Next-generation mTOR inhibitors in clinical oncology: how pathway complexity informs therapeutic strategy

Targeting mTOR globally in cancer: Thinking beyond rapamycin

(2011) Boris Shor et al.   CELL CYCLE

BRAF as therapeutic target in melanoma

(2010) Claudia Wellbrock et al.   BIOCHEMICAL PHARMACOLOGY

Not all substrates are treated equally: Implications for mTOR, rapamycin-resistance, and cancer therapy

(2010) Andrew Y. Choo et al.   CELL CYCLE

The Efficacy of the Novel Dual PI3-Kinase/mTOR Inhibitor NVP-BEZ235 Compared with Rapamycin in Renal Cell Carcinoma

(2010) D. C. Cho et al.   CLINICAL CANCER RESEARCH

Deregulation of the PI3K and KRAS signaling pathways in human cancer cells determines their response to everolimus

(2010) Federica Di Nicolantonio et al.   JOURNAL OF CLINICAL INVESTIGATION

Temsirolimus Has Activity in Non–Mantle Cell Non-Hodgkin's Lymphoma Subtypes: The University of Chicago Phase II Consortium

(2010) Sonali M. Smith et al.   JOURNAL OF CLINICAL ONCOLOGY

Antitumor Efficacy Profile of PKI-402, a Dual Phosphatidylinositol 3-Kinase/Mammalian Target of Rapamycin Inhibitor

(2010) Robert Mallon et al.   MOLECULAR CANCER THERAPEUTICS

Status of PI3K inhibition and biomarker development in cancer therapeutics

(2009) B. Markman et al.   ANNALS OF ONCOLOGY

Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR)

(2009) Juan M. García-Martínez et al.   BIOCHEMICAL JOURNAL

Activity of a novel, dual PI3-kinase/mTor inhibitor NVP-BEZ235 against primary human pancreatic cancers grown as orthotopic xenografts

(2009) P Cao et al.   BRITISH JOURNAL OF CANCER

AKT-Independent Signaling Downstream of Oncogenic PIK3CA Mutations in Human Cancer

(2009) Krishna M. Vasudevan et al.   CANCER CELL

Antimyeloma Activity of the Orally Bioavailable Dual Phosphatidylinositol 3-Kinase/Mammalian Target of Rapamycin Inhibitor NVP-BEZ235

(2009) D. W. McMillin et al.   CANCER RESEARCH

AZD8055 Is a Potent, Selective, and Orally Bioavailable ATP-Competitive Mammalian Target of Rapamycin Kinase Inhibitor with In vitro and In vivo Antitumor Activity

(2009) C. M. Chresta et al.   CANCER RESEARCH

Biochemical, Cellular, and In vivo Activity of Novel ATP-Competitive and Selective Inhibitors of the Mammalian Target of Rapamycin

(2009) K. Yu et al.   CANCER RESEARCH

DEPTOR Is an mTOR Inhibitor Frequently Overexpressed in Multiple Myeloma Cells and Required for Their Survival

(2009) Timothy R. Peterson et al.   CELL

A Branched-Chain Amino Acid-Related Metabolic Signature that Differentiates Obese and Lean Humans and Contributes to Insulin Resistance

(2009) Christopher B. Newgard et al.   Cell Metabolism

Spectrum of Phosphatidylinositol 3-Kinase Pathway Gene Alterations in Bladder Cancer

(2009) F. M. Platt et al.   CLINICAL CANCER RESEARCH

An Emerging Role of mTOR in Lipid Biosynthesis

(2009) Mathieu Laplante et al.   CURRENT BIOLOGY

An ATP-competitive Mammalian Target of Rapamycin Inhibitor Reveals Rapamycin-resistant Functions of mTORC1

(2009) Carson C. Thoreen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Randomized Phase II Study Comparing Two Schedules of Everolimus in Patients With Recurrent/Metastatic Breast Cancer: NCIC Clinical Trials Group IND.163

(2009) Susan L. Ellard et al.   JOURNAL OF CLINICAL ONCOLOGY

Targeting the mTOR Signaling Network for Cancer Therapy

(2009) Funda Meric-Bernstam et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase III Study to Evaluate Temsirolimus Compared With Investigator's Choice Therapy for the Treatment of Relapsed or Refractory Mantle Cell Lymphoma

(2009) Georg Hess et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase II Randomized Study of Neoadjuvant Everolimus Plus Letrozole Compared With Placebo Plus Letrozole in Patients With Estrogen Receptor–Positive Breast Cancer

(2009) José Baselga et al.   JOURNAL OF CLINICAL ONCOLOGY

Aberrant expression of TSC2 gene in the newly diagnosed acute leukemia

(2009) Zhifang Xu et al.   LEUKEMIA RESEARCH

Characterization of Rictor Phosphorylation Sites Reveals Direct Regulation of mTOR Complex 2 by S6K1

(2009) C. C. Dibble et al.   MOLECULAR AND CELLULAR BIOLOGY

mTORC1-Activated S6K1 Phosphorylates Rictor on Threonine 1135 and Regulates mTORC2 Signaling

(2009) L.-A. Julien et al.   MOLECULAR AND CELLULAR BIOLOGY

Targeting Melanoma with Dual Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitors

(2009) R. Marone et al.   MOLECULAR CANCER RESEARCH

NVP-BEZ235, a novel dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor, elicits multifaceted antitumor activities in human gliomas

