The dual PI3K/mTOR inhibitor NVP-BEZ235 induces tumor regression in a genetically engineered mouse model of PIK3CA wild-type colorectal cancer

scientific article

The dual PI3K/mTOR inhibitor NVP-BEZ235 induces tumor regression in a genetically engineered mouse model of PIK3CA wild-type colorectal cancer is …
instance of (P31):
scholarly articleQ13442814

External links are
P819ADS bibcode2011PLoSO...625132R
P356DOI10.1371/JOURNAL.PONE.0025132
P932PMC publication ID3180374
P698PubMed publication ID21966435
P5875ResearchGate publication ID51687556

P50authorJatin RoperQ57659291
P2093author name stringWei Chen
Roderick T Bronson
Peng-Chieh Chen
Kenneth E Hung
Lydia Lee
Eric S Martin
Erin M Coffee
Mark J Sinnamon
Wei Vivian Wang
Michael P Richardson
Larissa Georgeon Richard
P2860cites workRole of phosphatidylinositol 3,4,5-trisphosphate in regulating the activity and localization of 3-phosphoinositide-dependent protein kinase-1Q24531380
Deregulation of the PI3K and KRAS signaling pathways in human cancer cells determines their response to everolimusQ24600932
mTOR: from growth signal integration to cancer, diabetes and ageingQ24633662
NVP-BEZ235, a novel dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor, elicits multifaceted antitumor activities in human gliomasQ24646237
The role of PTEN/Akt/PI3K signaling in the maintenance and viability of prostate cancer stem-like cell populationsQ24646816
NVP-BEZ235, a dual PI3K/mTOR inhibitor, prevents PI3K signaling and inhibits the growth of cancer cells with activating PI3K mutations.Q27851451
Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancersQ27851457
The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutationsQ27851644
Cancer statistics, 2010Q27860525
High frequency of mutations of the PIK3CA gene in human cancersQ28131776
Defining the role of mTOR in cancerQ28235431
Characterization of a 3-phosphoinositide-dependent protein kinase which phosphorylates and activates protein kinase BalphaQ28616168
The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolismQ29547302
Targeting the phosphoinositide 3-kinase pathway in cancerQ29615809
Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activityQ29618117
Activating mutations in TOR are in similar structures as oncogenic mutations in PI3KCalphaQ30437618
mTOR and cancer: many loops in one pathway.Q33348248
Specific apoptosis induction by the dual PI3K/mTor inhibitor NVP-BEZ235 in HER2 amplified and PIK3CA mutant breast cancer cellsQ33564297
Development of a mouse model for sporadic and metastatic colon tumors and its use in assessing drug treatmentQ33667595
Dual inhibition of PI3K and mTOR inhibits autocrine and paracrine proliferative loops in PI3K/Akt/mTOR-addicted lymphomasQ33896731
Blocking phosphoinositide 3-kinase activity in colorectal cancer cells reduces proliferation but does not increase apoptosis alone or in combination with cytotoxic drugsQ33901504
The combination of RAD001 and NVP-BEZ235 exerts synergistic anticancer activity against non-small cell lung cancer in vitro and in vivoQ33939369
The efficacy of the novel dual PI3-kinase/mTOR inhibitor NVP-BEZ235 compared with rapamycin in renal cell carcinomaQ34001234
Dual blocking of mTor and PI3K elicits a prodifferentiation effect on glioblastoma stem-like cellsQ34480703
The dual PI3K/mTOR inhibitor, NVP-BEZ235, is efficacious against follicular lymphomaQ34522360
The role of mTORC1 pathway in intestinal tumorigenesis.Q43255342
Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors.Q46047974
Effects of the dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235 on the tumor vasculature: implications for clinical imagingQ46431103
Dose- and schedule-dependent inhibition of the mammalian target of rapamycin pathway with everolimus: a phase I tumor pharmacodynamic study in patients with advanced solid tumors.Q46708758
Mutant PIK3CA-bearing colon cancer cells display increased metastasis in an orthotopic model.Q53568151
