Current development of mTOR inhibitors as anticancer agents.

Inhibition of mTORC1 leads to MAPK pathway activation through a PI3K-dependent feedback loop in human cancer. J Clin Invest (2008) 10.74

Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov (2009) 10.59

Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2. PLoS Biol (2009) 9.63

Targeting cancer with small molecule kinase inhibitors. Nat Rev Cancer (2009) 9.26

Regulation of autophagy by cytoplasmic p53. Nat Cell Biol (2008) 5.97

Antitumor activity of rapamycin in a Phase I trial for patients with recurrent PTEN-deficient glioblastoma. PLoS Med (2008) 5.54

Inhibitor hijacking of Akt activation. Nat Chem Biol (2009) 4.91

Translational control in cancer. Nat Rev Cancer (2010) 4.59

Cell size and invasion in TGF-beta-induced epithelial to mesenchymal transition is regulated by activation of the mTOR pathway. J Cell Biol (2007) 3.47

A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A (2007) 3.21

Rare cancer-specific mutations in PIK3CA show gain of function. Proc Natl Acad Sci U S A (2007) 3.15

Deregulation of the PI3K and KRAS signaling pathways in human cancer cells determines their response to everolimus. J Clin Invest (2010) 3.11

Dominant-activating germline mutations in the gene encoding the PI(3)K catalytic subunit p110δ result in T cell senescence and human immunodeficiency. Nat Immunol (2013) 3.02

mTOR signaling and drug development in cancer. Nat Rev Clin Oncol (2010) 2.77

An oscillatory switch in mTOR kinase activity sets regulatory T cell responsiveness. Immunity (2010) 2.71

Common corruption of the mTOR signaling network in human tumors. Oncogene (2008) 2.60

Metabolic catastrophe as a means to cancer cell death. J Cell Sci (2007) 2.58

Therapeutic suppression of translation initiation modulates chemosensitivity in a mouse lymphoma model. J Clin Invest (2008) 2.40

The mTOR signalling pathway in human cancer. Int J Mol Sci (2012) 2.38

PI3K/PTEN signaling in angiogenesis and tumorigenesis. Adv Cancer Res (2009) 2.32

Emerging therapeutic targets in endometrial cancer. Nat Rev Clin Oncol (2011) 1.99

Angiogenesis inhibitors: current strategies and future prospects. CA Cancer J Clin (2010) 1.98

Multi-parameter phenotypic profiling: using cellular effects to characterize small-molecule compounds. Nat Rev Drug Discov (2009) 1.95

Targeting PI3K/Akt/mTOR Signaling in Cancer. Front Oncol (2014) 1.95

Role of mTOR in anticancer drug resistance: perspectives for improved drug treatment. Drug Resist Updat (2008) 1.90

Delayed correlation of mRNA and protein expression in rapamycin-treated cells and a role for Ggc1 in cellular sensitivity to rapamycin. Mol Cell Proteomics (2009) 1.76

A novel mouse model of inflammatory bowel disease links mammalian target of rapamycin-dependent hyperproliferation of colonic epithelium to inflammation-associated tumorigenesis. Am J Pathol (2009) 1.70

Targeting tumorigenesis: development and use of mTOR inhibitors in cancer therapy. J Hematol Oncol (2009) 1.70

Caspase control: protagonists of cancer cell apoptosis. Exp Oncol (2012) 1.69

Rtp801, a suppressor of mTOR signaling, is an essential mediator of cigarette smoke-induced pulmonary injury and emphysema. Nat Med (2010) 1.67

Targeted therapy for advanced prostate cancer: inhibition of the PI3K/Akt/mTOR pathway. Curr Cancer Drug Targets (2009) 1.66

Stressin' Sestrins take an aging fight. EMBO Mol Med (2010) 1.65

mTOR: a pharmacologic target for autophagy regulation. J Clin Invest (2015) 1.61

Dual inhibition of akt/mammalian target of rapamycin pathway by nanoparticle albumin-bound-rapamycin and perifosine induces antitumor activity in multiple myeloma. Mol Cancer Ther (2010) 1.58

