PI3K inhibitors for cancer treatment: where do we stand?

Temsirolimus, Interferon Alfa, or Both for Advanced Renal-Cell Carcinoma

2007 • 3,560 citations

Efficacy of everolimus in advanced renal cell carcinoma: a double-blind, randomised, placebo-controlled phase III trial

2008 • 2,937 citations

The M2 splice isoform of pyruvate kinase is important for cancer metabolism and tumour growth

2008 • 2,636 citations

mTOR Inhibition Induces Upstream Receptor Tyrosine Kinase Signaling and Activates Akt

2006 • 2,463 citations

Inhibition of mTORC1 leads to MAPK pathway activation through a PI3K-dependent feedback loop in human cancer

2008 • 1,332 citations

The TSC1–TSC2 complex: a molecular switchboard controlling cell growth

2008 • 1,171 citations

Structural Determinants of Phosphoinositide 3-Kinase Inhibition by Wortmannin, LY294002, Quercetin, Myricetin, and Staurosporine

2000 • 1,121 citations

A Pharmacological Map of the PI3-K Family Defines a Role for p110α in Insulin Signaling

2006 • 1,119 citations

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

2008 • 1,099 citations

Enhanced sensitivity of PTEN-deficient tumors to inhibition of FRAP/mTOR

2001 • 981 citations

Pyruvate kinase M2 is a phosphotyrosine-binding protein

2008 • 961 citations

mTOR inhibition reverses Akt-dependent prostate intraepithelial neoplasia through regulation of apoptotic and HIF-1-dependent pathways

2004 • 951 citations

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

2008 • 722 citations

Phase II Trial of Temsirolimus (CCI-779) in Recurrent Glioblastoma Multiforme: A North Central Cancer Treatment Group Study

2005 • 684 citations

Hypoxia-inducible factor determines sensitivity to inhibitors of mTOR in kidney cancer

2005 • 596 citations

A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma

2006 • 587 citations

An inhibitor of mTOR reduces neoplasia and normalizes p70/S6 kinase activity inPten^+/−mice

2001 • 574 citations

Targeting phosphoinositide 3-kinase—Moving towards therapy

2007 • 546 citations

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

2008 • 530 citations

The Structure of a Human p110α/p85α Complex Elucidates the Effects of Oncogenic PI3Kα Mutations

2007 • 523 citations

Structural insights into phosphoinositide 3-kinase catalysis and signalling

1999 • 478 citations

Phase I Pharmacokinetic and Pharmacodynamic Study of the Oral Mammalian Target of Rapamycin Inhibitor Everolimus in Patients With Advanced Solid Tumors

2008 • 473 citations

Phase II Study of Temsirolimus (CCI-779), a Novel Inhibitor of mTOR, in Heavily Pretreated Patients With Locally Advanced or Metastatic Breast Cancer

2005 • 467 citations

Critical role for the p110α phosphoinositide-3-OH kinase in growth and metabolic regulation

2006 • 449 citations

Exploring the specificity of the PI3K family inhibitor LY294002

2007 • 423 citations

Mechanism of Two Classes of Cancer Mutations in the Phosphoinositide 3-Kinase Catalytic Subunit

2007 • 389 citations

Antitumor Activity of ZSTK474, a New Phosphatidylinositol 3-Kinase Inhibitor

2006 • 381 citations

Amino Acids Activate mTOR Complex 1 via Ca2+/CaM Signaling to hVps34

2008 • 360 citations

Restraining PI3K: mTOR signalling goes back to the membrane

2004 • 360 citations

Pharmacologic Characterization of a Potent Inhibitor of Class I Phosphatidylinositide 3-Kinases

2007 • 354 citations

Antitumor Efficacy of Intermittent Treatment Schedules with the Rapamycin Derivative RAD001 Correlates with Prolonged Inactivation of Ribosomal Protein S6 Kinase 1 in Peripheral Blood Mononuclear Cells

2004 • 323 citations

A phase II clinical and pharmacodynamic study of temsirolimus in advanced neuroendocrine carcinomas

2006 • 317 citations

Tumour maintenance is mediated by eNOS

2008 • 312 citations

Molecular pharmacology and antitumor activity of PX-866, a novel inhibitor of phosphoinositide-3-kinase signaling

2004 • 307 citations

A Vascular Targeted Pan Phosphoinositide 3-Kinase Inhibitor Prodrug, SF1126, with Antitumor and Antiangiogenic Activity

2008 • 273 citations

Identifying Optimal Biologic Doses of Everolimus (RAD001) in Patients With Cancer Based on the Modeling of Preclinical and Clinical Pharmacokinetic and Pharmacodynamic Data

2008 • 210 citations

Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling

2007 • 200 citations

4E-Binding Protein 1, A Cell Signaling Hallmark in Breast Cancer that Correlates with Pathologic Grade and Prognosis

2007 • 200 citations

Synthesis and biological evaluation of 4-morpholino-2-phenylquinazolines and related derivatives as novel PI3 kinase p110α inhibitors

2006 • 188 citations

Effects of the Dual Phosphatidylinositol 3-Kinase/Mammalian Target of Rapamycin Inhibitor NVP-BEZ235 on the Tumor Vasculature: Implications for Clinical Imaging

2008 • 174 citations

The phosphatidylinositol-3-kinase inhibitor PX-866 overcomes resistance to the epidermal growth factor receptor inhibitor gefitinib in A-549 human non–small cell lung cancer xenografts

2005 • 149 citations

The phosphatidylinositol 3-kinase inhibitor, PX-866, is a potent inhibitor of cancer cell motility and growth in three-dimensional cultures

2007 • 135 citations

Dynamic Contrast-Enhanced and Diffusion MRI Show Rapid and Dramatic Changes in Tumor Microenvironment in Response to Inhibition of HIF-1α Using PX-478

2005 • 129 citations

Chemically targeting the PI3K family

2007 • 127 citations

Effective in vivo targeting of the mammalian target of rapamycin pathway in malignant peripheral nerve sheath tumors

2008 • 122 citations

Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110α inhibitors

2007 • 115 citations

Class 1A PI3K regulates vessel integrity during development and tumorigenesis

2008 • 97 citations

Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway

2008 • 87 citations

Promise and Progress for Functional and Molecular Imaging of Response to Targeted Therapies

2007 • 67 citations

Rapamycin inhibits multiple stages of c-Neu/ErbB2–induced tumor progression in a transgenic mouse model of HER2-positive breast cancer

2007 • 50 citations

Control of thrombin signaling through PI3K is a mechanism underlying plasticity between hair follicle dermal sheath and papilla cells

2008 • 36 citations

The skin and hair as surrogate tissues for measuring the target effect of inhibitors of phosphoinositide-3-kinase signaling

2006 • 28 citations

Class IA phosphoinositide 3-kinase isoforms and human tumorigenesis: implications for cancer drug discovery and development

2008 • 23 citations

A Versatile High-Throughput Screen for Inhibitors of Lipid Kinase Activity: Development of an Immobilized Phospholipid Plate Assay for Phosphoinositide 3-Kinase γ

2002 • 19 citations

New generation of anilino-substituted pyridopyrazine-urea derivatives show highly selective PI3K-inhibition

2007 • 5 citations