(Q37950771)

25 August 2017

Rapamycin passes the torch: a new generation of mTOR inhibitors (English)

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25 August 2017

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Don Benjamin

1

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25 August 2017

Marco Colombi

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2

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25 August 2017

Christoph Moroni

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3

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25 August 2017

Michael N Hall

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4

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25 August 2017

31 October 2011

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Nature Reviews Drug Discovery

25 August 2017

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25 August 2017

10

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25 August 2017

868-880

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25 August 2017

11

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https://scigraph.springernature.com/pub.10.1038/nrd3531

25 August 2017

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cites work

Rapamycin (AY-22,989), a new antifungal antibiotic. I. Taxonomy of the producing streptomycete and isolation of the active principle

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Human brain tumor xenografts in nude mice as a chemotherapy model.

21 January 2018

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Targets for Cell Cycle Arrest by the Immunosuppressant Rapamycin in Yeast

21 January 2018

1 reference

mTOR: from growth signal integration to cancer, diabetes and ageing

21 January 2018

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Prolonged rapamycin treatment inhibits mTORC2 assembly and Akt/PKB

21 January 2018

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TOR signaling in growth and metabolism

21 January 2018

1 reference

Mammalian cell size is controlled by mTOR and its downstream targets S6K1 and 4EBP1/eIF4E

21 January 2018

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Tor, a phosphatidylinositol kinase homologue, controls autophagy in yeast

21 January 2018

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mTOR regulation of autophagy

21 January 2018

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TOR2 is required for organization of the actin cytoskeleton in yeast

21 January 2018

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Two TOR complexes, only one of which is rapamycin sensitive, have distinct roles in cell growth control

21 January 2018

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Mammalian TOR complex 2 controls the actin cytoskeleton and is rapamycin insensitive

21 January 2018

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Rictor, a novel binding partner of mTOR, defines a rapamycin-insensitive and raptor-independent pathway that regulates the cytoskeleton

21 January 2018

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Role of mTOR signaling in tumor cell motility, invasion and metastasis

21 January 2018

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Phosphorylation and regulation of Akt/PKB by the rictor-mTOR complex

21 January 2018

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

21 January 2018

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Essential function of TORC2 in PKC and Akt turn motif phosphorylation, maturation and signalling

21 January 2018

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Activation of mTORC2 by association with the ribosome

21 January 2018

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mTORC2 can associate with ribosomes to promote cotranslational phosphorylation and stability of nascent Akt polypeptide

21 January 2018

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mTORC1 controls fasting-induced ketogenesis and its modulation by ageing.

21 January 2018

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Rictor/mTORC2 is essential for maintaining a balance between beta-cell proliferation and cell size

21 January 2018

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Skeletal muscle-specific ablation of raptor, but not of rictor, causes metabolic changes and results in muscle dystrophy

21 January 2018

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Muscle inactivation of mTOR causes metabolic and dystrophin defects leading to severe myopathy

21 January 2018

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Adipose-specific knockout of raptor results in lean mice with enhanced mitochondrial respiration

21 January 2018

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mTOR complex 2 in adipose tissue negatively controls whole-body growth

21 January 2018

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Mediobasal hypothalamic p70 S6 kinase 1 modulates the control of energy homeostasis

21 January 2018

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Inappropriate activation of the TSC/Rheb/mTOR/S6K cassette induces IRS1/2 depletion, insulin resistance, and cell survival deficiencies

21 January 2018

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The TSC1-2 tumor suppressor controls insulin-PI3K signaling via regulation of IRS proteins

21 January 2018

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Absence of S6K1 protects against age- and diet-induced obesity while enhancing insulin sensitivity

21 January 2018

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Disruption of the mouse mTOR gene leads to early postimplantation lethality and prohibits embryonic stem cell development

21 January 2018

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mTOR is essential for growth and proliferation in early mouse embryos and embryonic stem cells

21 January 2018

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Role of mTOR in podocyte function and diabetic nephropathy in humans and mice

21 January 2018

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Cardiac raptor ablation impairs adaptive hypertrophy, alters metabolic gene expression, and causes heart failure in mice.