(2009) T.-J. Liu et al.   MOLECULAR CANCER THERAPEUTICS

Oncogenic B-RAF Negatively Regulates the Tumor Suppressor LKB1 to Promote Melanoma Cell Proliferation

(2009) Bin Zheng et al.   MOLECULAR CELL

Targeting the phosphoinositide 3-kinase pathway in cancer

(2009) Pixu Liu et al.   NATURE REVIEWS DRUG DISCOVERY

The nuts and bolts of AGC protein kinases

(2009) Laura R. Pearce et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Common corruption of the mTOR signaling network in human tumors

(2009) S Menon et al.   ONCOGENE

Uncoupling of the LKB1-AMPKα Energy Sensor Pathway by Growth Factors and Oncogenic BRAFV600E

(2009) Rosaura Esteve-Puig et al.   PLoS One

RSK1 drives p27Kip1 phosphorylation at T198 to promote RhoA inhibition and increase cell motility

(2009) M. D. Larrea et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Specific apoptosis induction by the dual PI3K/mTor inhibitor NVP-BEZ235 in HER2 amplified and PIK3CA mutant breast cancer cells

(2009) Saskia M. Brachmann et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Human cancers converge at the HIF-2α oncogenic axis

(2009) Aleksandra Franovic et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Active-Site Inhibitors of mTOR Target Rapamycin-Resistant Outputs of mTORC1 and mTORC2

(2009) Morris E Feldman et al.   PLOS BIOLOGY

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

(2008) Jingxiang Huang et al.   BIOCHEMICAL JOURNAL

mTOR complex 2 (mTORC2) controls hydrophobic motif phosphorylation and activation of serum- and glucocorticoid-induced protein kinase 1 (SGK1)

(2008) Juan M. García-Martínez et al.   BIOCHEMICAL JOURNAL

Involvement of TSC genes and differential expression of other members of the mTOR signaling pathway in oral squamous cell carcinoma

(2008) Sanjukta Chakraborty et al.   BMC CANCER

Low-dose, single-agent temsirolimus for relapsed mantle cell lymphoma

(2008) Stephen M. Ansell et al.   CANCER

Tumor Cell Metabolism: Cancer's Achilles' Heel

(2008) Guido Kroemer et al.   CANCER CELL

Palomid 529, a Novel Small-Molecule Drug, Is a TORC1/TORC2 Inhibitor That Reduces Tumor Growth, Tumor Angiogenesis, and Vascular Permeability

(2008) Q. Xue et al.   CANCER RESEARCH

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

(2008) C. R. Schnell et al.   CANCER RESEARCH

NVP-BEZ235, a Dual PI3K/mTOR Inhibitor, Prevents PI3K Signaling and Inhibits the Growth of Cancer Cells with Activating PI3K Mutations

(2008) V. Serra et al.   CANCER RESEARCH

The Biology of Cancer: Metabolic Reprogramming Fuels Cell Growth and Proliferation

(2008) Ralph J. DeBerardinis et al.   Cell Metabolism

Oncogenic MAPK Signaling Stimulates mTORC1 Activity by Promoting RSK-Mediated Raptor Phosphorylation

(2008) Audrey Carrière et al.   CURRENT BIOLOGY

Hypoxia regulates TSC1/2 mTOR signaling and tumor suppression through REDD1-mediated 14 3 3 shuttling

(2008) M. P. DeYoung et al.   GENES & DEVELOPMENT

Efficacy of RAD001 (Everolimus) and Octreotide LAR in Advanced Low- to Intermediate-Grade Neuroendocrine Tumors: Results of a Phase II Study

(2008) James C. Yao et al.   JOURNAL OF CLINICAL ONCOLOGY

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) Josep Tabernero et al.   JOURNAL OF CLINICAL ONCOLOGY

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

(2008) Robert J Motzer et al.   LANCET

PI-103, a dual inhibitor of Class IA phosphatidylinositide 3-kinase and mTOR, has antileukemic activity in AML

(2008) S Park et al.   LEUKEMIA

mTOR-Raptor Binds and Activates SGK1 to Regulate p27 Phosphorylation

(2008) Feng Hong et al.   MOLECULAR CELL

AMPK Phosphorylation of Raptor Mediates a Metabolic Checkpoint

(2008) Dana M. Gwinn et al.   MOLECULAR CELL

Sirolimus for Angiomyolipoma in Tuberous Sclerosis Complex or Lymphangioleiomyomatosis

(2008) John J. Bissler et al.   NEW ENGLAND JOURNAL OF MEDICINE

Suppression of PTEN function increases breast cancer chemotherapeutic drug resistance while conferring sensitivity to mTOR inhibitors

(2008) L S Steelman et al.   ONCOGENE

The PTEN–PI3K pathway: of feedbacks and cross-talks

(2008) A Carracedo et al.   ONCOGENE

Rapamycin differentially inhibits S6Ks and 4E-BP1 to mediate cell-type-specific repression of mRNA translation

(2008) A. Y. Choo et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Targeting phosphoinositide 3-kinase—Moving towards therapy

(2007) Romina Marone et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

The oral mTOR inhibitor RAD001 (everolimus) in combination with letrozole in patients with advanced breast cancer: Results of a phase I study with pharmacokinetics

(2007) Ahmad Awada et al.   EUROPEAN JOURNAL OF CANCER

Pulmonary lymphangioleiomyomatosis (LAM): Progress and current challenges

(2007) Elena A. Goncharova et al.   JOURNAL OF CELLULAR BIOCHEMISTRY