CDC25B mediates rapamycin-induced oncogenic responses in cancer cells. Cancer Res (2009) 1.57

Differential requirement of mTOR in postmitotic tissues and tumorigenesis. Sci Signal (2009) 1.47

Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer. J Med Chem (2011) 1.45

The splicing-factor oncoprotein SF2/ASF activates mTORC1. Proc Natl Acad Sci U S A (2008) 1.42

Safety and pharmacokinetics of paclitaxel and the oral mTOR inhibitor everolimus in advanced solid tumours. Br J Cancer (2009) 1.37

mTORC1 inhibitors: is temsirolimus in renal cancer telling us how they really work? Br J Cancer (2008) 1.37

The phosphoinositide 3-kinase pathway in human cancer: genetic alterations and therapeutic implications. Curr Genomics (2007) 1.33

Identification of a novel small molecule HIF-1alpha translation inhibitor. Clin Cancer Res (2009) 1.33

Activation and function of the mTORC1 pathway in mast cells. J Immunol (2008) 1.31

A phase I trial to determine the safety, tolerability, and maximum tolerated dose of deforolimus in patients with advanced malignancies. Clin Cancer Res (2009) 1.30

Docosahexaenoic acid induces autophagy through p53/AMPK/mTOR signaling and promotes apoptosis in human cancer cells harboring wild-type p53. Autophagy (2011) 1.30

Everolimus. Nat Rev Drug Discov (2009) 1.29

Targeting the mitochondria activates two independent cell death pathways in ovarian cancer stem cells. Mol Cancer Ther (2011) 1.28

Updates of mTOR inhibitors. Anticancer Agents Med Chem (2010) 1.27

Update on triple-negative breast cancer: prognosis and management strategies. Int J Womens Health (2012) 1.26

EGFR-PI3K-AKT-mTOR signaling in head and neck squamous cell carcinomas: attractive targets for molecular-oriented therapy. Expert Opin Ther Targets (2010) 1.25

Molecular aspects of renal cell carcinoma: a review. Am J Cancer Res (2010) 1.25

Mammalian target of rapamycin inhibitors and their potential role in therapy in leukaemia and other haematological malignancies. Br J Haematol (2009) 1.25

Inhibition of fatty-acid synthase induces caspase-8-mediated tumor cell apoptosis by up-regulating DDIT4. J Biol Chem (2008) 1.23

Targeting the PI3K/AKT/mTOR signaling axis in children with hematologic malignancies. Paediatr Drugs (2012) 1.22

Targeting mTORC2 inhibits colon cancer cell proliferation in vitro and tumor formation in vivo. Mol Cancer (2010) 1.21

PTEN loss does not predict for response to RAD001 (Everolimus) in a glioblastoma orthotopic xenograft test panel. Clin Cancer Res (2008) 1.21

Everolimus (RAD001) in the treatment of advanced renal cell carcinoma: a review. Oncologist (2010) 1.20

A novel signaling network as a critical rheostat for the biology and maintenance of the normal stem cell and the cancer-initiating cell. Curr Opin Genet Dev (2009) 1.20

Dual inhibition of phosphatidylinositol 3-kinase/Akt and mammalian target of rapamycin signaling in human nonsmall cell lung cancer cells by a dietary flavonoid fisetin. Int J Cancer (2011) 1.18

Immunosuppressants in cancer prevention and therapy. Oncoimmunology (2013) 1.17

Fisetin induces autophagic cell death through suppression of mTOR signaling pathway in prostate cancer cells. Carcinogenesis (2010) 1.17

Shared signaling networks active in B cells isolated from genetically distinct mouse models of lupus. J Clin Invest (2007) 1.14

Attenuation of multi-targeted proliferation-linked signaling by 3,3'-diindolylmethane (DIM): from bench to clinic. Mutat Res (2011) 1.13

Pharmacokinetic and tumor distribution characteristics of temsirolimus in patients with recurrent malignant glioma. Clin Cancer Res (2007) 1.13