Systemic treatment of colorectal cancerQ81253030
The two TORCs and Akt.Q34617423
PIK3CA mutations in patients with advanced cancers treated with PI3K/AKT/mTOR axis inhibitorsQ34769343
Dual targeting of phosphoinositide 3-kinase and mammalian target of rapamycin using NVP-BEZ235 as a novel therapeutic approach in human ovarian carcinomaQ34810176
Phosphorylated AKT expression is associated with PIK3CA mutation, low stage, and favorable outcome in 717 colorectal cancersQ34970844
Targeting renal cell carcinoma with NVP-BEZ235, a dual PI3K/mTOR inhibitor, in combination with sorafenibQ35177682
Augmentation of NVP-BEZ235's anticancer activity against human lung cancer cells by blockage of autophagyQ35556966
The mighty mouse: genetically engineered mouse models in cancer drug developmentQ36568461
Inhibition of the mTORC1 pathway suppresses intestinal polyp formation and reduces mortality in ApcDelta716 miceQ36869970
Phosphatidylinositol 3-kinase hyperactivation results in lapatinib resistance that is reversed by the mTOR/phosphatidylinositol 3-kinase inhibitor NVP-BEZ235.Q36983065
Mutations in the phosphatidylinositol-3-kinase pathway predict for antitumor activity of the inhibitor PX-866 whereas oncogenic Ras is a dominant predictor for resistanceQ37036297
Activity of a novel, dual PI3-kinase/mTor inhibitor NVP-BEZ235 against primary human pancreatic cancers grown as orthotopic xenografts.Q37177892
Equivalent benefit of mTORC1 blockade and combined PI3K-mTOR blockade in a mouse model of tuberous sclerosisQ37242436
PTEN and the PI3-kinase pathway in cancerQ37259680
Dual phosphoinositide 3-kinase/mammalian target of rapamycin blockade is an effective radiosensitizing strategy for the treatment of non-small cell lung cancer harboring K-RAS mutationsQ37382669
Differential induction of apoptosis in HER2 and EGFR addicted cancers following PI3K inhibition.Q37396608
Mouse models of colon cancerQ37407244
Phosphoinositide signalling in cancer: beyond PI3K and PTEN.Q37736257
Growth inhibition by NVP-BEZ235, a dual PI3K/mTOR inhibitor, in hepatocellular carcinoma cell linesQ39513509
Levels of p27 sensitize to dual PI3K/mTOR inhibitionQ39529578
The dual PI3K/mTOR inhibitor BEZ235 is effective in lung cancer cell lines.Q39557570
mTORC1 and mTORC2 regulate EMT, motility, and metastasis of colorectal cancer via RhoA and Rac1 signaling pathwaysQ39571848
Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitorQ39591379
The PI3 kinase/mTOR blocker NVP-BEZ235 overrides resistance against irreversible ErbB inhibitors in breast cancer cells.Q39636381
Activity of the novel dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235 against T-cell acute lymphoblastic leukemia.Q39650704
Crosstalk between the PI3K/mTOR and MEK/ERK pathways involved in the maintenance of self-renewal and tumorigenicity of glioblastoma stem-like cells.Q39653276
Compensatory activation of Akt in response to mTOR and Raf inhibitors - a rationale for dual-targeted therapy approaches in neuroendocrine tumor diseaseQ39720433
Inhibition profiles of phosphatidylinositol 3-kinase inhibitors against PI3K superfamily and human cancer cell line panel JFCR39.Q39744205
NVP-BEZ235 as a new therapeutic option for sarcomas.Q39752874
Effects of combined inhibition of MEK and mTOR on downstream signaling and tumor growth in pancreatic cancer xenograft modelsQ39763382
Antimyeloma activity of the orally bioavailable dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235.Q39827794
Dual inhibition of PI3K and mTORC1/2 signaling by NVP-BEZ235 as a new therapeutic strategy for acute myeloid leukemia.Q39832054
The novel orally bioavailable inhibitor of phosphoinositol-3-kinase and mammalian target of rapamycin, NVP-BEZ235, inhibits growth and proliferation in multiple myelomaQ39906851
Mammalian target of rapamycin is activated in human gastric cancer and serves as a target for therapy in an experimental modelQ40182123