21 January 2018

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mTOR complex 2 is required for the development of prostate cancer induced by Pten loss in mice

21 January 2018

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Differential requirement of mTOR in postmitotic tissues and tumorigenesis

21 January 2018

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Activation of a metabolic gene regulatory network downstream of mTOR complex 1

21 January 2018

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Regulation of yeast replicative life span by TOR and Sch9 in response to nutrients

21 January 2018

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Regulation of lifespan in Drosophila by modulation of genes in the TOR signaling pathway

21 January 2018

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Regulation of elongation phase of mRNA translation in diabetic nephropathy: amelioration by rapamycin

21 January 2018

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Rapamycin reverses cellular phenotypes and enhances mutant protein clearance in Hutchinson-Gilford progeria syndrome cells

21 January 2018

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Comparison of acute rapamycin nephrotoxicity with cyclosporine and FK506.

21 January 2018

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Temsirolimus, an inhibitor of mammalian target of rapamycin

21 January 2018

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Everolimus: a proliferation signal inhibitor with clinical applications in organ transplantation, oncology, and cardiology.

21 January 2018

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Temsirolimus, interferon alfa, or both for advanced renal-cell carcinoma

21 January 2018

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

21 January 2018

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Phase III study to evaluate temsirolimus compared with investigator's choice therapy for the treatment of relapsed or refractory mantle cell lymphoma

21 January 2018

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Everolimus for advanced pancreatic neuroendocrine tumors.

21 January 2018

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Sirolimus for angiomyolipoma in tuberous sclerosis complex or lymphangioleiomyomatosis

21 January 2018

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mTOR inhibition induces upstream receptor tyrosine kinase signaling and activates Akt

21 January 2018

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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.

21 January 2018

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

21 January 2018

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Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2

21 January 2018

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An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1

21 January 2018

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mTORC1-mediated cell proliferation, but not cell growth, controlled by the 4E-BPs

21 January 2018

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Myeloma cell growth inhibition is augmented by synchronous inhibition of the insulin-like growth factor-1 receptor by NVP-AEW541 and inhibition of mammalian target of rapamycin by Rad001.

21 January 2018

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Disruption of parallel and converging signaling pathways contributes to the synergistic antitumor effects of simultaneous mTOR and EGFR inhibition in GBM cells

21 January 2018

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Longitudinal inhibition of PI3K/Akt/mTOR signaling by LY294002 and rapamycin induces growth arrest of adult T-cell leukemia cells.

21 January 2018

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Hybrid inhibitors of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR): design, synthesis, and superior antitumor activity of novel wortmannin-rapamycin conjugates

21 January 2018

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Dual inhibition of akt/mammalian target of rapamycin pathway by nanoparticle albumin-bound-rapamycin and perifosine induces antitumor activity in multiple myeloma.

21 January 2018

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Rapamycin and mTOR kinase inhibitors

21 January 2018

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A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling

21 January 2018

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

21 January 2018

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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

21 January 2018

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Targeting the mTOR kinase domain: the second generation of mTOR inhibitors

21 January 2018

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The novel orally bioavailable inhibitor of phosphoinositol-3-kinase and mammalian target of rapamycin, NVP-BEZ235, inhibits growth and proliferation in multiple myeloma

21 January 2018

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NVP-BEZ235 as a new therapeutic option for sarcomas.

21 January 2018

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Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers

21 January 2018

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Vertical targeting of the phosphatidylinositol-3 kinase pathway as a strategy for treating melanoma

21 January 2018

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First-in-class, first-in-human phase I results of targeted agents: highlights of the 2008 American society of clinical oncology meeting

21 January 2018

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A vascular targeted pan phosphoinositide 3-kinase inhibitor prodrug, SF1126, with antitumor and antiangiogenic activity

21 January 2018

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Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases

21 January 2018

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Genetic dissection of the oncogenic mTOR pathway reveals druggable addiction to translational control via 4EBP-eIF4E

21 January 2018

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Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor

21 January 2018

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Targeting eukaryotic translation initiation factor 4E (eIF4E) in cancer

21 January 2018

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AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity

21 January 2018

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Benefits of mTOR kinase targeting in oncology: pre-clinical evidence with AZD8055.