Prospects for mTOR inhibitor use in patients with polycystic kidney disease and hamartomatous diseases. Clin J Am Soc Nephrol (2010) 1.12

Targeted therapy for breast cancer prevention. Front Oncol (2013) 1.12

Deregulated signaling pathways in glioblastoma multiforme: molecular mechanisms and therapeutic targets. Cancer Invest (2012) 1.12

Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach. J Med Chem (2009) 1.10

Growth factors and myometrium: biological effects in uterine fibroid and possible clinical implications. Hum Reprod Update (2011) 1.10

Metformin induces apoptosis and cell cycle arrest mediated by oxidative stress, AMPK and FOXO3a in MCF-7 breast cancer cells. PLoS One (2014) 1.10

Targeted therapies in neuroendocrine tumors (NET): clinical trial challenges and lessons learned. Oncologist (2013) 1.09

Safety, tolerability, pharmacokinetics and pharmacodynamics of AZD8055 in advanced solid tumours and lymphoma. Br J Cancer (2012) 1.09

Tumour Angiogenesis and Angiogenic Inhibitors: A Review. J Clin Diagn Res (2015) 1.09

Fucoidan from seaweed Fucus vesiculosus inhibits migration and invasion of human lung cancer cell via PI3K-Akt-mTOR pathways. PLoS One (2012) 1.08

Mammalian target of rapamycin activator RHEB is frequently overexpressed in human carcinomas and is critical and sufficient for skin epithelial carcinogenesis. Cancer Res (2010) 1.08

Cancer cell signaling pathways targeted by spice-derived nutraceuticals. Nutr Cancer (2011) 1.07

c-myc Repression of TSC2 contributes to control of translation initiation and Myc-induced transformation. Cancer Res (2007) 1.07

Reprogramming of the microRNA transcriptome mediates resistance to rapamycin. J Biol Chem (2013) 1.06

Selective anti-cancer agents as anti-aging drugs. Cancer Biol Ther (2013) 1.06

Adrenocortical Carcinoma: Current Therapeutic State-of-the-Art. J Oncol (2012) 1.05

Overcoming resistance and restoring sensitivity to HER2-targeted therapies in breast cancer. Ann Oncol (2012) 1.05

mTOR inhibitors: A novel class of anti-cancer agents. Infect Agent Cancer (2012) 1.04

mTORC1 inhibition restricts inflammation-associated gastrointestinal tumorigenesis in mice. J Clin Invest (2013) 1.03

Effects of mTOR inhibitor everolimus (RAD001) on bladder cancer cells. Clin Cancer Res (2011) 1.03

Novel paradigms for drug discovery: computational multitarget screening. Trends Pharmacol Sci (2008) 1.03

Oral infusion of pomegranate fruit extract inhibits prostate carcinogenesis in the TRAMP model. Carcinogenesis (2011) 1.03

Combining mTOR Inhibitors with Chemotherapy and Other Targeted Therapies in Advanced Breast Cancer: Rationale, Clinical Experience, and Future Directions. Breast Cancer (Auckl) (2013) 1.02

Extracellular ATP is a pro-angiogenic factor for pulmonary artery vasa vasorum endothelial cells. Angiogenesis (2007) 1.01

North Central Cancer Treatment Group Phase I trial N057K of everolimus (RAD001) and temozolomide in combination with radiation therapy in patients with newly diagnosed glioblastoma multiforme. Int J Radiat Oncol Biol Phys (2010) 1.01

Sustained inhibition of PKCα reduces intravasation and lung seeding during mammary tumor metastasis in an in vivo mouse model. Oncogene (2010) 1.00

Pharmacological and genetic evaluation of proposed roles of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK), extracellular signal-regulated kinase (ERK), and p90(RSK) in the control of mTORC1 protein signaling by phorbol esters. J Biol Chem (2011) 0.99

Differentiating mTOR inhibitors in renal cell carcinoma. Cancer Treat Rev (2013) 0.98

