BYL719, a selective inhibitor of phosphoinositide 3-Kinase α, enhances the effect of selumetinib (AZD6244, ARRY-142886) in KRAS-mutant non-small cell lung cancer

scientific article

BYL719, a selective inhibitor of phosphoinositide 3-Kinase α, enhances the effect of selumetinib (AZD6244, ARRY-142886) in KRAS-mutant non-small cell lung cancer is …
instance of (P31):
scholarly articleQ13442814

External links are
P6179Dimensions Publication ID1016933503
P356DOI10.1007/S10637-014-0163-9
P698PubMed publication ID25342139

P2093author name stringKeunchil Park
Myung-Ju Ahn
Jin Seok Ahn
Jong-Mu Sun
Eun Hye Jho
Bo Mi Ku
Yeon-Hee Bae
P2860cites work14-3-3 Inhibits Bad-Induced Cell Death through Interaction with Serine-136Q24291932
Synthetic lethal interaction of combined BCL-XL and MEK inhibition promotes tumor regressions in KRAS mutant cancer modelsQ24306326
PI3K inhibition results in enhanced HER signaling and acquired ERK dependency in HER2-overexpressing breast cancerQ24338724
The role of RAS oncogene in survival of patients with lung cancer: a systematic review of the literature with meta-analysisQ24650902
Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluationQ27684731
MEK1 mutations confer resistance to MEK and B-RAF inhibitionQ27777362
Phase I pharmacokinetic and pharmacodynamic study of the oral, small-molecule mitogen-activated protein kinase kinase 1/2 inhibitor AZD6244 (ARRY-142886) in patients with advanced cancersQ27851426
In vivo activity of combined PI3K/mTOR and MEK inhibition in a Kras(G12D);Pten deletion mouse model of ovarian cancerQ45842339
A Phase II, open-label, randomised study to assess the efficacy and safety of the MEK1/2 inhibitor AZD6244 (ARRY-142886) versus capecitabine monotherapy in patients with colorectal cancer who have failed one or two prior chemotherapeutic regimensQ82758717
Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancersQ27851457
Selumetinib plus docetaxel for KRAS-mutant advanced non-small-cell lung cancer: a randomised, multicentre, placebo-controlled, phase 2 studyQ27851971
Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trialsQ27852946
Intrinsic resistance to MEK inhibition in KRAS mutant lung and colon cancer through transcriptional induction of ERBB3.Q27852991
14-3-3 proteins and survival kinases cooperate to inactivate BAD by BH3 domain phosphorylationQ28144100
Regulation of bad phosphorylation and association with Bcl-x(L) by the MAPK/Erk kinaseQ28145921
KRAS mutations in non-small cell lung cancerQ28240568
RAS oncogenes: weaving a tumorigenic webQ28250360
Serine phosphorylation of death agonist BAD in response to survival factor results in binding to 14-3-3 not BCL-X(L)Q28297419
Combination Treatment with MEK and AKT Inhibitors Is More Effective than Each Drug Alone in Human Non-Small Cell Lung Cancer In Vitro and In VivoQ28476362
Apoptosis Induction by MEK Inhibition in Human Lung Cancer Cells Is Mediated by BimQ28749134
Advances in targeting the Ras/Raf/MEK/Erk mitogen-activated protein kinase cascade with MEK inhibitors for cancer therapyQ33316645
High level of AKT activity is associated with resistance to MEK inhibitor AZD6244 (ARRY-142886)Q33717222
RAS Interaction with PI3K: More Than Just Another Effector PathwayQ34202692
Intrinsic resistance to selumetinib, a selective inhibitor of MEK1/2, by cAMP-dependent protein kinase A activation in human lung and colorectal cancer cellsQ34273541
Ras family signaling: therapeutic targetingQ35087208
The BAD protein integrates survival signaling by EGFR/MAPK and PI3K/Akt kinase pathways in PTEN-deficient tumor cellsQ35469548
