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

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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

11

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25 August 2017

868-880

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

25 August 2017

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

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

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

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

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

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

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

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

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Differential requirement of mTOR in postmitotic tissues and tumorigenesis

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

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

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

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

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mTOR inhibition induces upstream receptor tyrosine kinase signaling and activates Akt

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

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

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

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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.

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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

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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

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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

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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

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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

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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

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25 August 2017

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