Effect of mTOR inhibitors in nude mice with endometrial carcinoma and variable PTEN expression status. Med Sci Monit Basic Res (2014) 0.98

Small-molecule inhibitors of the PI3K signaling network. Future Med Chem (2011) 0.98

PIM kinase (and Akt) biology and signaling in tumors. Pharmacol Ther (2015) 0.97

A retroinhibition approach reveals a tumor cell-autonomous response to rapamycin in head and neck cancer. Cancer Res (2008) 0.97

Therapeutic targeting of the mTOR-signalling pathway in cancer: benefits and limitations. Br J Pharmacol (2014) 0.96

Targeting the Akt/mTOR pathway in Brca1-deficient cancers. Oncogene (2011) 0.96

Mapping similarities in mTOR pathway perturbations in mouse lupus nephritis models and human lupus nephritis. Arthritis Res Ther (2008) 0.96

Predicting relapse in favorable histology Wilms tumor using gene expression analysis: a report from the Renal Tumor Committee of the Children's Oncology Group. Clin Cancer Res (2009) 0.96

Autophagy in the pathogenesis of disease. Cell (2008) 34.68

Guidelines for the use and interpretation of assays for monitoring autophagy in higher eukaryotes. Autophagy (2007) 20.92

Guidelines for the use and interpretation of assays for monitoring autophagy. Autophagy (2012) 20.08

Self-eating and self-killing: crosstalk between autophagy and apoptosis. Nat Rev Mol Cell Biol (2007) 15.47

The hallmarks of aging. Cell (2013) 14.29

Toll-like receptor 4-dependent contribution of the immune system to anticancer chemotherapy and radiotherapy. Nat Med (2007) 13.90

The pathophysiology of mitochondrial cell death. Science (2004) 13.87

Functional and physical interaction between Bcl-X(L) and a BH3-like domain in Beclin-1. EMBO J (2007) 11.72

Calreticulin exposure dictates the immunogenicity of cancer cell death. Nat Med (2006) 10.54

Inhibition of macroautophagy triggers apoptosis. Mol Cell Biol (2005) 10.27

Molecular mechanisms of necroptosis: an ordered cellular explosion. Nat Rev Mol Cell Biol (2010) 9.06

Safety, pharmacokinetic, and antitumor activity of SU11248, a novel oral multitarget tyrosine kinase inhibitor, in patients with cancer. J Clin Oncol (2005) 7.12

Activation of the NLRP3 inflammasome in dendritic cells induces IL-1beta-dependent adaptive immunity against tumors. Nat Med (2009) 6.73

Immunological aspects of cancer chemotherapy. Nat Rev Immunol (2008) 6.61

Cancer despite immunosurveillance: immunoselection and immunosubversion. Nat Rev Immunol (2006) 6.13

Phase I pharmacokinetic and pharmacodynamic study of the oral mammalian target of rapamycin inhibitor everolimus in patients with advanced solid tumors. J Clin Oncol (2008) 5.98

Regulation of autophagy by cytoplasmic p53. Nat Cell Biol (2008) 5.97

Autophagy and aging. Cell (2011) 5.96

Autophagy-dependent anticancer immune responses induced by chemotherapeutic agents in mice. Science (2011) 5.62

Cytoplasmic functions of the tumour suppressor p53. Nature (2009) 5.23

Induction of autophagy by spermidine promotes longevity. Nat Cell Biol (2009) 5.00

Cell death by mitotic catastrophe: a molecular definition. Oncogene (2004) 4.75

Cell death by necrosis: towards a molecular definition. Trends Biochem Sci (2006) 4.67

The intestinal microbiota modulates the anticancer immune effects of cyclophosphamide. Science (2013) 4.60

Bcl-2 family members: dual regulators of apoptosis and autophagy. Autophagy (2008) 4.42

An immunosurveillance mechanism controls cancer cell ploidy. Science (2012) 4.35

Immunogenic and tolerogenic cell death. Nat Rev Immunol (2009) 4.34

Caspase-dependent immunogenicity of doxorubicin-induced tumor cell death. J Exp Med (2005) 4.32