Mutant PIK3CA promotes cell growth and invasion of human cancer cellsQ40410776
Dual targeting of the PI3K/Akt/mTOR pathway as an antitumor strategy in Waldenstrom macroglobulinemia.Q42081736
Interfering with resistance to smoothened antagonists by inhibition of the PI3K pathway in medulloblastoma.Q42282551
Increased AKT S473 phosphorylation after mTORC1 inhibition is rictor dependent and does not predict tumor cell response to PI3K/mTOR inhibitionQ42452282
NVP-BEZ235, a dual pan class I PI3 kinase and mTOR inhibitor, promotes osteogenic differentiation in human mesenchymal stromal cells.Q43055104
P275copyright licenseCreative Commons Attribution 4.0 InternationalQ20007257
P6216copyright statuscopyrightedQ50423863
P433issue9
P407language of work or nameEnglishQ1860
P921main subjectcolorectal cancerQ188874
colorectal carcinomaQ25493920
P304page(s)e25132
P577publication date2011-09-26
P1433published inPLOS OneQ564954
P1476titleThe dual PI3K/mTOR inhibitor NVP-BEZ235 induces tumor regression in a genetically engineered mouse model of PIK3CA wild-type colorectal cancer
P478volume6

Reverse relations

cites work (P2860)
Q35987253AKT inhibition overcomes rapamycin resistance by enhancing the repressive function of PRAS40 on mTORC1/4E-BP1 axis
Q33999493Activated cMET and IGF1R-driven PI3K signaling predicts poor survival in colorectal cancers independent of KRAS mutational status
Q34188530Antitumor activities of ATP-competitive inhibitors of mTOR in colon cancer cells
Q36985432Blockage of Autophagy Rescues the Dual PI3K/mTOR Inhibitor BEZ235-induced Growth Inhibition of Colorectal Cancer Cells
Q35321647Cell specific apoptosis by RLX is mediated by NFκB in human colon carcinoma HCT-116 cells
Q47558200Colonoscopy-based colorectal cancer modeling in mice with CRISPR-Cas9 genome editing and organoid transplantation.
Q42085487Combination PI3K/MEK inhibition promotes tumor apoptosis and regression in PIK3CA wild-type, KRAS mutant colorectal cancer
Q27852136Concomitant BRAF and PI3K/mTOR blockade is required for effective treatment of BRAF(V600E) colorectal cancer
Q50027355Crosstalk signaling between HER3 and HPV16 E6 and E7 mediates resistance to PI3K inhibitors in head and neck cancer
Q38824026Design, Synthesis, Activity and Docking Study of Sorafenib Analogs Bearing Sulfonylurea Unit.
Q38080710Development of PI3K inhibitors: lessons learned from early clinical trials
Q37632641Development of a colon cancer GEMM-derived orthotopic transplant model for drug discovery and validation.
Q64055917EMT Regulation by Autophagy: A New Perspective in Glioblastoma Biology
Q33934922Effective inhibition of colon cancer cell growth with MgAl-layered double hydroxide (LDH) loaded 5-FU and PI3K/mTOR dual inhibitor BEZ-235 through apoptotic pathways
Q89156992Facile construction of fused benzimidazole-isoquinolinones that induce cell-cycle arrest and apoptosis in colorectal cancer cells
Q34332175Genetically engineered mouse models of PI3K signaling in breast cancer
Q28534803Genotype directed therapy in murine mismatch repair deficient tumors
Q38705367In vivo genome editing and organoid transplantation models of colorectal cancer and metastasis
Q39255433Inhibition of autophagy enhances apoptosis induced by the PI3K/AKT/mTor inhibitor NVP-BEZ235 in renal cell carcinoma cells
Q34182679MET and PI3K/mTOR as a potential combinatorial therapeutic target in malignant pleural mesothelioma
Q92059453Mouse models of colorectal cancer: Past, present and future perspectives
Q89558411NVP-BEZ235 inhibits thyroid cancer growth by p53- dependent/independent p21 upregulation
Q35063769NVP-BEZ235 overcomes gefitinib-acquired resistance by down-regulating PI3K/AKT/mTOR phosphorylation
Q34679652NVP-BEZ235, a novel dual PI3K/mTOR inhibitor, enhances the radiosensitivity of human glioma stem cells in vitro
Q37660260Novel PI3K and mTOR Inhibitor NVP-BEZ235 Radiosensitizes Breast Cancer Cell Lines under Normoxic and Hypoxic Conditions.