Rapamycin induces Bad phosphorylation in association with its resistance to human lung cancer cellsQ35667143
4E-BP1 is a key effector of the oncogenic activation of the AKT and ERK signaling pathways that integrates their function in tumorsQ35778060
STAT3 Mediates Resistance to MEK Inhibitor through MicroRNA miR-17Q36083385
Treatment of B-RAF mutant human tumor cells with a MEK inhibitor requires Bim and is enhanced by a BH3 mimeticQ36945203
(V600E)BRAF is associated with disabled feedback inhibition of RAF-MEK signaling and elevated transcriptional output of the pathwayQ37112466
Genetic predictors of MEK dependence in non-small cell lung cancerQ37113682
Differential induction of apoptosis in HER2 and EGFR addicted cancers following PI3K inhibition.Q37396608
Enhanced PI3K p110α signaling confers acquired lapatinib resistance that can be effectively reversed by a p110α-selective PI3K inhibitorQ37517706
Ras signaling and therapiesQ37548931
Personalized Medicine in Non–Small-Cell Lung Cancer: Is KRAS a Useful Marker in Selecting Patients for Epidermal Growth Factor Receptor–Targeted Therapy?Q37797818
KRAS Mutations in Lung CancerQ38057476
Strategies for co-targeting the PI3K/AKT/mTOR pathway in NSCLC.Q38140353
KRAS mutations and resistance to EGFR-TKIs treatment in patients with non-small cell lung cancer: a meta-analysis of 22 studiesQ39213209
Targeting KRAS-Mutant Non–Small Cell Lung Cancer with the Hsp90 Inhibitor GanetespibQ39271324
KRAS mutant lung cancer cells are differentially responsive to MEK inhibitor due to AKT or STAT3 activation: implication for combinatorial approachQ39720116
Intrinsic resistance to the MEK1/2 inhibitor AZD6244 (ARRY-142886) is associated with weak ERK1/2 signalling and/or strong PI3K signalling in colorectal cancer cell linesQ39819940
PI3K pathway activation mediates resistance to MEK inhibitors in KRAS mutant cancersQ39859169
AZD6244 (ARRY-142886), a potent inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 1/2 kinases: mechanism of action in vivo, pharmacokinetic/pharmacodynamic relationship, and potential for combination in preclQ40093939
Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitorQ40164535
P433issue1
P407language of work or nameEnglishQ1860
P921main subjectselumetinibQ7448840
P304page(s)12-21
P577publication date2014-10-25
P1433published inInvestigational New DrugsQ2312231
P1476titleBYL719, a selective inhibitor of phosphoinositide 3-Kinase α, enhances the effect of selumetinib (AZD6244, ARRY-142886) in KRAS-mutant non-small cell lung cancer
P478volume33

Reverse relations

cites work (P2860)
Q37421296Enhanced anti-tumour activity of the combination of the novel MEK inhibitor WX-554 and the novel PI3K inhibitor WX-037.
Q37214847Enhancement of hyperthermia-induced apoptosis by 5Z-7-oxozeaenol, a TAK1 inhibitor, in A549 cells
Q38731776K-Ras4B/calmodulin/PI3Kα: A promising new adenocarcinoma-specific drug target?
Q91826369Pharmacogenomic landscape of patient-derived tumor cells informs precision oncology therapy
Q38836927Selumetinib in the treatment of non-small-cell lung cancer
Q36398758Targeting KRAS-mutant non-small cell lung cancer: challenges and opportunities.
Q38740315Targeting the MEK signaling pathway in non-small cell lung cancer (NSCLC) patients with RAS aberrations
Q92135408The antipsychotic agent flupentixol is a new PI3K inhibitor and potential anticancer drug for lung cancer
Q38860372The comparison between dual inhibition of mTOR with MAPK and PI3K signaling pathways in KRAS mutant NSCLC cell lines

Search more.