Molecular basis for sunitinib efficacy and future clinical development. Nat Rev Drug Discov (2007) 4.27

Targeting mitochondria for cancer therapy. Nat Rev Drug Discov (2010) 4.07

The anticancer immune response: indispensable for therapeutic success? J Clin Invest (2008) 4.01

The apoptosis/autophagy paradox: autophagic vacuolization before apoptotic death. J Cell Sci (2005) 3.93

Targeted deletion of AIF decreases mitochondrial oxidative phosphorylation and protects from obesity and diabetes. Cell (2007) 3.82

Mitochondria and the autophagy-inflammation-cell death axis in organismal aging. Science (2011) 3.74

Mechanism of action of conventional and targeted anticancer therapies: reinstating immunosurveillance. Immunity (2013) 3.73

Tumor cells convert immature myeloid dendritic cells into TGF-beta-secreting cells inducing CD4+CD25+ regulatory T cell proliferation. J Exp Med (2005) 3.64

The secret ally: immunostimulation by anticancer drugs. Nat Rev Drug Discov (2012) 3.60

Decoding cell death signals in inflammation and immunity. Cell (2010) 3.41

Immune parameters affecting the efficacy of chemotherapeutic regimens. Nat Rev Clin Oncol (2011) 3.41

Mitotic catastrophe: a mechanism for avoiding genomic instability. Nat Rev Mol Cell Biol (2011) 3.40

Anticancer chemotherapy-induced intratumoral recruitment and differentiation of antigen-presenting cells. Immunity (2013) 3.26

Does autophagy contribute to cell death? Autophagy (2005) 3.21

A novel dendritic cell subset involved in tumor immunosurveillance. Nat Med (2006) 3.21

Heat shock proteins 27 and 70: anti-apoptotic proteins with tumorigenic properties. Cell Cycle (2006) 3.21

AIF deficiency compromises oxidative phosphorylation. EMBO J (2004) 3.19

BH3-only proteins and BH3 mimetics induce autophagy by competitively disrupting the interaction between Beclin 1 and Bcl-2/Bcl-X(L). Autophagy (2007) 3.08

Alternatively spliced NKp30 isoforms affect the prognosis of gastrointestinal stromal tumors. Nat Med (2011) 3.03

The interaction between HMGB1 and TLR4 dictates the outcome of anticancer chemotherapy and radiotherapy. Immunol Rev (2007) 2.96

Stimulation of autophagy by the p53 target gene Sestrin2. Cell Cycle (2009) 2.72

Mechanisms of pre-apoptotic calreticulin exposure in immunogenic cell death. EMBO J (2009) 2.72

Platelet formation is the consequence of caspase activation within megakaryocytes. Blood (2002) 2.62

Necroptosis: a specialized pathway of programmed necrosis. Cell (2008) 2.61

Lysosomal membrane permeabilization induces cell death in a mitochondrion-dependent fashion. J Exp Med (2003) 2.56

Autophagy regulation by p53. Curr Opin Cell Biol (2010) 2.56

Can autophagy promote longevity? Nat Cell Biol (2010) 2.55

Safety and efficacy of sunitinib in patients with advanced hepatocellular carcinoma: an open-label, multicentre, phase II study. Lancet Oncol (2009) 2.53

Cell death assays for drug discovery. Nat Rev Drug Discov (2011) 2.51

Apoptosis-inducing factor is involved in the regulation of caspase-independent neuronal cell death. J Cell Biol (2002) 2.47

Sunitinib versus sorafenib in advanced hepatocellular cancer: results of a randomized phase III trial. J Clin Oncol (2013) 2.46