Q26781367PI3K and AKT: Unfaithful Partners in Cancer
Q37727180PI3K and Akt as molecular targets for cancer therapy: current clinical outcomes
Q40509393PI3K/Akt/mTOR pathway dual inhibitor BEZ235 suppresses the stemness of colon cancer stem cells.
Q55518346PIK3CA mutations confer resistance to first-line chemotherapy in colorectal cancer.
Q47128334PKM2 is not required for colon cancer initiated by APC loss.
Q52310328PP242 Counteracts Glioblastoma Cell Proliferation, Migration, Invasiveness and Stemness Properties by Inhibiting mTORC2/AKT.
Q41472038PTRF suppresses the progression of colorectal cancers.
Q35987363PUMA mediates the combinational therapy of 5-FU and NVP-BEZ235 in colon cancer
Q26766292Pharmacodynamic Biomarker Development for PI3K Pathway Therapeutics
Q89036516Phase 1/1b dose escalation and expansion study of BEZ235, a dual PI3K/mTOR inhibitor, in patients with advanced solid tumors including patients with advanced breast cancer
Q91745562Pretargeted delivery of PI3K/mTOR small-molecule inhibitor-loaded nanoparticles for treatment of non-Hodgkin's lymphoma
Q33776641Recent advances in the use of PI3K inhibitors for glioblastoma multiforme: current preclinical and clinical development
Q39067602Selective targeting of human colon cancer stem-like cells by the mTOR inhibitor Torin-1.
Q57477082Sodium tanshinone IIA sulfonate protects ARPE-19 cells against oxidative stress by inhibiting autophagy and apoptosis
Q28396388Sustained proliferation in cancer: Mechanisms and novel therapeutic targets
Q39735209Synergistic inhibition of colon cancer cell growth with nanoemulsion-loaded paclitaxel and PI3K/mTOR dual inhibitor BEZ235 through apoptosis
Q42360077Targeted inhibition of the phosphoinositide 3-kinase impairs cell proliferation, survival, and invasion in colon cancer
Q92550221Targeting Akt by SC66 triggers GSK-3β mediated apoptosis in colon cancer therapy
Q38105322Targeting PI3K in Cancer: Any Good News?
Q38375141Targeting PI3Kδ: emerging therapy for chronic lymphocytic leukemia and beyond
Q37708005Targeting mTOR network in colorectal cancer therapy
Q38121524Targeting the mTOR signaling network for Alzheimer's disease therapy
Q26744721The Inositide Signaling Pathway As a Target for Treating Gastric Cancer and Colorectal Cancer
Q38043507The promise of mTOR inhibitors in the treatment of colorectal cancer
Q37687348The role of SH3GL3 in myeloma cell migration/invasion, stemness and chemo-resistance
Q89846048The synergistic anti-proliferative effect of the combination of diosmin and BEZ-235 (dactolisib) on the HCT-116 colorectal cancer cell line occurs through inhibition of the PI3K/Akt/mTOR/NF-κB axis
Q91716178Therapeutic Potency of PI3K Pharmacological Inhibitors of Gastrointestinal Cancer
Q38946538Therapeutic Potential of Targeting PI3K/AKT Pathway in Treatment of Colorectal Cancer: Rational and Progress.
Q38208069Therapeutic targeting of the mTOR-signalling pathway in cancer: benefits and limitations
Q38042938Therapeutic targeting of the phosphatidylinositol 3-kinase signaling pathway: novel targeted therapies and advances in the treatment of colorectal cancer
Q36471425Treatment of Triple-Negative Breast Cancer with TORC1/2 Inhibitors Sustains a Drug-Resistant and Notch-Dependent Cancer Stem Cell Population
Q64274877mTOR Signaling in Cancer and mTOR Inhibitors in Solid Tumor Targeting Therapy
Q37649634mTOR pathway in colorectal cancer: an update