30 [InstanceEdit:2463861] Orlic-Milacic, M, 2012-08-30 [InstanceEdit:3080613] Orlic-Milacic, M, 2013-02-07 [InstanceEdit:9732444] Stephan, Ralf, 2021-05-27 [InstanceEdit:9830342] Matthews, Lisa, 2023-03-08
name	PI3K inhibitors block PI3K catalytic activity
output	[Complex:2400008] PI3K Inhibitors:PI3K [cytosol] [Homo sapiens]
releaseDate	2012-09-18
reviewed	[InstanceEdit:2463860] Thorpe, Lauren, 2012-08-13 [InstanceEdit:2463859] Yuzugullu, Haluk, 2012-08-13 [InstanceEdit:2463854] Zhao, Jean J, 2012-08-13
reviewStatus	[ReviewStatus:9821382] five stars
species	[Species:48887] Homo sapiens
stableIdentifier	[StableIdentifier:2464986] R-HSA-2400009.3
summation	[Summation:2404213] A variety of inhibitors capable of blocking the phosphoinosi...
(hasEvent)	[Pathway:2219530] Constitutive Signaling by Aberrant PI3K in Cancer [Homo sapiens] [Pathway:2632528] Constitutive Signaling by PI3K Mutants [Homo sapiens]
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No pathways have been reviewed or authored by PI3K inhibitors block PI3K catalytic activity (2400009)