The IKK complex contributes to the induction of autophagy. EMBO J (2009) 2.41

Fatty acids trigger mitochondrion-dependent necrosis. Cell Cycle (2010) 2.37

Complex inhibitory effects of nitric oxide on autophagy. Mol Cell (2011) 2.36

An AIF orthologue regulates apoptosis in yeast. J Cell Biol (2004) 2.33

Metabolic targets for cancer therapy. Nat Rev Drug Discov (2013) 2.32

Defining the critical hurdles in cancer immunotherapy. J Transl Med (2011) 2.32

Immunogenic tumor cell death for optimal anticancer therapy: the calreticulin exposure pathway. Clin Cancer Res (2010) 2.29

Mitochondria: master regulators of danger signalling. Nat Rev Mol Cell Biol (2012) 2.28

miR-181a and miR-630 regulate cisplatin-induced cancer cell death. Cancer Res (2010) 2.24

Spermidine and resveratrol induce autophagy by distinct pathways converging on the acetylproteome. J Cell Biol (2011) 2.23

Viral control of mitochondrial apoptosis. PLoS Pathog (2008) 2.21

Nonapoptotic role for Apaf-1 in the DNA damage checkpoint. Mol Cell (2007) 2.20

Prognostic and predictive impact of intra- and peritumoral immune infiltrates. Cancer Res (2011) 2.16

Cytoplasmic STAT3 represses autophagy by inhibiting PKR activity. Mol Cell (2012) 2.14

Alternative cell death mechanisms in development and beyond. Genes Dev (2010) 2.14

Mitochondrial membrane permeabilization is a critical step of lysosome-initiated apoptosis induced by hydroxychloroquine. Oncogene (2003) 2.09

Involvement of p38alpha in the mitotic progression of p53(-/-) tetraploid cells. Cell Cycle (2010) 2.08

Decoding cell death signals in liver inflammation. J Hepatol (2013) 2.05

To die or not to die: that is the autophagic question. Curr Mol Med (2008) 2.05

Contribution of IL-17-producing gamma delta T cells to the efficacy of anticancer chemotherapy. J Exp Med (2011) 2.04

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Mutant p53 protein localized in the cytoplasm inhibits autophagy. Cell Cycle (2008) 2.03

A comprehensive glossary of autophagy-related molecules and processes (2nd edition). Autophagy (2011) 2.02

Identifying optimal biologic doses of everolimus (RAD001) in patients with cancer based on the modeling of preclinical and clinical pharmacokinetic and pharmacodynamic data. J Clin Oncol (2008) 2.01

A comprehensive glossary of autophagy-related molecules and processes. Autophagy (2010) 2.00

Methods for assessing autophagy and autophagic cell death. Methods Mol Biol (2008) 1.96

Chemotherapy and radiotherapy: cryptic anticancer vaccines. Semin Immunol (2010) 1.94

Role of the c subunit of the FO ATP synthase in mitochondrial permeability transition. Cell Cycle (2013) 1.94

Apoptosis and genomic instability. Nat Rev Mol Cell Biol (2004) 1.92

Anti- and pro-tumor functions of autophagy. Biochim Biophys Acta (2009) 1.92

Mitochondria, the killer organelles and their weapons. J Cell Physiol (2002) 1.92

Pharmacological manipulation of cell death: clinical applications in sight? J Clin Invest (2005) 1.91

Autophagy is required for the activation of NFκB. Cell Cycle (2012) 1.89

Apoptosis regulation in tetraploid cancer cells. EMBO J (2006) 1.89

High-mobility group box 1 is essential for mitochondrial quality control. Cell Metab (2011) 1.89

Immunogenic cancer cell death: a key-lock paradigm. Curr Opin Immunol (2008) 1.89

Trial Watch: Experimental Toll-like receptor agonists for cancer therapy. Oncoimmunology (2012) 1.88

A dual role of p53 in the control of autophagy. Autophagy (2008) 1.88

Apoptosis-inducing factor (AIF): key to the conserved caspase-independent pathways of cell death? J Cell Sci (2002) 1.88

Roscovitine and other purines as kinase inhibitors. From starfish oocytes to clinical trials. Acc Chem Res (2003) 1.88

Liver mitochondrial membrane crosslinking and destruction in a rat model of Wilson disease. J Clin Invest (2011) 1.86