Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941
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Targeting the mTOR kinase domain: the second generation of mTOR inhibitorsOther targeted drugs in melanomaProtein-intrinsic and signaling network-based sources of resistance to EGFR- and ErbB family-targeted therapies in head and neck cancerA kinome-wide RNAi screen in Drosophila Glia reveals that the RIO kinases mediate cell proliferation and survival through TORC2-Akt signaling in glioblastomaThe p110δ structure: mechanisms for selectivity and potency of new PI(3)K inhibitorsThe discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug designThe p110α and p110β isoforms of PI3K play divergent roles in mammary gland development and tumorigenesis.First-in-human phase I study of pictilisib (GDC-0941), a potent pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor, in patients with advanced solid tumors.mTOR inhibitors in cancer therapyPI3K inhibition enhances doxorubicin-induced apoptosis in sarcoma cellsActive PI3K pathway causes an invasive phenotype which can be reversed or promoted by blocking the pathway at divergent nodesInhibition of mTOR-kinase destabilizes MYCN and is a potential therapy for MYCN-dependent tumorsA computational method for drug repositioning using publicly available gene expression data.Effects of novel isoform-selective phosphoinositide 3-kinase inhibitors on natural killer cell function.Recent advances in the use of PI3K inhibitors for glioblastoma multiforme: current preclinical and clinical developmentRecent advances in the discovery of small molecule mTOR inhibitors.Probing the probes: fitness factors for small molecule tools.Deciphering combinations of PI3K/AKT/mTOR pathway drugs augmenting anti-angiogenic efficacy in vivo.PI3Kα inhibitors that inhibit metastasis.Personalized drug combinations to overcome trastuzumab resistance in HER2-positive breast cancer.Synergistic effects of concurrent blockade of PI3K and MEK pathways in pancreatic cancer preclinical modelsInhibition of the PI3K/Akt/GSK3 pathway downstream of BCR/ABL, Jak2-V617F, or FLT3-ITD downregulates DNA damage-induced Chk1 activation as well as G2/M arrest and prominently enhances induction of apoptosis.Essential role of Stat3 in PI3K-induced oncogenic transformationMicroenvironmental stiffness enhances glioma cell proliferation by stimulating epidermal growth factor receptor signaling.Oncogenic PIK3CA-driven mammary tumors frequently recur via PI3K pathway-dependent and PI3K pathway-independent mechanisms.PI3K in cancer: divergent roles of isoforms, modes of activation and therapeutic targeting.Drugging the PI3 kinome: from chemical tools to drugs in the clinic.Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR inhibitors: rationale and importance to inhibiting these pathways in human health.CDKN2A/p16 Loss Implicates CDK4 as a Therapeutic Target in Imatinib-Resistant Dermatofibrosarcoma Protuberans.Direct and indirect targeting of MYC to treat acute myeloid leukemiaFunctional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agentCell-to-cell variability in PI3K protein level regulates PI3K-AKT pathway activity in cell populations.Genetic disruption of the PI3K regulatory subunits, p85α, p55α, and p50α, normalizes mutant PTPN11-induced hypersensitivity to GM-CSF.The association of PI3 kinase signaling and chemoresistance in advanced ovarian cancer.Harnessing the PI3K/Akt/mTOR pathway in T-cell acute lymphoblastic leukemia: eliminating activity by targeting at different levelsThe insulin response integrates increased TGF-β signaling through Akt-induced enhancement of cell surface delivery of TGF-β receptors.Measurement of PIP3 levels reveals an unexpected role for p110β in early adaptive responses to p110α-specific inhibitors in luminal breast cancer.Inhibition of LRRK2 kinase activity leads to dephosphorylation of Ser(910)/Ser(935), disruption of 14-3-3 binding and altered cytoplasmic localization[18F]-FLT positron emission tomography can be used to image the response of sensitive tumors to PI3-kinase inhibition with the novel agent GDC-0941.Targeting the PI3K/Akt pathway in murine MDS/MPN driven by hyperactive Ras.
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Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941
description
article científic
@ca
article scientifique
@fr
articolo scientifico
@it
artigo científico
@pt
bilimsel makale
@tr
scientific article published on 07 July 2009
@en
vedecký článok
@sk
vetenskaplig artikel
@sv
videnskabelig artikel
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vědecký článek
@cs
name
Biological properties of poten ...... 620 to the oral agent GDC-0941
@en
Biological properties of poten ...... 20 to the oral agent GDC-0941.
@nl
type
label
Biological properties of poten ...... 620 to the oral agent GDC-0941
@en
Biological properties of poten ...... 20 to the oral agent GDC-0941.
@nl
prefLabel
Biological properties of poten ...... 620 to the oral agent GDC-0941
@en
Biological properties of poten ...... 20 to the oral agent GDC-0941.
@nl
P2093
P2860
P1476
Biological properties of poten ...... 620 to the oral agent GDC-0941
@en
P2093
Adrian Folkes
Alan T Henley
Alexander Zhyvoloup
Alexis De Haven Brandon
Angela Hayes
Anthony Robson
Edward McDonald
Florence I Raynaud
Francesca Di Stefano
P2860
P304
P356
10.1158/1535-7163.MCT-08-1200
P50
P577
2009-07-07T00:00:00Z