21 January 2018

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Simultaneous inhibition of mTORC1 and mTORC2 by mTOR kinase inhibitor AZD8055 induces autophagy and cell death in cancer cells

21 January 2018

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Critical roles for mTORC2- and rapamycin-insensitive mTORC1-complexes in growth and survival of BCR-ABL-expressing leukemic cells

21 January 2018

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Palomid 529, a novel small-molecule drug, is a TORC1/TORC2 inhibitor that reduces tumor growth, tumor angiogenesis, and vascular permeability

21 January 2018

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Muller cell reactivity and photoreceptor cell death are reduced after experimental retinal detachment using an inhibitor of the Akt/mTOR pathway

21 January 2018

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Targeting the Akt/mTOR pathway in Brca1-deficient cancers

21 January 2018

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The TORC1/TORC2 inhibitor, Palomid 529, reduces tumor growth and sensitizes to docetaxel and cisplatin in aggressive and hormone-refractory prostate cancer cells.

21 January 2018

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The novel Akt inhibitor Palomid 529 (P529) enhances the effect of radiotherapy in prostate cancer

21 January 2018

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Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin

21 January 2018

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Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2.

21 January 2018

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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.

21 January 2018

1 reference

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

21 January 2018

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WJD008, a dual phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin inhibitor, prevents PI3K signaling and inhibits the proliferation of transformed cells with oncogenic PI3K mutant

21 January 2018

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Antitumor efficacy profile of PKI-402, a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor

21 January 2018

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Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors.

21 January 2018

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Reduced VEGF production, angiogenesis, and vascular regrowth contribute to the antitumor properties of dual mTORC1/mTORC2 inhibitors

21 January 2018

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Recent advances in the discovery of small-molecule ATP competitive mTOR inhibitors: a patent review

21 January 2018

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Structure of the FKBP12-rapamycin complex interacting with the binding domain of human FRAP

21 January 2018

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Refined structure of the FKBP12-rapamycin-FRB ternary complex at 2.2 A resolution

21 January 2018

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The FRB domain of mTOR: NMR solution structure and inhibitor design

21 January 2018

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The solution structure of the FATC domain of the protein kinase target of rapamycin suggests a role for redox-dependent structural and cellular stability

21 January 2018

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Insights into the domain and repeat architecture of target of rapamycin

21 January 2018

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Structure of the human mTOR complex I and its implications for rapamycin inhibition.

21 January 2018

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Activating mutations in TOR are in similar structures as oncogenic mutations in PI3KCalpha

21 January 2018

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Phosphatidic acid-mediated mitogenic activation of mTOR signaling

21 January 2018

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Structural characterization of the interaction of mTOR with phosphatidic acid and a novel class of inhibitor: compelling evidence for a central role of the FRB domain in small molecule-mediated regulation of mTOR

21 January 2018

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Phospholipase D regulates myogenic differentiation through the activation of both mTORC1 and mTORC2 complexes

21 January 2018

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Metformin and reduced risk of cancer in diabetic patients

21 January 2018

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New users of metformin are at low risk of incident cancer: a cohort study among people with type 2 diabetes

21 January 2018

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The LKB1 tumor suppressor negatively regulates mTOR signaling

21 January 2018

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AMPK phosphorylation of raptor mediates a metabolic checkpoint

21 January 2018

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Metformin, independent of AMPK, inhibits mTORC1 in a rag GTPase-dependent manner

21 January 2018

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21 January 2018

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The influence of glucose-lowering therapies on cancer risk in type 2 diabetes

21 January 2018

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Antidiabetic therapies affect risk of pancreatic cancer

21 January 2018

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Metformin use and prostate cancer in Caucasian men: results from a population-based case-control study

21 January 2018

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Metformin and pathologic complete responses to neoadjuvant chemotherapy in diabetic patients with breast cancer

21 January 2018

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Recent advances in the therapeutic perspectives of Nutlin-3.

21 January 2018

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ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor

21 January 2018

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Molecular organization of target of rapamycin complex 2.

21 January 2018

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Drosophila target of rapamycin kinase functions as a multimer.

21 January 2018

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Farnesylthiosalicylic acid inhibits mammalian target of rapamycin (mTOR) activity both in cells and in vitro by promoting dissociation of the mTOR-raptor complex

21 January 2018

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GCN2 protein kinase is required to activate amino acid deprivation responses in mice treated with the anti-cancer agent L-asparaginase.

21 January 2018

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The Rag GTPases bind raptor and mediate amino acid signaling to mTORC1

21 January 2018

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Ragulator-Rag complex targets mTORC1 to the lysosomal surface and is necessary for its activation by amino acids

21 January 2018

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The rapamycin-sensitive phosphoproteome reveals that TOR controls protein kinase A toward some but not all substrates.

21 January 2018

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Characterization of the rapamycin-sensitive phosphoproteome reveals that Sch9 is a central coordinator of protein synthesis

21 January 2018

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The mTOR-regulated phosphoproteome reveals a mechanism of mTORC1-mediated inhibition of growth factor signaling.

21 January 2018

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Phosphoproteomic analysis identifies Grb10 as an mTORC1 substrate that negatively regulates insulin signaling

21 January 2018

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Genome-wide shRNA screen reveals increased mitochondrial dependence upon mTORC2 addiction

21 January 2018

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Mammalian target of rapamycin: hitting the bull's-eye for neurological disorders

21 January 2018

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Target of rapamycin in yeast, TOR2, is an essential phosphatidylinositol kinase homolog required for G1 progression

21 January 2018

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A mammalian protein targeted by G1-arresting rapamycin-receptor complex

21 January 2018

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RAFT1: a mammalian protein that binds to FKBP12 in a rapamycin-dependent fashion and is homologous to yeast TORs

21 January 2018

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RAPT1, a mammalian homolog of yeast Tor, interacts with the FKBP12/rapamycin complex

21 January 2018

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Isolation of a protein target of the FKBP12-rapamycin complex in mammalian cells

21 January 2018

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TOR controls translation initiation and early G1 progression in yeast

21 January 2018

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Regulation of eIF-4E BP1 phosphorylation by mTOR.

21 January 2018

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Phosphorylation of the translational repressor PHAS-I by the mammalian target of rapamycin

21 January 2018

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RAFT1 phosphorylation of the translational regulators p70 S6 kinase and 4E-BP1

21 January 2018

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Amino acid sufficiency and mTOR regulate p70 S6 kinase and eIF-4E BP1 through a common effector mechanism

21 January 2018

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Amino acid availability regulates p70 S6 kinase and multiple translation factors

21 January 2018

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TOR, a central controller of cell growth

21 January 2018

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Akt regulates growth by directly phosphorylating Tsc2

21 January 2018

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TSC2 is phosphorylated and inhibited by Akt and suppresses mTOR signalling

21 January 2018

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Tsc tumour suppressor proteins antagonize amino-acid-TOR signalling

21 January 2018

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Identification of the tuberous sclerosis complex-2 tumor suppressor gene product tuberin as a target of the phosphoinositide 3-kinase/akt pathway

21 January 2018

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A mouse model of TSC1 reveals sex-dependent lethality from liver hemangiomas, and up-regulation of p70S6 kinase activity in Tsc1 null cells

21 January 2018

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Rheb GTPase is a direct target of TSC2 GAP activity and regulates mTOR signaling

21 January 2018

1 reference

Tuberous sclerosis complex gene products, Tuberin and Hamartin, control mTOR signaling by acting as a GTPase-activating protein complex toward Rheb

21 January 2018

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Insulin activation of Rheb, a mediator of mTOR/S6K/4E-BP signaling, is inhibited by TSC1 and 2

21 January 2018

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Rheb binds tuberous sclerosis complex 2 (TSC2) and promotes S6 kinase activation in a rapamycin- and farnesylation-dependent manner

21 January 2018

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Rheb is a direct target of the tuberous sclerosis tumour suppressor proteins

21 January 2018

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TSC2 mediates cellular energy response to control cell growth and survival

21 January 2018

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mTOR interacts with raptor to form a nutrient-sensitive complex that signals to the cell growth machinery

21 January 2018

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Raptor, a binding partner of target of rapamycin (TOR), mediates TOR action

21 January 2018

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Genetics: influence of TOR kinase on lifespan in C. elegans

21 January 2018

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Regulation of TORC1 by Rag GTPases in nutrient response

21 January 2018

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Inhibition of the immune response by rapamycin, a new antifungal antibiotic

21 January 2018

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Rapamycin fed late in life extends lifespan in genetically heterogeneous mice

31 March 2020

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Deforolimus (AP23573) a novel mTOR inhibitor in clinical development

31 March 2020

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Rapamycin blocks the phosphorylation of 4E-BP1 and inhibits cap-dependent initiation of translation

31 March 2020

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Rapamycin-mediated FOXO1 inactivation reduces the anticancer efficacy of rapamycin.

31 March 2020

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/22037041

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

First drug-eluting coronary stent approved

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/22037041

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1038/NRD3531

1 reference

25 August 2017

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